| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| GDC 0980 - RG 7422 | GNE 390 | Apitolisib | Axon 1782
CAS [1032754-93-0]
MF C23H30N8O3SMW 498.60
Purity:
99%
Soluble in DMSO
Description
Selective, potent, orally bioavailable inhibitor of Class I PI3 kinase and mTOR kinase (TORC1/2) with in vitro IC50 of 5, 27, 7 and 14 nM for p110 α, β, δ and γ isoforms and apparent Ki of 17.3 nM for human mTOR. GDC-0980 has excellent pharmacokinetic and pharmaceutical properties and demonstrates broad activity in xenograft cancer models (breast, ovarian, lung, and prostate)
References
Certificates
Categories
Extra info
JJ Wallin et al. GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway. Mol. Cancer Ther. 2011, 10(12), 2426-2436.
AJ Wagner et al. A first-in-human phase I study to evaluate GDC-0980, an oral PI3K/mTOR inhibitor, administered QD in patients with advanced solid tumors. J. Clin. Oncol. 2011, 29 (suppl; abstr 3020).
DP Sutherlin et al. Discovery of a Potent, Selective, and Orally Available Class I Phosphatidylinositol 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor (GDC-0980) for the Treatment of Cancer. J. Med. Chem. 2011, 54(21), 7579-87.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
PI3K
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Dual PI3K and mTOR inhibitor
Chemical name
(S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one
Parent CAS No.
[1032754-93-0]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| Palomid 529 - SG 00529 | Axon 1718
CAS [914913-88-5]
MF C24H22O6MW 406.43
Purity:
98%
Soluble in DMSO
Description
Small molecule tyrosine kinase inhibitor, targeting Akt/mTOR; Dual TORC1/2 inhibitor of the PI3K/Akt//mTOR pathway having broad activity in angiogenesis and cellular proliferation; P529 inhibits cell growth of a broad spectrum of cancer cell lines
References
Certificates
Categories
Extra info
Q Xue et al. Palomid 529, a Novel Small-Molecule Drug, Is a TORC1/TORC2 Inhibitor That Reduces Tumor Growth, Tumor Angiogenesis, and Vascular Permeability. Cancer Res. 2008, 68(22), 9551-9557.
R Diaz et al. The novel Akt inhibitor Palomid 529 (P529) enhances the effect of radiotherapy in prostate cancer. Br. J. Cancer 2009, 100, 932–940.
GL Gravina et al. The TORC1/TORC2 inhibitor, Palomid 529, reduces tumor growth and sensitizes to docetaxel and cisplatin in aggressive and hormone-refractory prostate cancer cells. Endocr. Relat. Cancer. 2011, 18(4), 385-400.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
mTOR inhibitor
Chemical name
8-(1-hydroxyethyl)-2-methoxy-3-(4-methoxybenzyloxy)-6H-benzo[c]chromen-6-one
Parent CAS No.
[914913-88-5]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| XL PI3K/mTOR inhibitor | Axon 1706
CAS [934529-30-3]
MF C31H29N5O6SMW 599.66
Purity:
99%
Moderately soluble in DMSO
Description
Orally active PI3K/mTOR tyrosine kinase inhibitor; matching the profile of XL 765.
Note | | axonmedchem |
| Temsirolimus - CCI 779 | Torisel | Axon 1699
CAS [162635-04-3]
MF C56H87NO16MW 1030.29
Purity:
99%
Soluble in DMSO
Description
Specific mTOR inhibitor; a signaling protein that regulates cell growth and angiogenesis; a therapeutic for the treatment of advanced renal cell carcinoma (RCC), kidney cancer and other cancer types.
References
Certificates
Categories
Extra info
X Wan et al. CCI-779 Inhibits rhabdomyosarcoma xenograft growth by an antiangiogenic mechanism linked to the targeting of mTOR/HIF-1alpha/VEGF signaling. Neoplasia 2006, 8(5), 394–401.
D DelBufalo et al. Antiangiogenic potential of the mammalian target of rapamycin inhibitor temsirolimus. Cancer Res. 2006, 66(11), 5549–5554.
GV Thomas et al. Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer. Nature Medicine 2006, 12(1), 122–127.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Immunology
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
Pfizer Licensed Products
mTOR inhibitor
Chemical name
42-[3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate]-Rapamycin
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[162635-04-3]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| GSK 2126458 - Omipalisib | Axon 1596
CAS [1086062-66-9]
MF C25H17F2N5O3SMW 505.50
Purity:
99%
Soluble in DMSO
Description
Highly potent and orally bioavailable inhibitor of PI3K and mTOR in vitro and in vivo; Ki values to be 0.019, 0.13, 0.024 and 0.06 nM for p110 α, β, δ and γ isoforms and 0.18 and 0.3 nM for mTORC1 and mTORC2 respectively.
KEYWORDS: GSK 2126458 | supplier | PI3K/mTOR inhibitor | Omipalisib | GSK2126458 | GSK-2126458 | CAS [1086062-66-9] | Phosphatidylinositol | mTOR | PI3K | orally bioavailable | TORC | | axonmedchem |
| AZD 8055 | Axon 1561
CAS [1009298-09-2]
MF C25H31N5O4MW 465.54
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective mTOR inhibitor, with IC50 values to be 0.8 nM and selectivity ca 1000-fold against class I PI3K and other PIKKs
References
Certificates
Categories
Extra info
CM Chresta et al. AZD8055 Is a Potent, Selective, and Orally Bioavailable ATP-Competitive Mammalian Target of Rapamycin Kinase Inhibitor with In vitro and In vivo Antitumor Activity. Cancer Res. 2010, 70(1), 288-298.
P Sini et al. Simultaneous inhibition of mTORC1 and mTORC2 by mTOR kinase inhibitor AZD8055 induces autophagy and cell death in cancer cells. Autophagy. 2010, 6(4).
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
mTOR
PI3K-Akt-mTOR
EC 2.7.11.1
mTOR inhibitor
Chemical name
(5-(2,4-bis((S)-3-methylmorpholino)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol
Parent CAS No.
[1009298-09-2]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| KU 0063794 - KU 63794 | Axon 1472
CAS [938440-64-3]
MF C25H31N5O4MW 465.54
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective mTOR inhibitor, with IC50 values to be about 10 nM for mTORC1 and mTORC2.
