| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| LY 2940680 - Taladegib | Axon 2196
CAS [1258861-20-9]
MF C26H24F4N6OMW 512.50
Purity:
99%
Soluble in DMSO
Description
Small-molecule antagonist of the Smoothened (SMO) receptor (IC50 value 2.4 nM), a key signal transducer in the hedgehog signalling pathway, responsible for the maintenance of normal embryonic development and implicated in carcinogenesis. LY 2940680 lacks an undesired inhibitory effect on CYP3A4.
References
Certificates
Categories
Extra info
C. Wang et al. Structure of the human smoothened receptor bound to an antitumour agent. Nature. 2013, 497, 338-343.
P.A. Hipskind et al. Preparation of disubstituted phthalazine derivatives for use as hedgehog pathway antagonists and useful in treatment of cancer. PCT Int. Appl. WO 2010147917 A1 20101223.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Small-molecule antagonist of the Smoothened (SMO) receptor
Chemical name
4-fluoro-N-methyl-N-(1-(4-(1-methyl-1H-pyrazol-5-yl)phthalazin-1-yl)piperidin-4-yl)-2-(trifluoromethyl)benzamide
Parent CAS No.
[1258861-20-9]
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Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| Purmorphamine | Axon 1690
CAS [483367-10-8]
MF C31H32N6O2MW 520.62
Purity:
99%
Soluble in DMSO
Description
Hedgehog (Hh) agonist that directly targets Smoothened (SMO) transmembrane protein. Purmorphamine up-regulates gene expression of mediators of Hh pathway, SMO, PTCH1, GLI1, and GLI2, and induces osteoblast differentiation of multipotent mesenchymal progenitor cells and lineage-committed preosteoblasts.
References
Certificates
Categories
Extra info
S. Sinha et al. Purmorphamine activates the Hedgehog pathway by targeting Smoothened. Nat. Chem. Biol. 2006, 2, 29-30.
F.S. Oliveira et al. Hedgehog signaling and osteoblast gene expression are regulated by purmorphamine in human mesenchymal stem cells. J. Cell. Biochem. 2012, 113, 204–208.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
Smoothened (SMO)
Hedgehog
F
Stem Cell Differentiator
Hedgehog signaling pathway activator
Chemical name
9-cyclohexyl-N-(4-morpholinophenyl)-2-(naphthalen-1-yloxy)-9H-purin-6-amine
Parent CAS No.
[483367-10-8]
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Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| NVP-LDE225 - LDE 225 | Sonidegib | Erismodegib | Axon 1619
CAS [956697-53-3]
MF C26H26F3N3O3MW 485.50
Purity:
98%
Soluble in DMSO
Description
Potent, selective and orally bioavailable Smoothened (SMO) antagonist (IC50: 50 nM); it inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO)
References
Certificates
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Extra info
S Pan et al. Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist. ACS Med. Chem. Lett., 2010, 1 (3), pp 130–134.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Smoothened (SMO) antagonist
Chemical name
N-(6-((2S,6R)-2,6-dimethylmorpholino)pyridin-3-yl)-2-methyl-4'-(trifluoromethoxy)biphenyl-3-carboxamide
Parent CAS No.
[956697-53-3]
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Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| SSR 125543A - SSR 125543 hydrochloride | Axon 1799
CAS [321839-75-2 ]
MF C27H28ClFN2OS.HClMW 519.50
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, selective, and orally active corticotropin-releasing factor 1 receptor (CRF1) antagonist (pKi values of 8.73 and 9.08 for human cloned or native CRF1 receptors, respectively) with antidepressant-like and anxiolytic-like effects in the Flinders Sensitive Line rats. SSR 125543A shows a 1000-fold selectivity for CRF1 versus CRF2α receptor and CRF binding protein, has a long duration of action, and readily crosses the blood-brain barrier.
References
Certificates
Categories
Extra info
A. Urani et al. The corticotropin-releasing factor 1 receptor antagonist, SSR125543, and the vasopressin 1b receptor antagonist, SSR149415, prevent stress-induced cognitive impairment in mice. Pharmacol. Biochem. Behav. 2011, 98, 425-431.
D.H. Overstreet et al. Antidepressant-like effects of CRF1 receptor antagonist SSR125543 in an animal model of depression. Eur. J. Pharmacol. 2004, 497, 49-53.
C.Q. Huang et al. Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists. Bioorg. Med. Chem. Lett. 2004, 14, 2083-2086.
G. Gully et al. 4-(2-Chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]5-methyl-N-(2-propynyl)-1,3-thiazol-2-amine hydrochloride (SSR125543A).... J. Pharmacol. Exp. Ther. 2002, 301, 322-332.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
CRF1
B1
Potent, selective, and orally active corticotropin-releasing factor 1 receptor (CRF1) antagonist
Chemical name
(S)-4-(2-chloro-4-methoxy-5-methylphenyl)-N-(2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl)-5-methyl-N-(prop-2-ynyl)thiazol-2-amine hydrochloride
Parent CAS No.
[752253-39-7]
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Size
Unit Price
Stock
5 mg
€160.00
In Stock | | axonmedchem |
| PF 5274857 hydrochloride - PF 05274857 hydrochloride | Axon 2027
CAS [1373615-35-0]
MF C20H25ClN4O3S.HClMW 473.42
Purity:
99%
Soluble in water and DMSO
Description
Potent and selective smoothened (SMO) antagonist with Ki value of 4.6 nM; a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway
References
Certificates
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Extra info
A Rohner et al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Mol Cancer Ther. 2012, 11(1), 57-65.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Pfizer Licensed Products
Smoothened (SMO) antagonist
Chemical name
1-(4-(5'-chloro-3,5-dimethyl-2,4'-bipyridin-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one hydrochloride
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1373615-35-0]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MRT 10 | Axon 1938
CAS [330829-30-6]
MF C24H23N3O5SMW 465.52
Purity:
99%
Soluble in DMSO
Description
Smoothened (SMO) receptor antagonist
References
Certificates
Categories
Extra info
F Manetti et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010, 78(4), 658-665.
A Solinas et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J. Med. Chem. 2012, 55(4), 1559-1571.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Smoothened (SMO) receptor antagonist
Chemical name
N-(3-benzamidophenylcarbamothioyl)-3,4,5-trimethoxybenzamide
Parent CAS No.
[330829-30-6]
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Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| GDC 0449 - Vismodegib | HhAntag 691 | Axon 1500
CAS [879085-55-9]
MF C19H14Cl2N2O3SMW 421.30
Purity:
99%
Soluble in DMSO
Description
The first-in-class inhibitor of Hedgehog (Hh) signaling pathway; more specifically, an orally bioavailable and potent inhibitor of smoothened homologue (SMO); an investigational anti-cancer drug for Medulloblastoma, advanced basal cell skin cancer etc
References
Certificates
Categories
Extra info
CM Rudin et al. Treatment of Medulloblastoma with Hedgehog Pathway Inhibitor GDC-0449. N. Engl. J. Med. 2009, 361, 1173-8.
