| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| LP-935509 | Axon 2638
CAS [1454555-29-3]
MF C20H24N6O3MW 396.44
Purity:
99%
Soluble in DMSO
Description
Potent, brain penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1; IC50 value 3.3 nM and 14 nM and 320 nM for the closely related BIKE and GAK enzymes, repsectively). LP-935509 is antinociceptive in multiple rat models of neuropathic pain, but not acute pain. The AAK1 inhibitor-induced antinociception and inhibition of spontaneous neural activity can be blocked by α2 adrenergic antagonists.
KEYWORDS: LP-935509 | supplier | AAK1 inhibitor | LP935509 | CAS [1454555-29-3] | AAK | neuropathic pain | adapter protein-2 | AP-2 | antinociceptive | nociception | SNF1 family | endocytosis | clathrin | Notch | | axonmedchem |
| Roquinimex - Linomide | LS 2616 | FCF 89 | ABR 21261 | Axon 2868
CAS [84088-42-6]
MF C18H16N2O3MW 308.33
Purity:
98%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Roquinimex has been demonstrated to have immunomodulating activity and antitumor effects. Effective stimulator of NK cells. Antiangiogenic.
KEYWORDS: Roquinimex | supplier | Immunomodulator | Linomide | LS 2616 | FCF 89 | ABR 21261 | PNU 212616 | CAS [84088-42-6] | Immunology | Non Selective | Modulator | NK cell | Antitumor | Antiangiogenic | | axonmedchem |
| MLN 2238 - Ixazomib | Axon 2556
CAS [1072833-77-2]
MF C14H19BCl2N2O4MW 361.03
Purity:
98%
Solubble in DMSO
Description
Selective and reversible inhibitor of the β5 subunit sites of the 20S proteasome with antitumor activity in various malignancies. MLN 2238 exhibits improved pharmacodynamics and antitumor activity compared with bortezomib in various B-cell lymphoma models, due to a greater tumor to blood ratio of proteasome inhibition that ultimately translates into improved tumor pharmacodynamic response and antitumor activity in several tumor xenograft models.
MLN 2238 is also available as the more stable citrate prodrug MLN 9708 (Axon 2557).
KEYWORDS: MLN 2238 | supplier | Proteasome inhibitor | Ixazomib | MLN2238 | CAS [1072833-77-2] | Ubiquitin | Proteasome 20S | Inhibitor | β5 subunit | B-cell lymphoma | FDA approved | MLN 9708 | | axonmedchem |
| ZCZ 011 | Axon 2543
CAS [1998197-39-9]
MF C21H18N2O2SMW 362.44
Purity:
99%
Soluble in DMSO
Description
Brain penetrant cannabinoid CB1 receptor positive allosteric modulator (PAM) which augments the in vitro and in vivo pharmacological actions of the CB1 orthosteric agonists CP55940 (pEC50 value 6.90) and N-arachidonoylethanolamine (AEA) and reduces neuropathic pain in the mouse with no psychoactive effects.
KEYWORDS: ZCZ 011 | supplier | PAM of CB1 | ZCZ011 | CAS [1998197-39-9] | Cannabinoids | CB1 | PAM | positive allosteric modulator | brain penetrant | neuropathic pain | | axonmedchem |
| Silibinin - Silybin | Silymarin I | Axon 2487
CAS [802918-57-6]
MF C25H22O10MW 482.44
Purity:
99%
Soluble in DMSO
Description
Natural flavonolignan, antihepatotoxic agent and antioxidant, exhibiting potent antitumor activities against various types of cancers. Interferes with many signaling pathways, such as notch, NF-κB, EGFR, SIRT1, PI3K/Akt and many others Mix of Silybin A and B
KEYWORDS: Silibinin | Natural Anti-cancer agent | supplier | Axon 2487 | Silybin | Silymarin I | 142797-34-0 | 802918-57-6 | 22888-70-6 | Antioxidant | antitumor | flavolignan | signaling | NF-κB | EGFR | Notch | SIRT | Pi3K | Akt | ERK | antihepatotoxic | cytoprotective | | axonmedchem |
| AM 4113 | Axon 2791
CAS [614726-85-1]
MF C17H12Cl3N3OMW 380.66
Purity:
99%
Soluble in DMSO
Description
Cannabinoid CB1 receptor antagonist. AM 4113 was able to bind with high affinity to CB1 receptors, exhibiting 100-fold selectivity for CB1 vs CB2 receptors (Ki values of 0.89 and 92 nM for CB1 and hCB2, respectively). AM 4113 does not show inverse agonist properties (ie no effects on cyclic-AMP production).