KEYWORDS: KU 0063794 | supplier | mTOR inhibitor | KU 63794 | KU0063794 | KU63794 | KU-0063794 | KU-63794 | CAS [938440-64-3] | Phosphatidylinositol | mTOR | Inhibitor | Enzymes | | axonmedchem |
| BEZ 235 - NVP-BEZ235 | Axon 1281
CAS [915019-65-7]
MF C30H23N5OMW 469.54
Purity:
99%
Moderately soluble in DMSO
Description
Orally active PI3K tyrosine kinase inhibitor; Dual PI3K/mTOR inhibition; BEZ235 showed high target specificity and demonstrated antiproliferative activity against tumor cell lines in animal models of cancer.
KEYWORDS: BEZ 235 | supplier | PI3K/mTOR inhibitor | NVP-BEZ235 | BEZ235 | BEZ-235 | CAS [915019-65-7] | Phosphatidylinositol | mTOR | PI3K | orally active | tyrosine kinase | antiproliferative | tumor cell lines | cancer | | axonmedchem |
| Farampator - CX691 | Org24448 | Axon 2687
CAS [211735-76-1]
MF C12H13N3O2MW 231.25
Purity:
99%
Soluble in DMSO
Description
Second-generation ampakine that potentiates AMPA receptor function (EC50 value 14 µM for increase of glutamate-induced steady state currents) and enhances glutamatergic synaptic transmission, demonstrating improved cognitive performance in a variety of tasks. CX691 aka Farampator is developed primarily as a putative antipsychotic.
KEYWORDS: Farampator | supplier | AMPA PAM | CX691 | Org24448 | CX-691 | CX 691 | Org-24448 | Org 24448 | CAS [211735-76-1] | Glutamate | positive allosteric modulator | Ion Channel | cognitive | putative antipsychotic | ampakine | memory | Alzheimer | CNS | | axonmedchem |
| SB 332235 | Axon 2593
CAS [276702-15-9]
MF C13H10Cl3N3O4SMW 410.66
Purity:
98%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Selective nonpeptide CXCR2 antagonist (IC50 values 9.3 nM and 9.6 µM for CXCR2 and CXCR1, respectively) exhibiting significant anti-inflammatory effects in acute and chronic models of arthritis in the rabbit. SB-332235 significantly reduced levels of proinflammatory mediators in the synovial fluid, including TNF-α, IL-8, PGE2, LTB4, and LTC4. SB-332235 was also found to abolish the GRO/CINC-1 mediated inhibition of C2-ceramide-induced cytochrome-c release from mitochondria.
KEYWORDS: SB 332235 | supplier | CXCR2 antagonist | SB332235 | SB-332235 | CAS [276702-15-9] | Chemokine | GPCR | anti-inflammatory | arthritis | TNF-α | IL-8 | interleukin-8 | PGE2 | prostaglandin | LTB4 | LTC4 | Alzheimer's | apoptosis | | axonmedchem |
| TB5 | Axon 2629
CAS [948841-07-4]
MF C15H14BrNOSMW 336.25
Purity:
100%
Soluble in DMSO
Description
Competitive and reversible MAO-B inhibitor (Ki values 1.45 µM and 0.11 µM for hMAO-A and hMAO-B, respectively) capable of crossing the BBB. Valuble tool for development of drugs for neurodegenerative disorders such as Parkinson’s and Alzheimer’s diseases.
KEYWORDS: TB5 | supplier | MAO-B inhibitor | TB-5 | CAS [948841-07-4] | Mono-amines | MAO | oxidase | Parkinson's | Alzheimer's | neurodegenerative | CNS | | axonmedchem |
| ML 252 | Axon 2615
CAS [N.A.]
MF C20H24N2O.HClMW 344.88
Purity:
99%
Soluble in DMSO
Description
Potent, selective and brain penetrant KCNQ2 inhibitor (Kv7.2; IC50 value 69 nM, and >40-fold selective over KCNQ1). A useful in vivo tool molecule to study KCNQ2 pharmocology.
KEYWORDS: ML 252 | supplier | KCNQ2 inhibitor | ML-252 | CAS [1392494-64-2] - [1392494-65-3] | Potassium | voltage-gated | Kv7.2 | Alzheimer’s | brain penetrant | selective | KCNQ1 | CNS | | axonmedchem |
| KN 93 | Axon 2566
CAS [1188890-40-5]
MF C26H29ClN2O4SMW 501.04
Purity:
99%
Soluble in DMSO
Description
Inhibitor of multifunctional Ca2+/Calmodulin-dependent protein kinase (CaMKII; Ki value 0.37 μM for inhibition of CaMKII phosphorylating activity). In addition, KN93 also affects CaV1.3 and CaV1.2 calcium channels in a CaMKII-independent manner.
The water soluble phosphate salt of KN 93 (Axon 2555) is available as well.
KEYWORDS: KN 93 | supplier | CaMKII inhibitor | KN93 | CAS [1188890-40-5] | [1188890-41-6] | LCC | RyRs |PLB| CaMK | Inhibitor | calcium | channel | calmodulin | myosin | dependent | Ca2+ | CaV1.3 | CaV1.2 | Alzheimer’s | Angelman | L-type | ryanodine | phospholamban | ECC | arrhythmia | | axonmedchem |
| KN 93 phosphate | Axon 2555
CAS [1188890-41-6]
MF C26H29ClN2O4S.H3PO4MW 599.03
Purity:
99%
Soluble in water and DMSO
Description
Inhibitor of multifunctional Ca2+/Calmodulin-dependent protein kinase (CaMKII; Ki value 0.37 μM for inhibition of CaMKII phosphorylating activity). In addition, KN93 also affects CaV1.3 and CaV1.2 calcium channels in a CaMKII-independent manner.
The parent molecule KN 93 (Axon 2566) is available as well.
KEYWORDS: KN 93 phosphate | supplier | CaMKII inhibitor | KN93 | CAS [1188890-41-6] | [1188890-40-5] | LCC | RyRs |PLB| CaMK | Inhibitor | calcium | channel | calmodulin | myosin | dependent | Ca2+ | CaV1.3 | CaV1.2 | Alzheimer’s | Angelman | L-type | ryanodine | phospholamban | ECC | arrhythmia | | axonmedchem |
| LRRK2-IN-1 | Axon 2493
CAS [1234480-84-2]
MF C31H38N8O3MW 570.69
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, ATP-competitive and selective inhibitor of the Parkinson's disease kinase LRRK2 (IC50 value 13 nM and 6 nM for inhibitions of WT and G2019S mutant LRRK2 kinase activity, respectively). LRRK2IN1 is neuroprotective in vitro and inhibits the activity of LRRK2 in kidney and spleen when administered in vivo. However, LRRK 2-IN-1 is not able to cross the BBB.
References
Certificates
Categories
Extra info
B.K. Gilsbach et al. Structural Characterization of LRRK2 Inhibitors. J Med Chem. 2015 May 14;58(9):3751-6.