SJ Scales and FJ de Sauvage. Mechanisms of Hedgehog pathway activation in cancer and implications for therapy. Trends Pharmacol. Sci. 2009, 30(6), 303-312.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Stem Cell
Smoothened (SMO)
Hedgehog
F
Hedgehog (Hh) pathway inhibitor
Chemical name
2-Chloro-N-(4-chloro-3-pyridin-2-yl-phenyl)-4-methanesulfonyl-benzamide
Parent CAS No.
[879085-55-9]
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Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| Antalarmin hydrochloride | Axon 1321
CAS [220953-69-5 ]
MF C24H34N4.HClMW 415.01
Purity:
99%
Soluble in DMSO
Description
Non-peptide CRF1 corticotropin-releasing factor receptor antagonist
References
Certificates
Categories
Extra info
EL Webster et al. In vivo and in vitro characterization of antalarmin, a nonpeptide corticotropin-releasing hormone (CRH) receptor antagonist: suppression of pituitary ACTH release and peripheral inflammation. Endocrinology, 1996, 137, 5747-5750.
EM Jutkiewicz et al. The effects of CRF antagonists, antalarmin, CP154,526, LWH234, and R121919, in the forced swim test and on swim-induced increases in adrenocorticotropin in rats. Psychopharmacology (Berl). 2005, 180(2), 215-223.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
CRF1
B1
CRF1 antagonist
Chemical name
Butyl-ethyl-[2,5,6-trimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-amine hydrochloride
Parent CAS No.
[157284-96-3]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| CP 154526 hydrochloride | Axon 1116
CAS [257639-98-8]
MF C23H32N4.HClMW 400.99
Purity:
99%
Soluble in DMSO and Ethanol
Description
Corticotropin-releasing factor CRF1 antagonist
References
Certificates
Categories
Extra info
SPH Alexander et al. Guide to Receptors and Channels (GRAC), 2nd edition (2007 revision). Br. J. Pharmacol. 2007, 150 (Suppl. 1), S1–S168.
Lundkist et al. A non peptidic corticotropin releasing factor receptor antagonist attenuates fever and exhibits anxiolytic activity. Eur. J. Pharmacol. 1996, 309, 195.
Schulz et al. CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors. Proc. Natl. Acad. Sci. USA 1996, 93 10477.
Hodgson et al. Comparison of the V1b antagonist, SSR149415, and the CRF1 antagonist, CP-154,526, in rodent models of anxiety and depression. Pharmacol. Biochem. Behav. 2007, 86, 431.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
Endocrinology
CRF1
B1
CRF1 antagonist
Chemical name
Butyl-[2,5-dimethyl-7-(2,4,6-trimethyl-phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]-ethyl-amine hydrochloride
Parent CAS No.
[157286-86-7]
Order
Size
Unit Price
Stock
10 mg
€115.00
In Stock | | axonmedchem |
| iCRT14 - CRT Inhibitor iCRT14 | Axon 2135
CAS [677331-12-3]
MF C21H17N3O2SMW 375.44
Purity:
98%
Soluble in DMSO
Description
Small-molecule inhibitor of the Wnt/wingless signaling pathway (IC50 value 40 nM in a Wnt responsive STF16-luc reporter assay) that antagonizes the transcriptional function of nuclear β-catenin, and inhibits direct interactions between β-cat and TCF4. iCRT 14 exhibits specific cytotoxicity towards human colon tumor biopsy cultures as well as colon cancer cell lines that exhibit deregulated Wnt signaling. Similar mode of action as iCRT5 (Axon 2133)
References
Certificates
Categories
Extra info
FC Gonsalves et al. An RNAi-based chemical genetic screen identifies three small-molecule inhibitors of the Wnt/wingless signaling pathway. Proc Natl Acad Sci USA 2011, 108, 5954-5963.
BA Narayanan et al. Antagonistic Effect of Small-molecule Inhibitors of Wnt/β-catenin in Multiple Myeloma. Anticancer Res. 2012, 32(11), 4697-4707.
JN Anastas & RT Moon. WNT signalling pathways as therapeutic targets in cancer. Nat. Rev. Cancer 2013, 13, 11-26.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
β-Catenin
Wnt-β-Catenin
Wnt
Small-molecule inhibitor of the Wnt/wingless signaling pathway; CRT inhibitor
Chemical name
5-((2,5-dimethyl-1-(pyridin-3-yl)-1H-pyrrol-3-yl)methylene)-3-phenylthiazolidine-2,4-dione
Parent CAS No.
[677331-12-3]
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Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| WAY 316606 hydrochloride | Axon 2325
CAS [915759-45-4 (parent)]
MF C18H19F3N2O4S2.HClMW 484.94
Purity:
99%
Soluble in DMSO
Description
Potent and water soluble inhibitor of secreted Frizzled-Related Protein I (sFRP-1; Kd value 0.08 μM and EC50 value 0.65 μM for Wnt-luciferase activity from U2-OS cells) that stimulates the Wnt/β-catenin canonical signaling pathway. WAY316606 increased total bone area in a murine calvarial organ culture assay at concentrations as low as 0.0001 μM. WAY-316606 also bound to sFRP-2, albeit over 10 times weaker (Kd value 1.0 μM) and shows moderate to low inhibition of cytochrome p450 isozymes (3A4, 2D6, 2C9) and good stability in rat and human liver microsomes (t1/2 > 60 min in each species).
This product is not intended/sold for (self-)diagnostic and/or therapeutic use.
References
Certificates
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Extra info
W.J. Moore et al. Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides. J Med Chem. 2009 Jan 8;52(1):105-16.
W.J. Moore et al. Modulation of Wnt signaling through inhibition of secreted frizzled-related protein I (sFRP-1) with N-substituted piperidinyl diphenylsulfonyl sulfonamides: part II. Bioorg Med Chem. 2010 Jan 1;18(1):190-201.
P.V. Bodine et al. A small molecule inhibitor of the Wnt antagonist secreted frizzled-related protein-1 stimulates bone formation. Bone. 2009 Jun;44(6):1063-8.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cardiovascular
Cell Cycle Regulation
Cell Signaling & Oncology
CNS
Wnt-β-Catenin
Wnt
Potent inhibitor of sFRP-1 that stimulates Wnt signaling
Chemical name
5-(phenylsulfonyl)-N-(piperidin-4-yl)-2-(trifluoromethyl)benzenesulfonamide hydrochloride
Parent CAS No.
[915759-45-4]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| Cannabidiol, Abnormal - Abn-CBD | Axon 1235
CAS [22972-55-0]
MF C21H30O2MW 314.46
Purity:
98%
Soluble in DMSO
Description
A regioisomer of cannabidiol without psychotropic activity; inactive at CB1 or CB2 receptors. However, it activates a third type of non-CB1/CB2 endo-cannabinoid receptor. Mechanism is under study
References
Certificates
Categories
Extra info
Z Járai et al. Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors. Proc. Natl. Acad. Sci. USA 1999, 96(24), 14136-14141.