KEYWORDS: AM 4113 | supplier | CB1 antagonist | AM4113 | AM-4113 | CAS [614726-85-1] | Cannabinoids | CB1 | Antagonist | Receptors | | axonmedchem |
| NXY 059 - Disufenton sodium | Cerovive | Axon 1752
CAS [168021-79-2]
MF C11H13NNa2O7S2MW 381.33
Purity:
99%
Soluble in water
Description
Free radical scavenger, having neuroprotective potential for acute stroke
References
Certificates
Categories
Extra info
KR Lees et al. NXY-059 for Acute Ischemic Stroke. N. Engl. J. Med. 2006, 354, 588-600.
JJ Fong et al. NXY-059: Review of Neuroprotective Potential for Acute Stroke. Ann. Pharmacother. 2006, 40(3), 461-471.
Certificate of Analysis
Material Safety Data Sheet
CNS
Miscellaneous
Antioxidant
Free radical scavenger, neuroprotectant
Chemical name
sodium 4-((tert-butyloxidoimino)methyl)benzene-1,3-disulfonate
Parent CAS No.
[168021-77-0]
Order
Size
Unit Price
Stock
10 mg
€78.00
In Stock | | axonmedchem |
| Pirfenidone - AMR-69 | Axon 2647
CAS [53179-13-8]
MF C12H11NOMW 185.22
Purity:
100%
Soluble in DMSO
Description
Orally available agent with therapeutic potential for idiopathic pulmonary fibrosis (IPF; IC50 value 14.44 mM for inhibition of cell proliferation against MRC-5 cells) that has combined anti-inflammatory, antioxidant and antifibrotic effects in experimental models of pulmonary fibrosis. Mechanistically, Pirfenidone inhibits not only TGF-β-induced Smad3, p38 and Akt phosphorylation in human lung fibroblasts (HLFs), but also significantly increased RGS2 mRNA and protein expression in fibroblasts.
KEYWORDS: Pirfenidone | supplier | anti-inflammatory | anti-fibrosis agent | AMR-69 | AMR69 | CAS [53179-13-8] | Immunology | idiopathic | pulmonary fibrosis | IPF | antioxidant | antifibrotic | TGF-β | Smad3 | p38 | Akt | RGS2 | | axonmedchem |
| Stobadine | Axon 1467
CAS [85202-17-1]
MF C13H18N2MW 202.30
Purity:
99%
Soluble in 0.1N HCl(aq)
Description
Antioxidant; antiarrhythmic, cardiovascular drug
References
Certificates
Categories
Extra info
T Demiryurek et al. Effect of Stobadine on Leukocyte Free Radical Generation in Streptozotocin-Diabetic Rats: Comparison with Vitamin E. Pharmacology 2004, 70, 1-4.
L Horáková and S Stolc. Antioxidant and pharmacodynamic effects of pyridoindole stobadine. Gen Pharmacol. 1998, 30(5), 627-38.
Certificate of Analysis
Material Safety Data Sheet
Miscellaneous
Antioxidant
Antioxidant
Chemical name
(4aR,9bS)-2,8-Dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole
Parent CAS No.
[85202-17-1]
Order
Size
Unit Price
Stock
5 mg
€135.00
In Stock | | axonmedchem |
| CCG 232601 | Axon 2753
CAS [1922099-21-5]
MF C24H20ClF2N3O2MW 455.88
Purity:
99%
Soluble in DMSO
Description
Inhibitor of the Rho/MRTF/SRF signaling pathway (IC50 value of 0.55 μM (SRE.L assay)) as potential antifibrotic therapeutic for systemic scleroderma. CCG-232601 inhibited the development of bleomycin-induced dermal fibrosis in mice when administered orally.
KEYWORDS: CCG 232601 | supplier | Rho/MRTF/SRF inhibitor | CCG-232601 | CCG232601 | CAS [1922099-21-5] | Non Selective (Phosphorylation Substrates) | ROCK | Inhibitor | Enzymes | Scleroderma | Sclerosis | Antifibrotic | | axonmedchem |
| GlyH 101 | Axon 2572
CAS [328541-79-3]
MF C19H15Br2N3O3MW 493.15
Purity:
98%
Soluble in DMSO
Description
Highly potent and selective cystic fibrosis (CF) transmembrane regulator (CFTR) inhibitor (Ki value 4.3 µM in CFTR-expressing FRT cells) targeting mitochondrial functions, independently of chloride channel inhibition. GlyH 101 induces a rapid increase in ROS levels and depolarizes mitochondria in the four cell types, suggesting that these effects are independent of CFTR inhibition. Moreover, intraluminal GlyH 101 (2.5 g) reduced by 80% cholera toxin-induced intestinal fluid secretion in a closed-loop model of cholera.