X. Deng et al. Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2. Nat Chem Biol. 2011 Apr;7(4):203-5.
L. Munoz et al. Optimisation of LRRK2 inhibitors and assessment of functional efficacy in cell-based models of neuroinflammation. Eur J Med Chem. 2015 May 5;95:29-34.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
Pain & Inflammation
LRRK2
Ubiquitin
EC 2.7.11.1
Potent, ATP-competitive and selective inhibitor of LRRK2
Chemical name
2-(2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl)phenylamino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
Parent CAS No.
[1234480-84-2]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| EUK 134 - Salen-Mn | Axon 2292
CAS [81065-76-1]
MF C18H18ClMnN2O4MW 416.74
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
A salen manganese complex with superoxide dismutase (SOD) and catalase mimetic characteristics. EUK134 exhibits potent antioxidant activities, and inhibits the formation of β-amyloid and related amyloid fibril (IAPP). Useful pharmacological tool for the development of new compounds for the treatment of Alzheimer's and Parkinson's disease and type 2 diabetes.
References
Certificates
Categories
Extra info
S.J. Ophoven et al. Salen-manganese complexes: sophisticated tools for the analysis of intercellular ROS signaling pathways. Anticancer Res. 2010 Oct;30(10):3967-79.
P. Failli et al. A novel manganese complex effective as superoxide anion scavenger and therapeutic agent against cell and tissue oxidative injury. J Med Chem. 2009 Nov 26;52(22):7273-83.
D. Decraene et al. A synthetic superoxide dismutase/catalase mimetic (EUK-134) inhibits membrane-damage-induced activation of mitogen-activated protein kinase pathways and reduces p53 accumulation .... J Invest Dermatol. 2004 Feb;122(2):484-91.
Y. Rong et al. EUK-134, a synthetic superoxide dismutase and catalase mimetic, prevents oxidative stress and attenuates kainate-induced neuropathology. Proc Natl Acad Sci U S A. 1999 Aug 17;96(17):9897-902.
S. Bahramikia et al. Inhibition of human islet amyloid polypeptide or amylin aggregation by two manganese-salen derivatives. Eur J Pharmacol. 2013 May 5;707(1-3):17-25.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
Miscellaneous
Pain & Inflammation
Antioxidant
Antioxidant with superoxide dismutase (SOD) and catalase mimetic characteristics.
Chemical name
(SP-5-13) Chloro[[2,2'-[1,2-ethanediylbis[(nitrilo-kN)methylidyne]]bis[6-methoxyphenolato-kO]](2-)]-manganese
Parent CAS No.
[81065-76-1]
Order
Size
Unit Price
Stock
10 mg
€50.00
In Stock | | axonmedchem |
| CGS 9343B - Zaldaride maleate | Axon 1252
CAS [109826-27-9]
MF C26H28N4O2.C4H4O4MW 544.60
Purity:
98%
Soluble in DMSO
Description
Inhibitor of Calmodulin activity.
KEYWORDS: CGS 9343B | supplier | Calmodulin inhibitor | Zaldaride maleate | CGS9343B | CGS-9343B | CAS [109826-27-9] | [109826-26-8] | Calcium | Calcium | Inhibitor | Proteins | | axonmedchem |
| XE 991 | Axon 1987
CAS [122955-42-4]
MF C26H20N2OMW 376.45
Purity:
99%
Soluble in DMSO
Description
KCNQ channel and M-current blocker; potential AD therapeutic. The hydrochloride salt of XE 991 (Axon 1305) is available as well.
References
Certificates
Categories
Extra info
Wang et al. KCNQ2 and KCNQ3 potassium channel subunits: molecular correlates of the M-channel. Science 1998, 282 1890.
Zaczek et al. Two new potent neurotransmitter release enhancers, 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone and 10,10-bis(2-fluoro-4-pyridinylmethyl) -9(10H)-anthracenone: comparison to linopirdine. J. Pharmacol. Exp. Ther. 1998, 285 724.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Pain & Inflammation
Kv7.1
KCNQ1
KCNQ channel and M-current blocker
Chemical name
10,10-bis(pyridin-4-ylmethyl)anthracen-9(10H)-one
Parent CAS No.
[122955-42-4]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| GNE 7915 | Axon 2348
CAS [1351761-44-8]
MF C19H21F4N5O3MW 443.40
Purity:
99%
Soluble in DMSO
Description
Highly potent, selective, metabolically stable, and brain-penetrable LRRK2 inhibitor (IC50 value 9 nM for phospho-LRRK2 in vitro). GNE 7915 is selective across 187 screened kinases, and >3200 and 53 times selective over JAK2 and TTK, respectively. GNE 7915 does not suppress LPS-stimulated TNFα and CXCL10 levels in LPS-treated primary wild-type (WT) or knockout (KO) astrocyte cultures, and is not reported to cause cellular or genetic toxicity.
References
Certificates
Categories
Extra info
A.A. Estrada et al. Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J. Med. Chem. 2012, 55, 9416-9433.
G.C. Luerman et al. Phosphoproteomic evaluation of pharmacological inhibition of leucine-rich repeat kinase 2 reveals significant off-target effects of LRRK-2-IN-1. J. Neurochem. 2014, 128, 561-576.
M.E. Kavanagh et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg. Med. Chem. Lett. 2013, 23, 3690-3696.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
Pain & Inflammation
LRRK2
Ubiquitin
EC 2.7.11.1
Potent, selective, metabolically stable, and brain-penetrable LRRK2 inhibitor
Chemical name
(4-(4-(ethylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-2-fluoro-5-ethoxyphenyl)(morpholino)methanone
Parent CAS No.
[1351761-44-8]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| PF 06447475 | Axon 2546
CAS [1527473-33-1]
MF C17H15N5OMW 305.33
Purity:
99%
Soluble in DMSO
Description
Highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor (IC50 value 3 nM); an exceptional tool compound to study the function of LRRK2 PF 06447475 mitigates both neurodegeneration and neuroinflammation associated with G2019S-LRRK2 expression by LRRK2 kinase inhibition in rats.
KEYWORDS: PF 06447475 | supplier | LRRK2 inhibitor | PF06447475 | CAS [1527473-33-1] | LRRK2 | Inhibitor | neurodegeneration | neuroinflammation | Parkinson's |Huntington's | PD | dopamine | synuclein | | axonmedchem |
| GSK 2578215A | Axon 2181
CAS [1285515-21-0]
MF C24H18FN3O2MW 399.42
Purity:
99%
Soluble in DMSO
Description
Potent and exceptionally highly selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values 10.9 and 8.9 nM for wild-type LRRK2 and LRRK2[G2019S] mutant, respectively.) GSK2578215A possesses good blood-brain barrier (BBB) permeability with a high ratio of brain to plasma distribution in mice.