L Walter et al. Nonpsychotropic cannabinoid receptors regulate microglial cell migration. J. Neurosci. 2003, 23(4), 1398-1405.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GPR55
A15
Cannabinoid agonist
Chemical name
4-((1R,6R)-6-Isopropenyl-3-methyl-cyclohex-2-enyl)-5-pentyl-benzene-1,3-diol
Parent CAS No.
[22972-55-0]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| Cannabidiol - CBD | Axon 1234
CAS [13956-29-1]
MF C21H30O2MW 314.46
Purity:
97%
Soluble in DMSO
Description
Cannabidiol does not bind to CB1 or CB2 receptors but it does block the effects of cannabinoid agonists by an unknown indirect way. Recently it was found to be an antagonist at the putative new cannabinoid receptor, GPR55, a GPCR expressed in the caudate nucleus and putamen; a promising therapeutic agent for the treatment of psychosis, hyperalgesia, seizures, and stroke
References
Certificates
Categories
Extra info
A Thomas et al. Cannabidiol displays unexpectedly high potency as an antagonist of CB1 and CB2 receptor agonists in vitro. Br. J. Pharmacol. 2007,150 (5), 613–23.
E Ryberg et al. The orphan receptor GPR55 is a novel cannabinoid receptor. Br. J. Pharmacol. 2007, 152, 1092–1101.
LE Long et al. The pharmacological actions of cannabidiol. Drugs Fut. 2005, 30(7), 747-753.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GPR55
A15
GPR55 antagonist
Chemical name
2-((1R,6R)-6-Isopropenyl-3-methyl-cyclohex-2-enyl)-5-pentyl-benzene-1,3-diol
Parent CAS No.
[13956-29-1]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| KYA1797K | Axon 2668
CAS [1956356-56-1]
MF C17H11KN2O6S2MW 442.51
Purity:
99%
Soluble in DMSO
Description
Promotor of β-catenin and Ras degradation (IC50 value 0.75 μM for inhibition of TOPflash activity) that effectively suppresses the growth of CRCs (colorectal cancers) harboring APC and KRAS mutations in vitro and in vivo. KYA1797K binds the RGS domain of axin and enhances the binding affinity of β-catenin or Ras with the β-catenin destruction complex components, leading to simultaneous destabilization of β-catenin and Ras via GSK3β activation. KYA1797 also inhibits ASK1 (IC50 value 0.65 μM for inhibition of apoptosis signal-regulating kinase 1).
KEYWORDS: KYA1797K | supplier | dual ASK1 and Wnt/β-catenin inhibitor | KYA 1797K | CAS [1956356-56-1] | [ 851304-36-4] | Wnt Inhibitor | Axin | Axin1 | RGS domain | Ras | GSK3β activation | ASK1 | apoptosis signal-regulating kinase 1 | colorectal cancer | CRC | APC | | axonmedchem |
| SMT C1100 - Ezutromid | BMN-195 | Axon 2481
CAS [945531-77-1]
MF C19H15NO3SMW 337.39
Purity:
99%
Soluble in DMSO
Description
Orally active, non-toxic upregulator of utrophin production (EC50 value 0.91 µM in a utrophin A promoter H2K cell-based assay with a luciferase reporter readout) for the treatment of Duchenne muscular dystrophy (DMD). What's more, SMT C1100 significantly reduces dystrophin-deficient muscle pathology in vivo.
KEYWORDS: SMT C1100 | supplier | Utrophin upregulator | Ezutromid | BMN-195 | SMTC1100 | BMN195 | CAS [945531-77-1] | ECM-adhesion | Utrophin | Upregulator | matrix | adhesion | Duchenne | muscular | dystrophy | DMD | | axonmedchem |
| AZD 1080 | Axon 2171
CAS [612487-72-6]
MF C19H18N4O2MW 334.37
Purity:
98%
Soluble in DMSO
Description
Potent and selective inhibitor of Glycogen synthase kinase 3 (GSK-3), with Ki values of 6.9 nM and 31 nM for GSK-3α and GSK-3β respectively. In phase 1 clinical studies, AZD 1080 inhibits tau phosphorylation in cells expressing human tau and in intact rat brain. Interestingly, subchronic but not acute administration with AZD 1080 reverses MK-801-induced deficits, measured by long-term potentiation in hippocampal slices and in a cognitive test in mice.
References
Certificates
Categories
Extra info
B Georgievska et al. AZD1080, a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans. J Neurochem. 2013, 125, 446-456.
H Eldar-Finkelman et al. GSK-3 Inhibitors: Preclinical and Clinical Focus on CNS. Front. Mol. Neurosci. 2011, 4, 32..
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
Selective inhibitor of GSK-3α and GSK-3β
Chemical name
2-Hydroxy-3-(5-(morpholinomethyl)pyridin-2-yl)-1H-indole-5-carbonitrile
Parent CAS No.
[612487-72-6]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| AR-A 014418 | Axon 2167
CAS [487021-52-3]
MF C12H12N4O4SMW 308.31
Purity:
99%
Soluble in DMSO
Description
Specific glycogen synthase kinase GSK-3 inhibitor; ATP-competitive
References
Certificates
Categories
Extra info
R Bhat et al. Structural insights and biological effects of glycogen synthase kinase 3-specific inhibitor AR-A014418. J. Biol. Chem. 2003, 278(46), 45937-45945.
TD Gould et al. AR-A 014418, a selective GSK-3 inhibitor, produces antidepressant-like effects in the forced swim test. Int. J. Neuropsychopharmacol. 2004, 7(4), 387-390.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
ATP-competitive GSK-3 inhibitor
Chemical name
1-(4-methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea
Parent CAS No.
[487021-52-3]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| A 1070722 | Axon 1909
CAS [1384424-80-9]
MF C17H13F3N4O2MW 362.31
Purity:
99%
Soluble in DMSO
Description
Potent and selective glycogen synthase kinase GSK-3 inhibitor (Ki=6 nM). Brain penetrating and centrally active GSK-3 inhibitor for the treatment of psychiatric and neurodegenerative disorders
References
Certificates
Categories
Extra info
MHM Bakker et al. A-1070722, a potent, selective, and centrally active glycogen synthase kinase-3 (GSK-3) inhibitor for the treatment of psychiatric and neurodegenerative disorders. Society for Neuroscience 2011, Abstract 568.04.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
Selective inhibitor of GSK-3
Chemical name
1-(7-methoxyquinolin-4-yl)-3-(6-(trifluoromethyl)pyridin-2-yl)urea
Parent CAS No.