KEYWORDS: GlyH 101 | supplier | CFTR inhibitor | GlyH101 | CAS [328541-79-3] | Chloride | CFTR | Inhibitor | Ion Channels | cystic fobrosis | cholera | diarrhea | inward rectifying | current | ROS | conductance | mitochondrial | | axonmedchem |
| KD025 - SLx-2119 | Axon 2780
CAS [911417-87-3]
MF C26H24N6O2MW 452.51
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
KD025 is a selective, ATP-competitive inhibitor of human ROCK2 (IC50 value of 105 nM) with minimal effects on human ROCK1 (IC50 value of 24 µM).
KEYWORDS: KD025 | supplier | ROCK2 inhibitor | SLx-2119 | KD 025 | KD-025 | SLx 2119 | SLx2119 | CAS [911417-87-3] | Non Selective (Phosphorylation Substrates) | ROCK | Inhibitor | Enzymes | Adipogenesis | Obesitas | 3T3-L1 | | axonmedchem |
| Eact | Axon 2576
CAS [461000-66-8]
MF C22H24N2O5SMW 428.50
Purity:
100%
Soluble in DMSO
Description
Strong activator of TMEM16A (ANO1; calcium activated chloride channel;CaCC) without elevating cytoplasmic Ca2+, producing outwardly rectifying currents (EC50 value 3 µM). Eact increases secretion by submucosal glands, as well as by airway surface cells exposed to a proinflammatory milieu; may be useful for treatment of cystic fibrosis (CF), dry mouth, and dry eye syndromes, and motility disorders of the gastrointestinal tract.
KEYWORDS: Eact | supplier | TMEM16A activator | CAS [461000-66-8] | Chloride | ANO1 | calcium activated chloride channel | CaCC | Ion Channel | rectifying current | secretion | cystic fibrosis | CF | dry | motility disorder | gastrointestinal tract | | axonmedchem |
| Ascorbyl dodecanoate, L- | Axon 1317
CAS [16690-40-7]
MF C18H30O7MW 358.43
Purity:
99%
Optical purity:
>98% ee
No solubility data
Description
Fat-soluble Vitamin C ester; antioxidant
References
Certificates
Categories
Extra info
Certificate of Analysis
Material Safety Data Sheet
Immunology
Miscellaneous
Antioxidant
Vitamin C ester; Antioxidant
Chemical name
Dodecanoic acid (S)-2-((R)-3,4-dihydroxy-5-oxo-2,5-dihydro-furan-2-yl)-2-hydroxy-ethyl ester
Parent CAS No.
[16690-40-7]
Order
Size
Unit Price
Stock
25 mg
€85.00
In Stock | | axonmedchem |
| Adjudin - AF 2364 | Axon 2552
CAS [252025-52-8]
MF C15H12Cl2N4OMW 335.19
Purity:
99%
Soluble in DMSO
Description
Non-hormonal male contraceptive that exerts its effect by disrupting Sertoli-germ cell adhesion junctions, most notably apical ectoplasmic specialization (apical ES), by targeting testin and actin filament bundles that disrupt the actin-based cytoskeleton in Sertoli cells. Adjudin is a potent blocker of Cl- channels. Moreover, Adjudin is shown to induce apoptosis in cancer cells through a Caspase-3-dependent pathway, and triggers mitochondrial dysfunction in cancer cells, apparently affecting the mitochondrial mass, inducing the loss of mitochondrial membrane potential and reducing cellular ATP levels. Furthermore, Adjudin posesses anti-inflammation, anti-neurodegeneration, and anti-ototoxicity activities based on studies using different in vitro and in vivo models.
KEYWORDS: Adjudin | supplier | Male contraceptive | AF 2364 | AF2364 | CAS [252025-52-8] | Chloride | CFTR | Inhibitor | Ion Channels | fertility | actin | testin | Sertoli-germ | apical ectoplasmic specialization | cytoskeleton | blocker | apoptosis | Caspase-3 | mitochondrial | dysfunction | cancer cells | membrane potential | ATP | | axonmedchem |
| AS 1892802 | Axon 2187
CAS [928320-12-1]
MF C20H19N3O2MW 333.38
Purity:
100%
Optical purity:
>99% e.e.