References
Certificates
Categories
Extra info
A.D. Reith et al. GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor. Bioorg. Med. Chem. Lett. 2012, 22, 5625-5629.
M.E. Kavanagh et al. The development of CNS-active LRRK2 inhibitors using property-directed optimisation. Bioorg. Med. Chem. Lett. 2013, 23, 3690-3696.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
Pain & Inflammation
LRRK2
Ubiquitin
EC 2.7.11.1
Potent and highly selective LRRK2 inhibitor
Chemical name
2-(benzyloxy)-5-(2-fluoropyridin-4-yl)-N-(pyridin-3-yl)benzamide
Parent CAS No.
[1285515-21-0]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| PF 04447943 - PF 4447943 | Axon 2148
CAS [1082744-20-4]
MF C20H25N7O2MW 395.46
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective, brain penetrant PDE9A inhibitor for the treatment of cognitive disorders that exhibit a disrupted P50-gating response (IC50 values 8.3 nM and 1394 nM for PDE9A and PDE1C respectively). PF 04447943 elevates cGMP in multiple brain regions and in cerebral spinal fluid (CSF), and shows an impact on hippocampal synaptic plasticity.
References
Certificates
Categories
Extra info
P.R. Verhoest et al. Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943),..... J. Med. Chem. 2012, 55, 9045-9054.
M.M. Claffey et al. Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors. J. Med. Chem. 2012, 55, 9055-9068.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Pain & Inflammation
EC 3.1.4.35
PDE
Selective, brain penetrant PDE9A inhibitor
Chemical name
6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one
Parent CAS No.
[1082744-20-4]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| RVX 208 - RVX 000222 | Axon 2245
CAS [1044870-39-4]
MF C20H22N2O5MW 370.40
Purity:
100%
Soluble in DMSO
Description
BET bromodomain inhibitor specific for second bromodomains (BD2s), currently in phase I/II clinical trials for the treatment of cardiovascular diseases (IC50 values of 87 and 0.51 μM derived from the AlphaScreen data on BRD3 BD1 and BD2 resp.). RVX 208 preferentially binds to the second bromodomain found on BET proteins, exhibiting selectivity over BD1 of up to 23-fold with a KD of 195 nM against BD2 and 4 μM against BD1 of BRD3. RVX 208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner, and leads to an increase of plasma levels of the high-density lipid protein ApoA1, wich has emerged as a promising approach for the treatment of atherosclerosis.
References
Certificates
Categories
Extra info
S. Picaud et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc. Natl. Acad. Sci. U.S.A. 2013, 110, 19754-19759.
K.G. McLure et al. RVX-208, an inducer of ApoA-I in humans, is a BET bromodomain antagonist. PLoS One. 2013, 8, e83190.
E. McNeill, Eileen. RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases. Curr. Opini. Invest. Drugs. 2010, 11, 357-364.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
Cell Signaling & Oncology
CNS
Epigenetics
BET (BRD)
BET bromodomain inhibitor specific for second bromodomains (BD2s)
Chemical name
2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one
Parent CAS No.
[1044870-39-4]
Order
Size
Unit Price
Stock
2 mg
€65.00
In Stock | | axonmedchem |
| LY 2811376 | Axon 2225
CAS [1194044-20-6]
MF C15H14F2N4SMW 320.36
Purity:
99%
Soluble in 0.1N HCl(aq), DMSO, and Ethanol
Description
The first orally available non-peptidic BACE 1 inhibitor (IC50 value ranges from 239-249 nM in vitro) that produces profound Aβ-lowering effects in animals. LY2811376 demonstrated ~10-fold selectivity toward BACE 1 over BACE 2, and >50-fold selectivity over cathepsin D, pepsin, or renin. Clinical development of LY 2811376 was terminated as a result of toxicology findings identified in longer-term preclinical studies.
References
Certificates
Categories
Extra info
P.C. May et al. Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor. J. Neurosci. 2011, 31, 16507-16516.
Y. Lu et al. Cerebrospinal fluid amyloid-β (Aβ) as an effect biomarker for brain Aβ lowering verified by quantitative preclinical analyses. J. Pharmacol. Exp. Ther. 2012, 342, 366-375.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
BACE-1
EC 3.4.23.46
The first orally available non-peptidic BACE 1 inhibitor
Chemical name
(S)-4-(2,4-difluoro-5-(pyrimidin-5-yl)phenyl)-4-methyl-5,6-dihydro-4H-1,3-thiazin-2-amine
Parent CAS No.
[1194044-20-6]
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Size
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5 mg
€125.00
In Stock | | axonmedchem |
| AZD 2858 hydrochloride | Axon 2194
CAS [486424-21-9]
MF C21H23N7O3S.HClMW 489.98
Purity:
98%
Soluble in water and DMSO
Description
Potent and highly selective Glycogen Synthase Kinase-3β (GSK-3β; Ki value 4.9 nM) inhibitor for Alzheimer’s disease with good BBB permeability in a bovine endothelial cell assay. AZD 2858 inhibits GSK-3β-mediated tau phosphorylation (IC50 value 76 nM) in vitro, and shows a good overall selectivity versus a panel of 26 kinases and >100 fold selectivity over CDK2 (Ki value 540 nM).In rats, oral AZD2858 treatment caused a dose-dependent increase in trabecular bone mass by GSK-3 mediated inhibition of Wnt canonical signaling, making AZD2858 a possible therapeutic candidate for osteoporosis.
References
Certificates
Categories
Extra info
S. Berg et al. Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines. J. Med. Chem. 2012, 55, 9107-9119.
R. Marsell et al. GSK-3 inhibition by an orally active small molecule increases bone mass in rats. Bone. 2012, 50, 619-627.
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
Potent and highly selective Glycogen Synthase Kinase-3β inhibitor
Chemical name
4-amino-4'-(4-methylpiperazin-1-ylsulfonyl)-N-(pyridin-3-yl)biphenyl-3-carboxamide hydrocholride
Parent CAS No.
[486424-20-8]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| TDZD 8 | Axon 2010
CAS [327036-89-5]
MF C10H10N2O2SMW 222.26
Purity:
98%
Soluble in DMSO
Description
Selective and non-ATP-competitive inhibitor of glycogen synthase kinase-3β (GSK-3β); potential agent for the treatment of Alzheimer's disease
References
Certificates
Categories
Extra info
AA Martinez et al.First non-ATP competitive glycogen synthase kinase 3 beta (GSK-3beta) inhibitors: thiadiazolidinones (TDZD) as potential drugs for the treatment of Alzheimer's disease. J. Med. Chem. 2002, 45(6), 1292-1299.