[1384424-80-9]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Kartogenin - KGN | Axon 2378
CAS [4727-31-5]
MF C20H15NO3MW 317.34
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Small molecule promoting robust chondrocyte differentiation from primary human mesenchymal stem cells (MSCs; EC50 value 100 nM). Kartogenin (KGN) treatment of bone marrow stromal cells (BMSCs) induced the expresion of both Col. II and aggrecan in a dose-dependent manner, and upregulates Sox-9 gene expression. KGN does not alter either MMP-3, MMP-13, or aggrecanase expression in primary chondrocytes and MSCs. KGN may be used to enhance tendon/bone interface healing through the direct, local delivery of KGN injections into the gap between the tendon graft and the bone surface during ACL reconstruction.
References
Certificates
Categories
Extra info
K. Johnson et al. A stem cell-based approach to cartilage repair. Science. 2012, 336, 717-721.
J. Zhang et al. Kartogenin induces cartilage-like tissue formation in tendon-bone junction. Bone Res. 2014, 2, pii: 14008.
M.L. Kang et al. Intra-articular delivery of kartogenin-conjugated chitosan nano/microparticles for cartilage regeneration. Biomaterials. 2014, 35, 9984-9994.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Pain & Inflammation
Stem Cell
Stem Cell Differentiator
Aggrecan
Collagen
SOX-9
Promotor of chondrocyte differentiation from primary human MSCs
Chemical name
2-(biphenyl-4-ylcarbamoyl)benzoic acid
Parent CAS No.
[4727-31-5]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| TWS 119 | Axon 1562
CAS [601514-19-6]
MF C18H14N4O2MW 318.33
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of GSK-3β subtype (GSK-3β) (IC50: 30 nM); Neurogenesis inducer in murine ESC and thus a useful tool to regulate stem cell self-renewal and differentiation
References
Certificates
Categories
Extra info
Dessalew et al. Investigation of potential glycogen synthase kinase 3 inhibitors using pharmacophore mapping and virtual screening. Chem. Biol. Drug Design 2006, 68, 154-165.
S Ding et al. Synthetic small molecules that control stem cell fate. PNAS USA. 2003, 100(13), 7632-7637.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
Stem Cell Differentiator
GSK-3β inhibitor
Chemical name
3-[6-(3-Amino-phenyl)-7H-pyrrolo[2,3,-d]pyrimidin-4-yloxy]-phenol
Parent CAS No.
[601514-19-6]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| SB 216763 | Axon 1303
CAS [280744-09-4]
MF C19H12Cl2N2O2MW 371.22
Purity:
99%
Soluble in DMSO
Description
Potent and selective glycogen synthase kinase-3 (GSK-3) inhibitor
References
Certificates
Categories
Extra info
L Facci et al. Glycogen synthase kinase-3 inhibitors protect central neurons against excitotoxicity. Neuroreport. 2003, 14(11), 1467-1470.
Q Wang et al. Glycogen synthase kinase-3 is a negative regulator of extracellular signal-regulated kinase. Oncogene 2006, 25, 43–50.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
PI3K-Akt-mTOR
EC 2.7.11.26
GSK-3 inhibitor
Chemical name
3-(2,4-Dichloro-phenyl)-4-(1-methyl-1H-indol-3-yl)-pyrrole-2,5-dione
Parent CAS No.
[280744-09-4]
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Size
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10 mg
€85.00
In Stock | | axonmedchem |
| Palmitoylethanolamide | Axon 1211
CAS [544-31-0]
MF C18H37NO2MW 299.49
Purity:
98%
Soluble in Ethanol
Description
A putative endocannabinoid; selective GPR55 agonist
References
Certificates
Categories
Extra info
V di Marzo et al. Palmitoylethanolamide inhibits the expression of fatty acid amide hydrolase and enhances the anti-proliferative effect of anandamide in human breast cancer cells. Biochem. J. 2001, 358, 249-255.
S Conti et al. Antiinflammatory action of endocannabinoid palmitoylethanolamide and the synthetic cannabinoid nabilone in a model of acute inflammation in the rat. Br. J. Pharmacol. 2002, 135, 181-187.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
GPR55
A15
Endocannabinoid; GPR55 agonist
Chemical name
Hexadecanoic acid (2-hydroxy-ethyl)-amide
Parent CAS No.
[544-31-0]
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Size
Unit Price
Stock
20 mg
€75.00
In Stock | | axonmedchem |
| SB 525334 | Axon 2285
CAS [356559-20-1]
MF C21H21N5MW 343.42
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of the ALK5 receptor (IC50 value 14.3 nM). SB 525334 is approximately 4-fold less potent as an inhibitor of ALK4, and inactive as an inhibitor of ALK2, ALK3, and ALK6.
In cell-based assays, SB 525334 blocked TGF-β1-induced phosphorylation and nuclear translocation of Smad2/3 in renal proximal tubule cells and inhibited TGF-β1-induced increases in plasminogen activator inhibitor-1 (PAI-1) and procollagen alpha1(I) mRNA expression in renal epithelial carcinoma cells.
References
Certificates
Categories
Extra info
O. Fuchs. Inhibition of TGF-β signaling for the treatment of tumor metastasis and fibrotic diseases. Curr. Signal Trans. Ther. 2011, 6, 29-43.
N.J. Laping et al. Tumor-Specific Efficacy of Transforming Growth Factor-βRI Inhibition in Eker Rats. Clin. Cancer Res. 2007, 13, 3087-3099.
E.T. Grygielko et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J. Pharmacol. Exp. Ther. 2005, 313, 943-951.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
TGF-βR
Potent and selective inhibitor of the TGF-βR1 (ALK5) receptor
Chemical name
6-(2-tert-butyl-5-(6-methylpyridin-2-yl)-1H-imidazol-4-yl)quinoxaline
Parent CAS No.
[356559-20-1]
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Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| UK 383367 | Axon 2073
CAS [348622-88-8]
MF C15H24N4O4MW 324.38
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of bone morphogenetic protein 1 (BMP-1; also known as procollagen C proteinase, PCP) with IC50 values of 44 nM for BMP-1 and >10.000 nM for a range of other proteolytic matrix metalloproteinases MMP-1, 2, 3, 9, and 14.
References
Certificates
Categories
Extra info
PV Fish et al. Potent and Selective Nonpeptidic Inhibitors of Procollagen C-Proteinase. J. Med. Chem. 2007, 50, 3442-3456.
GA Allan et al. Pharmacokinetics and metabolism of UK-383,367 in rats and dogs: a rationale for long-lived plasma radioactivity. Xenobiotica. 2006, 36, 399-418.