Soluble in DMSO
Description
Potent, selective, ATP-competitive, and orally active ROCK inhibitor (in vitro IC50 values 1.69 μM and 0.10 μM for ROCK1 and ROCK2 resp.) that reduces both inflammatory and non-inflammatory pain in rat models. Another group published IC50 values of 122, 52, and 57 nM for human ROCK1, ROCK2, and rat ROCK2 respectively. AS 1892802 dose dependently prevented the formation of tibial cartilage lesions due to MIA induction of osteoarthritis (OA), and completely inhibited IL-1α–induced PGE2 production. Additionally, it potently inhibited the phosphorylation of the ROCK substrate MLC2 in intact human breast cancer cells.
References
Certificates
Categories
Extra info
R. Li et al. Fragment-Based and Structure-Guided Discovery and Optimization of Rho Kinase Inhibitors. J. Med. Chem. 2012, 55, 2474−2478.
N. Takeshita et al. Alleviating Effects of AS1892802, a Rho Kinase Inhibitor, on Osteoarthritic Disorders in Rodents. J. Pharmacol. Sci. 2011, 115, 481–489.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
ROCK
TGF-β
EC 2.7.11.1
Potent, selective, ATP-competitive ROCK inhibitor
Chemical name
(S)-1-(2-hydroxy-1-phenylethyl)-3-(4-(pyridin-4-yl)phenyl)urea
Parent CAS No.
[928320-12-1]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| RKI 1447 | Axon 2229
CAS [1342278-01-6]
MF C16H14N4O2SMW 326.37
Purity:
99%
Soluble in DMSO
Description
Potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer (IC50 values 14.5 and 6.2 nM for ROCK 1 and 2 respectively).RKI 1447 is a Type 1 inhibitor that binds both the hinge region and the DFG motif of the ROCK ATP binding site.
References
Certificates
Categories
Extra info
R.A. Patel et al. RKI-1447 is a potent inhibitor of the Rho-associated ROCK kinases with anti-invasive and antitumor activities in breast cancer. Cancer Res. 2012, 72, 5025-5034.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
ROCK
TGF-β
EC 2.7.11.1
Potent inhibitor of the Rho-associated ROCK kinases
Chemical name
1-(3-hydroxybenzyl)-3-(4-(pyridin-4-yl)thiazol-2-yl)urea
Parent CAS No.
[1342278-01-6]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| AT 13148 dihydrochloride | Axon 2166
CAS [1056901-62-2]
MF C17H16ClN3O.2HClMW 386.70
Purity:
98%
Soluble in DMSO
Description
An oral, ATP-competitive inhibitor of multi-AGC kinases with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. AT13148 caused substantial blockade of AKT, p70S6K (S6K1), PKA, ROCK, and SGK substrate phosphorylation and induced apoptosis in cancer cells, with IC50 values of 38, 402, 50, 8, 3, 6, 4, 63 nM for AKT1, AKT2, AKT3, p70S6K, PKA, ROCK1, ROCK2, and SGK3 respectively.
References
Certificates
Categories
Extra info
TA Yap et al. AT13148 Is a Novel, Oral Multi-AGC Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity. Clin. Cancer Res. 2012.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
ROCK
Akt
PKA
PI3K-Akt-mTOR
EC 2.7.11.1
SGK
ATP-competitive inhibitor of multi-AGC kinases
Chemical name
(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol dihydrochloride
Parent CAS No.
[1056901-62-2]
Order
Size
Unit Price
Stock
2 mg
€85.00
In Stock | | axonmedchem |
| Y 27632 dihydrochloride | Axon 1683
CAS [129830-38-2]
MF C14H21N3O.2HClMW 320.26
Purity:
100%
Optical purity:
>98% ee
Soluble in water and DMSO
Description
Selective inhibitor of Rho-Kinase (ROCK), with IC50 values of 140-220 nM for ROCK1 and ROCK2. Y-27632 was found to increase human embryonic stem cell (hESC) survival
*Promotion | | axonmedchem |
| SC 79 | Axon 2507
CAS [305834-79-1]
MF C17H17ClN2O5MW 364.78
Purity:
98%
Soluble in DMSO
Description
Unique specific activator of cytosolic Akt (PKB) with the potential to recapitulate the primary cellular function of Akt signaling in a hippocampal neuronal culture system and a mouse model for ischemic stroke, resulting in augmented neuronal survival. Paradoxically, SC 79 suppressed PH-Akt-GFP plasma membrane translocation.
Close analogue of HA 14-1 (Axon 2007), a Bcl-2 antagonist (IC50 value 9 µM).