M Collino et al. Treatment with the glycogen synthase kinase-3beta inhibitor, TDZD-8, affects transient cerebral ischemia/reperfusion injury in the rat hippocampus. Shock. 2008, 30(3), 299-307.
D Aguilar-Morante et al. Inhibition of Glioblastoma Growth by the Thiadiazolidinone Compound TDZD-8. PLoS ONE 2010, 5(11), e13879.
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
Selective and non-ATP-competitive inhibitor of GSK-3β
Chemical name
4-benzyl-2-methyl-1,2,4-thiadiazolidine-3,5-dione
Parent CAS No.
[327036-89-5]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| Ciproxifan maleate - FUB 359 maleate | Axon 1993
CAS [184025-19-2]
MF C16H18N2O2.C4H4O4MW 386.40
Purity:
99%
Soluble in DMSO
Description
Orally bioavailable, extremely potent and selective H3-receptor antagonist (Ki: 0.5-1.9 nM in vitro); a potential therapeutic agent in the treatment of Alzheimer's disease
References
Certificates
Categories
Extra info
X Ligneau et al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist.J. Pharmacol. Exp. Ther. 1998, 287, 658-666.
ME Bardgett et al. Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Neurobiol. Learn. Mem. 2011, 95(1), 64-72.
Certificate of Analysis
Material Safety Data Sheet
CNS
Immunology
H3
A18
H3 antagonist
Chemical name
(4-(3-(1H-imidazol-4-yl)propyl1H-imidazol-4-yl)propoxy)phenyl)(cyclopropyl)methanone maleate
Parent CAS No.
[184025-18-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| LY 2886721 hydrochloride | Axon 1964
CAS [1262036-49-6]
MF C18H16F2N4O2S.HClMW 426.87
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Orally active cell-permeable inhibitor of human β-secretase (BACE-1); potential agent to treat Alzheimer's Disease
References
Certificates
Categories
Extra info
M Townsend. When will Alzheimer's disease be cured? A pharmaceutical perspective. J. Alzheimers Dis. 2011, 24 (Suppl 2), 43-52.
P May et al. Preclinical characterization of LY2886721: A BACE1 inhibitor in clinical development for early Alzheimer's disease. Alzheimer's & Dementia 2012, 8(4), 95.
B Willis et al. Central BACE1 inhibition by LY2886721 produces opposing effects on APP processing as reflected by cerebrospinal fluid sAPPalpha and sAPPbeta. Alzheimer's & Dementia 2012, 8(4), 582.
F Martenyi et al. BACE inhibitor LY2886721 safety and central and peripheral PK and PD in healthy subjects (HSs). Alzheimer's & Dementia 2012, 8(4), 583.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
CNS
BACE-1
EC 3.4.23.46
BACE 1 inhibitor
Chemical name
N-(3-((4aS,7aS)-2-amino-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-7a-yl)-4-fluorophenyl)-5-fluoropicolinamide hydrochloride
Parent CAS No.
[1262036-50-9]
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Size
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5 mg
€105.00
In Stock | | axonmedchem |
| Prucalopride | Axon 1479
CAS [179474-81-8]
MF C18H26ClN3O3MW 367.87
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT4 receptor agonist; a gastroprokinetic agent for the treatment of constipation and irritable bowel syndrome; showed memory-enhancing effects in mice through modulation of cholinergic pathways; hence an indication of potential as Alzheimer's disease therapy
References
Certificates
Categories
Extra info
EP Bouras et al. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Gut. 1999, 44(5), 682-6.
JH De Maeyer et al. 5-HT4 receptor agonists: similar but not the same. Neurogastroenterol. Motility. 2008, 20(2), 99-112.
J Tack et al. Prucalopride (resolor(R)) in the treatment of severe chronic constipation in patients dissatisfied with laxatives. Gut. 2009, 58(3), 357-65.
M Cachard-Chastel et al. Prucalopride and donepezil act synergistically to reverse scopolamine-induced memory deficit in C57Bl/6j mice. Behav. Brain Res. 2008, 187(2), 455-61.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT4
A19
5-HT4 agonist
Chemical name
4-Amino-5+K445-chloro-2,3-dihydro-benzofuran-7-carboxylic acid [1-(3-methoxy-propyl)-piperidin-4-yl]-amide
Parent CAS No.
[179474-81-8]
Order
Size
Unit Price
Stock
10 mg
€90.00
In Stock | | axonmedchem |
| FK 960 | Axon 1607
CAS [133920-70-4]
MF C13H16FN3O2MW 265.28
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Somatostatin receptor agonist and also a 5-HT agonist; FK960 stimulates both serotonin and somatostatin production as a cognitive enhancer. However, its development for Alzheimer's disease (AD) was terminated in 2003
References
Certificates
Categories
Extra info
A Graul et al. FK-960, Congnition Enhancer. Drug. Fut. 1997, 22(8), 830-832.
N Matsuoka and TG Ainer. FK960 [N-(4-Acetyl-1-piperazinyl)-p-fluorobenzamide Monohydrate], a Novel Potential Antidementia Drug, Improves Visual Recognition Memory in Rhesus Monkeys... J. Pharmacol. Exp. Ther. 1997, 280(3), 1201-1209.
JP Hodgkiss and JS Kelly. Effect of FK960, a Putative Cognitive Enhancer, on Synaptic Transmission in CA1 Neurons of Rat Hippocampus. J. Pharmacol. Exp. Ther. 2001, 297(2), 620-628.
F Wang et al. Modulation of Ca2+Channel Currents by a Novel Antidementia Drug N-(4-Acetyl-1-piperazinyl)-p-fluorobenzamide Monohydrate (FK960) in Rat Hippocampal Neurons. J. Pharmacol. Exp. Ther. 2004, 308 (1), 120-126.
Certificate of Analysis
Material Safety Data Sheet
CNS
SST
Endocrinology
A4
Somatostatin agonist
Chemical name
N-(4-acetylpiperazin-1-yl)-4-fluorobenzamide
Parent CAS No.
[133920-70-4]
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10 mg
€95.00
In Stock | | axonmedchem |
| DHPG, (S)-3,5- - Dihydroxyphenylglycine, (S)-3,5- | Axon 1740
CAS [162870-29-3]
MF C8H9NO4MW 183.16
Purity:
99%
Optical purity:
>99%
Soluble in water and DMSO
Description
Potent and selective agonist of group I metabotropic glutamate (mGlu) receptors (mGluRs) mGluR1 and mGluR5; having therapeutic effects in the treatment of neuronal injury, cognitive enhancement and Alzheimer's disease.