S Bailey et al. Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents. Bioorg. Med. Chem. Lett. 2008, 18, 6562-6567.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.19
MMP
Pfizer Licensed Products
Inhibitor of bone morphogenetic protein 1 (BMP-1, aka PCP)
Chemical name
(R)-5-(6-cyclohexyl-1-(hydroxyamino)-1-oxohexan-3-yl)-1,2,4-oxadiazole-3-carboxamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[348622-88-8]
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Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| ADAMTS-5 inhibitor - Compound 12 | Axon 2083
CAS [929634-33-3]
MF C16H11ClF3N3OS3MW 449.92
Purity:
100%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Inhibitor of ADAMTS-5 (A Disintegrin And Metalloproteinase with ThromboSpondin motifs 5 or aggrecanase-2; IC50 1.1 μM) with >40-fold functional selectivity over ADAMTS-4. ADAMTS-5 is involved in the catabolism of aggrecan and collagen in the articular cartilage matrix during Osteoarthritis (OA).
References
Certificates
Categories
Extra info
A.M. Gilbert et al. 5-((1H-Pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5. Bioorg. Med. Chem. Lett. 2007, 17, 1189–1192.
J. Bondeson et al. The regulation of the ADAMTS4 and ADAMTS5 aggrecanases in osteoarthritis: a review. Clin. Exp. Rheumatol. 2008, 26, 139-145.
Certificate of Analysis
Material Safety Data Sheet
Pain & Inflammation
ADAMTS-5
EC 3.4.24
Selective inhibitor of ADAMTS-5 (aggrecanase-2)
Chemical name
(Z)-5-((5-(4-chlorobenzylthio)-1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one
Parent CAS No.
[929634-33-3]
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Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| ML348 | Axon 2646
CAS [899713-86-1]
MF C18H17ClF3N3O3MW 415.79
Purity:
99%
Soluble in DMSO
Description
Selective and in vivo active inhibitor for acyl-protein thioesterase APT1 (IC50 values 0.84 µM and >10 µM for APT1 and APT2, respectively; Ki values 280 nM and >10000 nM for WT APT1 and APT2, respectively). A useful tool to study LYPLA/APT mediated protein S-palmitoylation and related pharmacology. In some of the literature, APT1 and APT2 are also identified as lysophospholipases LYPLA1 and LYPLA2 as they were first discovered due to their ability to hydrolyze various lysophospholipids.
KEYWORDS: ML348 | supplier | APT1 inhibitor | ML-348 | CAS [899713-86-1] | S-palmitoylated proteins | APT | acyl-protein thioesterase | LYPLA | APT2 | LYPLA1 | LYPLA2 | lysophospholipids | | axonmedchem |
| SIS3 - Smad3 inhibitor SIS3 | Axon 2764
CAS [521985-36-4]
MF C28H27N3O3MW 453.53
Purity:
98%
Soluble in DMSO
Description
SIS3 is a potent and selective inhibitor of Smad3 and TGF-β signaling. Inhibition by SIS3 leads to abrogation of the TGF-β1-induced production of extracellular matrix proteins in normal fibroblasts and scleroderma fibroblasts. Moreover, Smad3 inhibition attenuates resistance to anti-HER2 drugs in HER2-positive breast cancer cells.
KEYWORDS: SIS3 | supplier | Smad3 inhibitor | Smad3 inhibitor SIS3 | SIS-3 | SIS 3 | CAS [521985-36-4] | DNA-RNA | Smad3 | Inhibitor | Transcription Factors | TGF-β | Breast Cancer | HER2 | | axonmedchem |
| PTIQ | Axon 2328
CAS [1032822-42-6]
MF C13H17NO3MW 235.28
Purity:
99%
Soluble in 0.1N NaOH(aq), DMSO, and Ethanol
Description
Brain penetrating neuroprotectant that attenuates MPTP induced motor deficits, prevents neurodegeneration and suppresses microglial activation in the substantia nigra. Mechanistically, PTIQ effectively suppresses expression of MMP-3 (IC50 value 60 nM in stressed dopaminergic cells), and NO production (IC50 value <100 µM in LPS stimulated BV-2 cells). PTIQ also inhibits IL-1β, TNF-α (IC50 value 6.5 µM) and COX-2 (IC50 value 9.3 µM) and blocked nuclear translocation of NF-κB, yet it shows no inhibition of hERG channels or CYP isozyme activities.
References
Certificates
Categories
Extra info
H.J. Son et al. A novel compound PTIQ protects the nigral dopaminergic neurones in an animal model of Parkinson's disease induced by MPTP. Br J Pharmacol. 2012 Apr;165(7):2213-27.
J.W. Seo et al. Syntheses of tetrahydroisoquinoline derivatives that inhibit NO production in activated BV-2 microglial cells. Eur J Med Chem. 2008 Jun;43(6):1160-70.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
CNS
Miscellaneous
Pain & Inflammation
EC 3.4.24.17
MMP
Neuroprotectant with attenuating effects on MMP-3 expression
Chemical name
1-(7-hydroxy-6-methoxy-3,4-dihydroisoquinolin-2(1H)-yl)propan-1-one
Parent CAS No.
[1032822-42-6]
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Size
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Stock
10 mg
€125.00
In Stock | | axonmedchem |
| SB-3CT | Axon 2370
CAS [292605-14-2]
MF C15H14O3S2MW 306.40
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of Gelatinases MMP-2 and MMP-9 (Ki values 13.9 nM and 600 nM, respectively). In contrast, the Ki values of SB-3CT against other MMPs (MMP-1, MMP-3, and MMP-7) are in the micromolar range. SB-3CT protects against brain damage and ameliorates neurological outcome after transient focal cerebral ischemia in mice
References
Certificates
Categories
Extra info
S. Brown et al. Potent and selective mechanism-based inhibition of gelatinases. J. Am. Chem. Soc. 2000, 122, 6799-6800.
F. Jia et al. MMP-9 inhibitor SB-3CT attenuates behavioral impairments and hippocampal loss after traumatic brain injury in rat. J Neurotrauma. 2014, 31, 1225-1234.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.24
MMP
Potent and selective inhibitor of Gelatinases MMP-2 and MMP-9
Chemical name
2-((4-phenoxyphenylsulfonyl)methyl)thiirane
Parent CAS No.
[292605-14-2]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| DDR1-IN-1 | Axon 2265
CAS [1449685-96-4]
MF C30H31F3N4O3MW 552.59
Purity:
98%
Soluble in DMSO
Description
Potent and selective DDR1 receptor tyrosine kinase (RTK) inhibitor (IC50 values 105 and 413 nM for DDR1 and DDR2 respectively); a useful pharmacological probe for DDR1-dependent signal transduction.
References
Certificates
Categories
Extra info
H.G. Kim et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. A.C.S. Chem. Biol. 2014, 9, 840.
P. Canning et al. Structural mechanisms determining inhibition of the collagen receptor DDR1 by selective and multi-targeted type II kinase inhibitors. J. Mol. Biol. 2014, 426, 2457-2470.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
DDR1
RTK class XVI; EC 2.7.10.1
Selective DDR1 receptor tyrosine kinase (RTK) inhibitor
Chemical name
4-((4-Ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide
Parent CAS No.