* (S)-3,5-DHPG is the active enantiomer of 3,5-DHPG (Axon 1739)
References
Certificates
Categories
Extra info
C Wiśniewski and H Car. (S)-3,5-DHPG: a review. CNS Drug Rev. 2002, 8(1), 101–116.
WM Zho et al. The group I metabotropic glutamate receptor agonist (S)-3,5-dihydroxyphenylglycine induces a novel form of depotentiation in the CA1 region of the hippocampus. J. Neurosci. 2002, 22(20), 8838-8849.
Certificate of Analysis
Material Safety Data Sheet
CNS
Pain & Inflammation
mGluR5
mGluR1
C3
mGluR1 and mGluR5 agonist
Chemical name
(S)-2-amino-2-(3,5-dihydroxyphenyl)acetic acid
Parent CAS No.
[162870-29-3]
Order
Size
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5 mg
€80.00
In Stock | | axonmedchem |
| Tenilsetam - PAS 997 | CAS 997 | HR 029 | Axon 1470
CAS [86696-86-8]
MF C8H10N2OSMW 182.24
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Endonuclease modulator; a nootropic agent and advanced glycation end product (AGE) inhibitor having potential for Alzheimer's disease (AD) treatment.
Preclinical studies on diabetic rats suggested that tenilsetam may be beneficial in the inhibition of diabetic retinopathy, without amelioration of pericyte loss
References
Certificates
Categories
Extra info
G Munch et al. The cognition-enhancing drug tenilsetam is an inhibitor of protein crosslinking by advance glycosylation. J. Neural. Transm. Sect. 1994, 8(3), 193-208.
TJ Roesler et al. Advanced glycation end product (AGE) inhibition as a possible pharmacotherapeutic strategy in the treatment of Alzheimer's disease. Drugs Fut. 1999, 24(4), 411.
Certificate of Analysis
Material Safety Data Sheet
CNS
Diabetes & Metabolism
AGE
Endonuclease
Alzheimer's disease therapeutic
Chemical name
3-Thiophen-2-yl-piperazin-2-one
Parent CAS No.
[86696-86-8]
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Size
Unit Price
Stock
10 mg
€65.00
In Stock | | axonmedchem |
| Dimebon - Dimebolin hydrochloride | Axon 1445
CAS [97657-92-6]
MF C21H25N3.2HClMW 392.37
Purity:
99%
Soluble in water
Description
An antihistamine drug; recent focus on it as potential neuroprotectant and nootropic, hence an Alzheimer's treatment; multiple mechanisms of action, including inhibiting L-type calcium channels, blocking the action of neurotoxic β-amyloid proteins; and modulating the action of AMPA and NMDA glutamate receptors etc
References
Certificates
Categories
Extra info
DJ DeNoon, Dimebon Shines as Alzheimer's Therapy. WebMD Health News. July 30, 2008.
RS Doody et al. Effect of dimebon on cognition, activities of daily living, behaviour, and global function in patients with mild-to-moderate Alzheimer's disease: a randomised, double-blind, placebo-controlled study. Lancet. 2008, 372(9634):207-15.
Certificate of Analysis
Material Safety Data Sheet
Cardiovascular
CNS
Immunology
Pain & Inflammation
H2
H3
H4
H1
A18
Alzheimer's disease therapeutic
Chemical name
2,8-Dimethyl-5-[2-(6-methyl-pyridin-3-yl)-ethyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole dihydrochloride
Parent CAS No.
[3613-73-8]
Order
Size
Unit Price
Stock
5 mg
€65.00
In Stock | | axonmedchem |
| TD 5108 - Velusetrag | Axon 2060
CAS [866933-46-2]
MF C25H36N4O5SMW 504.64
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective 5-HT4 receptor agonist with high intrinsic activity; drug candidate for the treatment of chronic constipation and irritable bowel syndrome
References
Certificates
Categories
Extra info
JAM Smith et al. The in vitro pharmacological profile of TD-5108, a selective 5-HT4 receptor agonist with high intrinsic activity. Naunyn-Schmiedeberg's Arch. Pharmacol. 2008, 378(1), 125-137.
ML Manini et al. Effects of Velusetrag (TD‐5108) on gastrointestinal transit and bowel function in health and pharmacokinetics in health and constipation. Neurogastroenterol. Motility, 2010, 22(1), 42-e8.
Certificate of Analysis
Material Safety Data Sheet
CNS
5-HT4
A19
Selective 5-HT4 receptor agonist
Chemical name
N-(8-((R)-2-hydroxy-3-(N-methylmethylsulfonamido)propyl)-8-azabicyclo[3.2.1]octan-3-yl)-1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxamide
Parent CAS No.
[866933-46-2]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| Caprospinol - SP 233 | Axon 1442
CAS [4952-56-1]
MF C33H52O4MW 512.76
Purity:
99%
Moderately soluble in Ethanol
Description
An efficacious therapeutic indicated in Alzheimer’s disease (AD); clearing β-amyloid plaque in-vivo; restoring memory in rats
References
Certificates
Categories
Extra info
L Lecanu et al. Caprospinol reduces amyloid deposits and improves cognitive function in a rat model of Alzheimer's disease. Neurosci. 2010, 165(2), 427-35.
L Lecanu et al. Caprospinol: moving from a neuroactive steroid to a neurotropic drug. Exp. Opin. Invest. Drugs, 2009, 18(3), 265-276(12).
Certificate of Analysis
Material Safety Data Sheet
CNS
Amyloid-β
APP
Alzheimer's disease therapeutic and antihistaminergic drug
Chemical name
(22R,25R)-20-a-spirost-5-en-3-b-yl hexanoate
Parent CAS No.
[4952-56-1]
Order
Size
Unit Price
Stock
10 mg
€110.00
In Stock | | axonmedchem |
| Donepezil hydrochloride | Axon 1438
CAS [120011-70-3]
MF C24H29NO3.HClMW 415.95
Purity:
99%
Soluble in water and DMSO
Description
A centrally acting reversible acetylcholinesterase (AChE) inhibitor, with 100% oral bioavailability and easily crossing the blood-brain barrier; therapeutic agent in the treatment of Alzheimer's disease
References
Certificates
Categories
Extra info
J Birks, RJ Harvey. Donepezil for dementia due to Alzheimer's disease. Cochrane Database Syst Rev 2006, (1): CD001190.