[1449685-96-4]
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Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| NSC 405020 | Axon 2162
CAS [7497-07-6]
MF C12H15Cl2NOMW 260.16
Purity:
99%
Soluble in DMSO
Description
MT1-MMP inhibitor (IC50>100 μM that specifically targets the hemopexin (PEX) domain. NSC 405020 shows significant antitumor efficacy in in vivo tests after intratumoral injections (0.5 mg/kg), and causes a fibrotic tumor phenotype and increases the level of COL-I.
References
Certificates
Categories
Extra info
A.G. Remacle et al. Novel MT1-MMP small-molecule inhibitors based on insights into hemopexin domain function in tumor growth. Cancer Res. 2012, 72, 2339-2349.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Miscellaneous
Pain & Inflammation
EC 3.4.24.80
MMP
MT1-MMP inhibitor specifically targeting PEX-domain.
Chemical name
3,4-dichloro-N-(pentan-2-yl)benzamide
Parent CAS No.
[7497-07-6]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| LY 2157299 - Galunisertib | Axon 1491
CAS [700874-72-2]
MF C22H19N5OMW 369.42
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally active transforming growth factor β receptor (TGF-βR) kinase inhibitor under clinical development; IC50 values to be 86 nm (TβR1) and 2 nM (TβR2) respectively.
KEYWORDS: LY 2157299 | supplier | TGF-βR2 inhibitor | Galunisertib | LY2157299 | LY-2157299 | CAS [700874-72-2] | TGF-beta | transforming growth factor | TβR1 | TβR2 | antagonist | non-small cell lung cancer | NSCLC | Smad | pSmad | | axonmedchem |
| Daglutril - SLV 306 | Axon 1918
CAS [182821-27-8]
MF C31H38N2O6MW 534.64
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
An orally active, dual endothelin converting enzyme (ECE)/neutral endopeptidase (NEP) inhibitor that reduces proteinuria and urinary albumin excretion in diabetic rats. Simultaneous augmentation of ANP and inhibition of ET-1 production by Daglutril treatment is of potential therapeutic benefit in cardiovascular disease, and for treatment of overt nephropathy and reduction of albuminuria in hypertensive patients with type 2 diabetes.
References
Certificates
Categories
Extra info
C. Thöne-Reinke et al. Inhibition of both neutral endopeptidase and endothelin-converting enzyme by SLV306 reduces proteinuria and urinary albumin excretion in diabetic rats. J. Cardiovasc. Pharmacol. 2004, 44, S76-79.
K. Dickstein et al. Effect of single doses of SLV306, an inhibitor of both neutral endopeptidase and endothelin-converting enzyme, on pulmonary pressures in congestive heart failure. Am. J. Cardiol. 2004, 94, 237-239.
R. Tabrizchi. SLV-306. Solvay. Curr. Opin. Investig. Drugs. 2003, 4, 329-332.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Pain & Inflammation
ECE1
NEP
EC 3.4.24
Orally active, dual ECE/NEP inhibitor
Chemical name
2-((S)-3-(1-((R)-2-(ethoxycarbonyl)-4-phenylbutyl)cyclopentanecarboxamido)-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-1-yl)acetic acid
Parent CAS No.
[182821-27-8]
Order
Size
Unit Price
Stock
2 mg
€125.00
In Stock | | axonmedchem |
| LY 2801653 - Merestinib | Axon 2553
CAS [1206799-15-6]
MF C30H22F2N6O3MW 552.53
Purity:
99%
Soluble in DMSO
Description
Orally bioavailable multi-kinase inhibitor with potent activity against c-MET (IC50 values 35 - 53 nM for cell-based activity), and several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1, DDR2 and against the serine/threonine kinases MKNK1 and MKNK2 (IC50 values 11, 7, 2, 10, 63, 23, 0.1, 7, 7, and 7 nM, respectively). In classic and orthotopic mouse xenograft models of lung cancer, LY2801653 decreased tumor growth, dramatically inhibiting mitotic events and angiogenesis.
KEYWORDS: LY 2801653 | supplier | Multi-kinase (c-MET) inhibitor | Merestinib | LY2801653 | CAS [1206799-15-6] | HGF | c-MET | MST1R | Axl | FLT3 | MERTK | TEK | ROS1 | DDR1 | DDR2 | RTKInhibitor | MKNK1 | MKNK2 | oncoproteins | | axonmedchem |
| CID 11654378 - FMS inhibitor compound 8 | FMS inhibitor compound 1b | Axon 2061
CAS [885704-21-2]
MF C23H30N6OMW 406.52
Purity:
99%
Soluble in DMSO
Description
A highly potent FMS kinase inhibitor (IC50 = 0.8 nM); a proof-of-concept candidate in a collagen-induced model of arthritis in mice
References
Certificates
Categories
Extra info
CR Illig et al. Discovery of novel FMS kinase inhibitors as anti-inflammatory agents. Bioorg. Med. Chem. Lett. 2008, 18(5), 1642-1648.
SK Meegalla et al. Structure-based optimization of a potent class of arylamide FMS inhibitors. Bioorg. Med. Chem. Lett. 2008, 18(12), 3632-3637.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Pain & Inflammation
FMS
RTK class III; EC 2.7.10.1
Potent FMS kinase inhibitor
Chemical name
4-cyano-N-(4-(4-methylpiperazin-1-yl)-2-(4-methylpiperidin-1-yl)phenyl)-1H-pyrrole-2-carboxamide
Parent CAS No.
[885704-21-2]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| LDN 212854 trihydrochloride | Axon 2201
CAS [2109414-80-2]
MF C25H22N6.3HClMW 515.87
Purity:
99%
Soluble in water and DMSO
Description
Potent ALK2-biased BMP type I receptor kinase inhibitor (IC50 values 2.4 nM, 1.3 nM, and 85.8 nM for ALK1, 2, and 3 resp.), showing nearly 4 orders of selectivity for BMP versus the closely related TGF-β and Activin type I receptors. Closely related to LDN 193189 (Axon 1509).
KEYWORDS: LDN 212854 trihydrochloride | supplier | BMP inhibitor | LDN212854 | LDN-212854 | CAS [2109414-80-2] | [1432597-26-6] | TGF-β | BMP-ALK | ALK | type I | dorsomorphin | ALK2 | ALK-2 | ALK1 | ALK3 | bone morphogenetic protein | Antagonist | Receptors | | axonmedchem |
| K 02288 | Axon 2189
CAS [1431985-92-0]
MF C20H20N2O4MW 352.38
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and highly selective inhibitor of BMP signaling, with low nanomolar IC50 values of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6 respectively and IC50s of 34.4, 302, 321 and 220 nM for other ALKs (3, 4, 5) and ActRIIA respectively.K02288 specifically inhibited the BMP-induced Smad pathway without affecting TGF-β signaling and induced dorsalization of zebrafish embryos. K02288 provides a useful tool to investigate BMP signaling and to research into stem cell biology and disease models of anemia, musculoskeletal dysplasia and cancer.
References
Certificates
Categories
Extra info
C.E. Sanvitale et al. A New Class of Small Molecule Inhibitor of BMP Signaling. PLoS One. 2013, 8, e62721.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Stem Cell
TGF-β
RSTK class I; EC 2.7.11.30
BMP-ALK
Inhibitor of BMP signaling. Inhibits ALK1, 2, and 6
Chemical name
3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol
Parent CAS No.
[1431985-92-0]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| Quininib | Axon 2620
CAS [143816-42-6]
MF C17H13NOMW 247.29
Purity:
99%
Soluble in DMSO
Description
Antagonist of the cysteinyl leukotriene receptor 1 and 2 (CysLT1-2; IC50 values 1.4 μM and 38.5 μM, respectively). Quininib robustly inhibits developmental angiogenesis in zebrafish (at 4-10 μM), and significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice, independently of VEGF receptors. Moreover, using ex vivo human CRC explants, Quininib significantly reduced the secretions of angiogenic growth factors and inflammatory cytokines IL-6, IL-8, VEGF, ENA-78, GRO-α, TNF, IL-1β and MCP-1.
KEYWORDS: Quininib | supplier | CysLT antagonist | 2-[(E)-2-(Quinolin-2-yl)vinyl]phenol | CAS [143816-42-6] | Cysteinyl leukotrienes | CysLT1 | CysLT2 | GPCR | VEGF | angiogenesis | LTD4 | LTE4 | blood vessels | retina | ocular | colorectal cancer | CRC | | axonmedchem |
| GW 2580 | Axon 2571
CAS [870483-87-7]
MF C20H22N4O3MW 366.41
Purity:
99%
Soluble in DMSO
Description
An orally bioavailable inhibitor of c-FMS kinase (IC50 value of 0.03 µM in vitro) and the CSF1R receptor (Kd value 1.6 nM) that competitively blocks the ATP binding site of c-FMS. GW 2580 was inactive against 26 kinases in vitro and did not inhibit the growth of mouse NS0 lymphoblastoid cells, human fibroblasts, human endothelial cells, and five human tumor cell lines. GW 2580 also interacts with TrkA, TrkB, and TrkC (Kd values 630 nM, 36 nM, and 120 nM, respectively)
KEYWORDS: GW 2580 | supplier | dual cFMS kinase/CSF1R inhibitor | GW2580 | GW-2580 | CAS [870483-87-7] | FLT3LG | FMS | Inhibitor |RTK| c-FMS| CSF1R | FLT3 | ATP binding site | TrkA | TrkB | TrkC | | axonmedchem |
| R 428 dihydrochloride - BGB324 | Bemcentinib | Axon 1946
CAS [N.A.]
MF C30H34N8.2HClMW 579.57
Purity:
99%
Optical purity:
99% ee
Soluble in water and DMSO
Description
Potent and selective inhibitor of Axl receptor tyrosine kinases (IC50: 14 nM); R428 inhibits Axl kinase and blocks Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.
Note: The hydrochloride salt of R428 is water-soluble and has an improved solubility in DMSO in comparison with its free base
KEYWORDS: R 428 dihydrochloride | supplier | Axl inhibitor | BGB324 | R428 HCl | R-428 | BGB-324 | CAS [1037624-75-1] | Gas6 | Axl | receptor tyrosine kinase | RTK | Akt | breast cancer | proinflammatory | cytokine production | | axonmedchem |
| AMG 208 | Axon 1916
CAS [1002304-34-8]
MF C22H17N5O2MW 383.40
Purity:
99%
Read COA for solubility
Description
Potent and selective inhibitor of c-MET receptor tyrosine kinase (RTK); AMG208 inhibits both ligand-dependent and ligand-independent c-MET activation. Inhibition of c-Met signaling with AMG 208 provides a potential mechanism for blocking tumor growth and survival
References
Certificates
Categories
Extra info
B.K. Albrecht et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J. Med. Chem. 2008, 51, 2879-2882.
A.A. Boezio et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg. Med. Chem. Lett. 2009, 19, 6307-6312.
X. Liu et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol. Med. 2010, 16, 37-45.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
c-MET
RTK class X; EC 2.7.10.1
Inhibitor of c-MET receptor tyrosine kinase (RTK)
Chemical name
7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methylphenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline
Parent CAS No.
[1002304-34-8]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Ensemble Compound 159 | Axon 2800
CAS [1449208-36-9]
MF C42H51ClN6O6MW 771.34
Purity:
97%
Optical purity:
Optically pure
Description
Ensemble Compound 159 is a peptide inhibitor of IL-17A. Ensemble Compound 159 binds to IL-17A and/or inhibits formation of the IL-17A–IL-17RA complex through an ELISA assay, an HT29-GROα cell based functional assay, a rheumatoid arthritis synovial fibroblast (RASF) assay, and surface plasmon resonance (SPR, Kd < 100 nM) based biophysical binding assessment. Moreover, Ensemble Compound 159 was reported to have efficacy in vivo.
KEYWORDS: Ensemble Compound 159 | supplier | IL-17A inhibitor | Cp159 | Cp-159 | Cp 159 | CAS [1449208-36-9] | Interleukin | IL-17 | Inhibitor | | axonmedchem |
| Amuvatinib - MP 470 | Axon 2368
CAS [850879-09-3]
MF C23H21N5O3SMW 447.51
Purity:
99%
Soluble in DMSO
Description
RTK inhibitor which effectively inhibits PDGFR, c-Kit and c-Met (IC50 values low µM range in vivo). Amuvatinib influences various survival and DNA repair related proteins such as pAKT, RAD51 and GSK-3β, inhibits cell proliferation, induces cell growth arrest and promotes apoptosis in prostate LNCaP cancer cells with low μM IC50 values. When combined with Erlotinib (Axon 1128), Amuvatinib abolished HER family/PI3K/Akt pathway with associated tumor growth inhibition in prostate cancer.
References
Certificates
Categories
Extra info
W. Qi et al. MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009, 9, 142.
D. Mahadevan et al. A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors. Oncogene. 2007, , 26, 3909-3919.
C.J. Phillip et al. Targeting MET kinase with the small-molecule inhibitor amuvatinib induces cytotoxicity in primary myeloma cells and cell lines. J. Hematol. Oncol. 2013, 6, 1-16.
J.W. Welsh et al. The c-Met receptor tyrosine kinase inhibitor MP470 radiosensitizes glioblastoma cells. Radiat. Oncol. 2009, 4, 69.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
BCR-ABL
c-MET
FLT3
PDGFR
PI3K-Akt-mTOR
c-KIT
RTK class III; EC 2.7.10.1
RTK inhibitor which effectively inhibits PDGFR, c-Kit and c-Met
Chemical name
N-(Benzo[d][1,3]dioxol-5-ylmethyl)-4-(benzofuro[3,2-d]pyrimidin-4-yl)piperazine-1-carbothioamide
Parent CAS No.