LS Steele, RH Glazier. Is donepezil effective for treating Alzheimer's disease? Can Fam Physician 1999, 45, 917–9.
G Xiong, PM Doraiswamy. Combination drug therapy for Alzheimer's disease: what is evidence-based, and what is not?. Geriatrics 2005, 60(6), 22–6.
Certificate of Analysis
Material Safety Data Sheet
CNS
AchE
EC 3.1.1.7
Acetylcholinesterase inhibitor
Chemical name
2-(1-Benzyl-piperidin-4-ylmethyl)-5,6-dimethoxy-indan-1-one hydrochloride
Parent CAS No.
[120014-06-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| Piboserod hydrochloride - SB 207266A | Axon 1098
CAS [178273-87-5]
MF C22H31N3O2.HClMW 405.96
Purity:
99%
Soluble in water
Description
Selective 5-HT4 antagonist.
KEYWORDS: Piboserod HCl | supplier | 5-HT4 antagonist | SB 207266A | SB207266A | CAS [178273-87-5] | [152811-62-6] | Serotonin | 5-HT4 | GPCR | orally active | | axonmedchem |
| SB 742457 hydrochloride - GSK 742457 HCl | Intepirdine HCl | Axon 1382
CAS [607742-55-2]
MF C19H19N3O2S.HClMW 389.90
Purity:
99%
Soluble in DMSO
Description
Selective 5-HT6 antagonist; a potential agent added to stabilize donepezil (Axon 1438) treatment in subjects with mild-to-moderate Alzheimer's disease.
KEYWORDS: SB 742457 hydrochloride | supplier | 5-HT6 antagonist | GSK 742457 HCl | Intepirdine HCl | SB-742457 | GSK-742457 | CAS [607742-55-2] | [607742-69-8] | Serotonin | 5-HT6 | CNS | donepezil | Alzheimer's disease | AD | GPCR | | axonmedchem |
| CHIR 98014 - CT 98014 | Axon 1126
CAS [252935-94-7]
MF C20H17Cl2N9O2MW 486.31
Purity:
98%
Moderately soluble in DMSO
Description
Very potent, selective, cell-permeable reversible inhibitor of GSK-3; highly recommended tool.
KEYWORDS: CHIR 98014 | supplier | GSK-3 inhibitor | CT 98014 | CHIR98014 | CT98014 | CHIR-98014 | CT-98014 | CAS [252935-94-7] | glycogen synthase kinase | cell-permeable | reversible | CNS | Alzheimer | tau | phosphorylation | plaque | | axonmedchem |
| SRI-011381 hydrochloride | Axon 2943
CAS [2070014-88-7]
MF C20H31N3O.HClMW 365.94
Purity:
98%
Soluble in water and DMSO
Recently added | | axonmedchem |
| Rolipram, (R)-(-)- | Axon 1229
CAS [85416-75-7]
MF C16H21NO3MW 275.34
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO and Ethanol
Description
PDE4 inhibitor, more active R-enantiomer of Rolipram (Axon 1212) in comparison with (S)-(+)-Rolipram (Axon 1432). Rolipram is an anti-inflammatory drug; also with rich CNS profile, such as antidepressive, antipsychotic effects and/or neuroprotection.
KEYWORDS: R)-(-)-Rolipram | supplier | PDE4 inhibitor | Rolipram | CAS [85416-75-7] | cAMP | PDE | Inhibitor | phosphodiesterase | anti-inflammatory | CNS | anti-depressive | antipsychotic | neurodegenerative | neuroprotection | Alzheimer's | | axonmedchem |
| Alofanib - RPT835 | ES000835 | Axon 2930
CAS [1612888-66-0]
MF C19H15N3O6SMW 413.40
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Alofanib is an allosteric inhibitor of FGFR2 and significantly inhibited bFGF-induced proliferation of HUVEC cells (IC50 value of 11 nM) and suppressed proliferation of SVEC-4-10 cells (IC50 value of 58 nM). Moreover, Alofanib suppressed the migration activity of endothelial cells, and their ability to form vessel-like structures in vitro. Also, Alofanib significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo.
KEYWORDS: Alofanib | supplier | FGFR2 inhibitor | RPT835 | ES000835 | RPT 835 | RPT-835 | ES 000835 | ES-000835 | CAS [1612888-66-0] | FGF | FGFR | Inhibitor | Receptors | Ovarian cancer | | axonmedchem |
| Roblitinib - FGF 401 | NVP-FGF401 | Axon 2953
CAS [1708971-55-4]
MF C25H30N8O4MW 506.56
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Recently added | | axonmedchem |
| Naive Stem Cell 5i inhibitor Set | Axon 5011
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of five small molecule pathway inhibitors (termed as Naive stem cell 5i inhibitors): - BRAF inhibitor SB 590885 (Axon 2504) - MEK inhibitor PD 0325901 (Axon 1408) - ROCK inhibitor Y 27632 dihydrochloride (Axon 1683) - SRC/LCK inhibitor WH 4-023 (Axon 2381) - GSK3β inhibitor IM-12 (Axon 2511).(*Alternatively, CHIR99021 (Axon 1386) can be used as GSK3β inhibitor. Not included.) The combination of five inhibitors of MEK, GSK3β, BRAF, ROCK, and SRC, supports the expansion of viable OCT4-ΔPE-GFP+ human pluripotent cells after exogenous transcription factor expression has been removed. Useful tool for the induction and maintenance of human naive stem cell pluripotency.
Read more: Additional Product Information
Show all | | axonmedchem |
| Naive Stem Cell NHSM inhibitor Set - Stem Cell 6i inhibitor Set | Axon 5010
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of six small molecule pathway inhibitors (termed as Naive stem cell 6i or NHSM inhibitors): - GSK3 inhibitor CHIR 99021 (Axon 1386) - MEK inhibitor PD 0325901 (Axon 1408) - p38 inhibitor BIRB 796 (Axon 1358) - JNK inhibitor SP 600125 (Axon 2519) - PKC inhibitor Gö 6983 (Axon 2466) - ROCK inhibitor Y 27632 dihydrochloride (Axon 1683) These 6 small molecule inhibitors were used in the basic NHSM composition as published in Nature 2013 by Gafni et al. and with modifications at Hanna lab, the Weizmann Institute of Science (WIS). Useful tool for isolation, generation, derivatization and stabilization of naive human pluripotent stem cells.
Read more: Additional Product Information
Show all | | axonmedchem |
| SJ000291942 | Axon 2903
CAS [425613-09-8]
MF C16H15FN2O4MW 318.30
Purity:
99%
Soluble in DMSO
Description
SJ000291942 is an activator of the canonical bone morphogenetic protein (BMP) signaling pathway.