[850879-09-3]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Apilimod dimesylate - STA 5326 dimesylate | Axon 2500
CAS [870087-36-8]
MF C23H26N6O2.2CH4O3SMW 610.70
Purity:
98%
Soluble in water and DMSO
Description
Potent and orally active inhibitor of the cytokines interleukin-12 (IL-12), and interleukin-23 (IL-23) production; potential regulators of certain autoimmune and inflammatory diseases. Blocks the translocation of c-Rel, a member of the Rel/NF-κB family of transcription factors, to the nucleus without affecting the translocation of the other NF-κB family members. Water soluble dimesylate salt of Axon 1369.
Note | | axonmedchem |
| CysLT1 Antagonist Q8 | Axon 2738
CAS [1541762-55-3]
MF C17H14ClNO2MW 299.75
Purity:
99%
Soluble in DMSO
Description
CysLT1 antagonist Q8 inhibits developmental angiogenesis in transgenic fluorescent zebrafish, and inhibits human microvascular endothelial cell (HMEC-1) proliferation, tubule formation, and migration. CysLT1 antagonist Q8 elicits antiangiogenic effects in a VEGF-independent in vitro model of angiogenesis and exerts an additive antiangiogenic response with the anti-VEGF biologic bevacizumab.
KEYWORDS: CysLT1 Antagonist Q8 | supplier | CysLT1 antagonist | CAS [1541762-55-3] | [1541762-52-0] | Cysteinyl leukotrienes | CysLT | Antagonist | Receptors | Angiogenesis | Antiangiogenic | | axonmedchem |
| SC 144 hydrochloride | Axon 2324
CAS [917497-70-2]
MF C16H111FN6O.HClMW 358.76
Purity:
99%
Soluble in DMSO
Description
The first-in-class small-molecule gp130 inhibitor with oral activity in ovarian cancer (IC50 values 0.43-0.95 µM for a range of human ovarian cancer cell lines). SC144 binds gp130, induces gp130 phosphorylation and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
References
Certificates
Categories
Extra info
C. Plasencia et al. Discovery of a novel quinoxalinhydrazide with a broad-spectrum anticancer activity. Cancer Biol Ther. 2009 Mar;8(5):458-65.
S. Xu et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.
T. Oshima et al. Combination effects of SC144 and cytotoxic anticancer agents. Anticancer Drugs. 2009 Jun;20(5):312-20.
F. Grande et al. Synthesis and antitumor activities of a series of novel quinoxalinhydrazides. Bioorg Med Chem. 2007 Jan 1;15(1):288-94.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Diabetes & Metabolism
MAPK
JAK-STAT
PI3K-Akt-mTOR
Type I
gp130
The first-in-class small-molecule gp130 inhibitor
Chemical name
N'-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)pyrazine-2-carbohydrazide hydrochloride
Parent CAS No.
[895158-95-9]
Order
Size
Unit Price
Stock
10 mg
€135.00
In Stock | | axonmedchem |
| PD 0220245 | Axon 1501
CAS [640736-79-4]
MF C24H26Cl2N4S2.2HClMW 578.45
Purity:
99%
Soluble in water and DMSO
Description
Potent and non-peptide interleukine 8 (IL-8) receptor antagonist
References
Certificates
Categories
Extra info
JJ Li et al. Synthesis and structure–Activity relationship of 2-amino-3-heteroaryl-quinoxalines as non-peptide, small-Molecule antagonists for interleukin-8 receptor. Bioorg. Med. Chem. 2003, 11(17), 3777-3790.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
Immunology
Pain & Inflammation
IL-8
A2
IL-8 antagonist
Chemical name
N-(3-[2,20]bithiophenyl-5-yl-6,7-dichloroquinoxalin-2-yl)-N,N-diethyl-butane-1,4-diamine.dihydrochloride
Parent CAS No.
[239094-97-4]
Order
Size
Unit Price
Stock
5 mg
€120.00
In Stock | | axonmedchem |
| PF 06465469 | Axon 2110
CAS [1407966-77-1]
MF C30H33N7O2MW 523.63
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, covalent inhibitor of interleukin-2 inducible T cell kinase (ITK) with nanomolar potency
References
Certificates
Categories
Extra info
CW Zapf et al. Covalent Inhibitors of Interleukin-2 Inducible T Cell Kinase (Itk) with Nanomolar Potency in a Whole-Blood Assay. J. Med. Chem. 2012, 55(22), 10047-10063.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Immunology
ITK
EC 2.7.10.2
Pfizer Licensed Products
Inhibitor of interleukin-2 inducible T cell kinase (ITK)
Chemical name
(R)-3-(1-(1-acryloylpiperidin-3-yl)-4-amino-1H-pyrazolo[3,4-d]pyrimidin-3-yl)-N-(4-isopropyl-3-methylphenyl)benzamide
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[1407966-77-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| SPD 304 | Axon 2143
CAS [1049741-03-8]
MF C32H32F3N3O2.2HClMW 620.53
Purity:
99%
Soluble in water and DMSO
Description
A cell permeable inhibitor of tumor necrosis factor-α (TNFα, IC50: 22 μM); inhibits TNF-α induced IkB-α depletion in HeLa cells (IC50: 4.6 μM)
References
Certificates
Categories
Extra info
MM He et al. Small-Molecule Inhibition of TNF-α. Science 2005, 310, 1022.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
Immunology
Pain & Inflammation
TNF-R1 (CD120)
NF-κB
Type 1
Cell permeable inhibitor of TNFα
Chemical name
6,7-dimethyl-3-((methyl(2-(methyl((1-(3-(trifluoromethyl)phenyl)-1H-indol-3-yl)methyl)amino)ethyl)amino)methyl)-4H-chromen-4-one dihydrochloride
Parent CAS No.
[869998-49-2]
Order
Size
Unit Price
Stock
5 mg
€145.00
In Stock | | axonmedchem |
| UNC 2250 | Axon 2346
CAS [1493694-70-4]
MF C24H36N6O2MW 440.58
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent Mer kinase inhibitor (in vitro IC50 values 1.7 nM, 270 nM, and 100 nM for Mer, Axl, and Tyro3 RTKs, respectively) with promising selectivity and PK properties. UNC 2250 efficiently inhibited both steady state and ligand-stimulated phosphorylation of Mer, and confirmed functional antitumor activity by exhibiting potential to reduced colony-forming in both rhabdoid tumor cells and NSCLC cells.
KEYWORDS: UNC 2250 | supplier | Mer Inhibitor | UNC2250 | CAS [1493694-70-4] | Gas6 | Mer | TAM | RTK | Axl | Tyro3 | antitumor | rhabdoid | NSCLC | lung cancer | | axonmedchem |