KEYWORDS: SJ000291942 | supplier | BMP activator | SJ 000291942 | SJ-000291942 | CAS [425613-09-8] | TGF-β | BMP-ALK | Activator | Receptors | Ventromorphin | C33A-2D2 | | axonmedchem |
| Stem Cell 4i inhibitor Set - iPSC-TSPC inhibitor Set | Axon 5009
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of four small molecule pathway inhibitors, ROCK inhibitor Thiazovivin (Axon 1535), TGF-β inhibitor SB 431542 (Axon 1661), MEK inhibitor PD 0325901 (Axon 1408) and GSK-3 inhibitor CHIR 99021 (Axon 1386) (termed as stem cell 4i or iPSC-TSPC). The small molecule cocktail of 4 inhibitors (SMC4) was reported to efficiently generate, characterize and maintain single cell and feeder-free (FF) cultural human induced pluripotent stem cells (iPSCs, or hiPSCs), hence a high-throughput reprogramming platform.
Read more: Additional Product Information
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References
Certificates
Categories
Extra info
S.M. Chambers et al. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature Biotechnol. 2012, 30, 715-720.
List of publications using PD 0325901 (Axon 1408) purchased from Axon Medchem
List of publications using CHIR 99021 (Axon 1386) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Apoptosis
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
ROCK
Wnt-β-Catenin
TGF-β
MAPK
PI3K-Akt-mTOR
Stem Cells
MEK
TGF-βR
Pfizer Licensed Products
Set of Thiazovivin, SB 431542, PD 0325901, and CHIR 99021 (inhibitors of ROCK, TGF-β, MEK, and GSK-3 resp.)
Chemical name
N.A.
Source information
Pfizer compound; Sold for research purposes under agreement from Pfizer Inc.
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
Each 2 mg
€190.00
In Stock | | axonmedchem |
| Stem Cell RG-BIX inhibitor Set | Axon 5008
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of two small molecule inhiitors, DNA methyltransferase (DNMT) inhibitor RG 108 (Axon 1691) and HMTase inhibitor BIX 01294 trihydrochloride (Axon 1692) (termed RG-BIX or RG/BIX). Combination of BIX 01294 and RG108 was reported to enhance the efficiency of induced pluripotent stem cell (iPS) generation.
Read more: Additional Product Information
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References
Certificates
Categories
Extra info
Y. Shi et al. A combined chemical and genetic approach for the generation of induced pluripotent stem cells. Cell Stem Cell. 2008, 2(6), 525-528.
T.V. Ho et al. in "Tissue Engineering in Regenerative Medicine. Stem Cell Biology and Regenerative Medicine". 2011. H.S. Bernstein (Ed.). ISBN 978-1-61779-321-9. Chapter 3: Current Status of Induced Pluripotent Stem Cells.2011, 39-52.
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Stem Cell
Stem Cells
DNA methyltransferase
HMTase
Set of RG 108 and BIX 01294 HCl, inhibitors of DNMT and HMTase, respectively
Chemical name
N.A.
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
Each 10 mg
€150.00
In Stock | | axonmedchem |
| Stem Cell Alternative 2i inhibitor Set | Axon 2130
CAS [N.A.]
MF N.A.MW N.A.
Purity:
99%
Soluble in DMSO
Description
A convenient set of SRC inhibitor CGP 77675 (Axon 2097) and GSK-3 inhibitor CHIR 99021 (Axon 1386); an alternative 2i inhibitor set vs the conventional 2i inhibitor set (Axon 2128) of MEK inhibitor PD 0325901 and GSK3 inhibitor CHIR 99021.
The dual inhibition of Src and GSK-3 signaling by CGP 77675 and CHIR 99021 (termed alternative 2i) was found to maintain mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression as efficiently as the dual inhibition of MAPK and GSK-3 by PD 0325901 and CHIR 99021 (conventional 2i, Axon 2128). This alternative 2i method provides a versatile tool not only for the maintenance of mESCs in serum-free conditions but also for the derivation of ESCs from mouse embryos.
Read more: Additional Product Information
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References
Certificates
Categories
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T. Shimizu et al. Dual inhibition of Src and GSK3 maintains mouse embryonic stem cells, whose differentiation is mechanically regulated by Src signaling. Stem Cells 2012, 30, 1394-1404.
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
SRC
Wnt-β-Catenin
PI3K-Akt-mTOR
Stem Cells
Set of SRC inhibitor CGP77675 (Axon 2097) and GSK-3 inhibitor CHIR99021 (Axon 1386)
Chemical name
N.A.
Parent CAS No.
[N.A.]
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Each 2 mg
€110.00
In Stock | | axonmedchem |
| Stem Cell LSC inhibitor Set | Axon 5005
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of BMP inhibitor LDN 193189 hydrochloride (Axon 1509), TGF-beta inhibitor SB 431542 (Axon 1661) and GSK-3 inhibitor CHIR 99021 (Axon 1386) (termed as LSC or LSB/CHIR by their name abbreviation), for differentiation of human pluripotent stem cells (hPSCs). Combining two-factor neuronal programming with small molecule–based inhibition of GSK-3β by CHIR 99021 (2 µM) and SMAD signaling by LDN 193189 (0.5 µM) and SB 431542 (10 µM), converted postnatal human fibroblasts into functional neuron-like cells with yields up to >200% and neuronal purities up to >80%.
LSC (or LSB/CHIR) inhibitor cocktail protocol can be further extended; with adding SU 5402 (Axon 1667) and DAPT (Axon 1484) to form LSB3i, a 5i inhibitor set (Axon 5007), for rapid differentiating hPSCs into nociceptors.
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References
Certificates
Categories
Extra info
J. Ladewig et al. Small molecules enable highly efficient neuronal conversion of human fibroblasts. Nat Methods. 2012, 9, 575-578.
S.M. Chambers et al. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature Biotechnol. 2012, 30, 715-720.
List of publications using LDN 193189 hydrochloride (Axon 1509) purchased from Axon Medchem
List of publications using CHIR 99021 (Axon 1386) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Apoptosis
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
TGF-β
PI3K-Akt-mTOR
Stem Cells
Stem Cell Differentiator
BMP-ALK
TGF-βR
Set of LDN 193189 HCl, SB 431542 and CHIR 99021, inhibitors of BMP, TGF-β, and GSK-3 resp.
Chemical name
N.A.
Parent CAS No.
[N.A.]
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Each 2 mg
€145.00
In Stock | | axonmedchem |