KEYWORDS: SC 79 | supplier | Akt activator | SC79 |CAS [305834-79-1] | Phosphatidylinositol | Akt | Activator | PKB | cytosolic | phosphorylation | ischemia | neuronal death | stroke | Bcl-2 | HA14-1 | plecstrin homolog | translocation | | axonmedchem |
| OAC2 | Axon 2651
CAS [6019-39-2]
MF C15H12N2OMW 236.27
Purity:
100%
Soluble in DMSO
Description
Oct4- and Nanog-activating compound that enhances 4F-induced reprogramming efficiency and considerably accelerates the generation of iPSC formation. OAC2 is one component of a mix of compounds (9C) that can be used to generate cardiomyocyte-like cells from human fibroblasts.KEYWORDS: OAC2 | supplier | Oct4 activator | CAS [6019-39-2] | DNA-RNA | Octamer | Transcription Factors | pluripotent | stem cell | fibroblast | reprogramming | iPSC | cardiomyocyte | | axonmedchem |
| FRAX 486 | Axon 2331
CAS [1232030-35-1]
MF C25H23Cl2FN6OMW 513.39
Purity:
99%
Soluble in DMSO
Description
Bioavailable and brain penetrating inhibitor of group I p21-activated kinases (IC50 values 8.25 nM, 39.5 nM, and 55.3 nM for PAK1, PAK2, and PAK3, respectively) with good selectivity over PAK4 (IC50 value 779 nM) FRAX486 rescues the dendritic spine abnormality and audiogenic seizures, and reduces autism-like phenotypes of hyperactivity and restrictive or repetitive behaviors in Fmr1 KO mice. Not only represents FRAX-486 a potential breakthrough in the research for a treatment of Fragile X syndrome (FXS), it was also found to ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence.
References
Certificates
Categories
Extra info
B.M. Dolan et al. Rescue of fragile X syndrome phenotypes in Fmr1 KO mice by the small-molecule PAK inhibitor FRAX486. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5671-6.
A. Hayashi-Takagi et al. PAKs inhibitors ameliorate schizophrenia-associated dendritic spine deterioration in vitro and in vivo during late adolescence. Proc Natl Acad Sci U S A. 2014 Apr 29;111(17):6461-6.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Signaling & Oncology
CNS
Immunology
Pain & Inflammation
EC 2.7.11.1
PAK
Bioavailable, brain penetrating inhibitor of p21-activated kinases (PAKs)
Chemical name
6-(2,4-dichlorophenyl)-8-ethyl-2-(3-fluoro-4-(piperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one
Parent CAS No.
[1232030-35-1]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| CC-930 - Tanzisertib | Axon 2634
CAS [899805-25-5]
MF C21H23F3N6O2MW 448.44
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl (aq) and DMSO
Description
Potent, selective, and orally active anti-fibrotic JNK inhibitor (IC50 values 61 nM, 7 nM, 6 nM, 480 nM, and 3400 nM for JNK1, JNK2, JNK3, ERK1, and p38α, respectively) for treatment of idiopathic pulmonary fibrosis (IPF).KEYWORDS: CC-930 | supplier | JNK inhibitor | Tanzisertib | CC930 | CAS [899805-25-5] | MAPK | c-Jun N-terminal kinase | JNK | JNK1 | JNK2 | JNK3 | p38α | idiopathic pulmonary fibrosis | IPF | TGF | | axonmedchem |
| HA 14-1 | Axon 2007
CAS [65673-63-4]
MF C17H17BrN2O5MW 409.23
Purity:
98%
Soluble in DMSO and Ethanol
Description
Bcl-2 antagonist and apoptosis inducer of tumor cells; HA14-1 induces the activation of Apaf-1 and caspases.
References
Certificates
Categories
Extra info
JL Wang et al. Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells. PNAS 2000, 97(13), 7124-7129.
J Skommen et al. HA14-1, a small molecule Bcl-2 antagonist, induces apoptosis and modulates action of selected anticancer drugs in follicular lymphoma B cells. Leukemia Res. 2006, 30(3), 322–331.
JM Doshi et al. Structure-activity relationship studies of ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate (HA 14-1), an antagonist for antiapoptotic Bcl-2 proteins to overcome (...). J. Med. Chem. 2006, 49(26), 7731-7739.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Bcl
Bcl-2 inhibitor and apoptosis inducer of tumor cells
Chemical name
ethyl 2-amino-6-bromo-4-(1-cyano-2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
Parent CAS No.
[65673-63-4]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| SB 590885 | Axon 2504
CAS [405554-55-4]
MF C27H27N5O2MW 453.54
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and selective inhibitor of B-Raf kinase (Kd value 0.3 nM for BRAF), devoid of significant activity against a wide panel of enzymes, including p38α, GSK3β, and Lck. SB590885 maintains OCT4-ΔPE-GFP reporter activity and pluripotency gene expression in human ESCs after removal of exogenous KLF2 and NANOG expression, preserving the best colony morphology and proliferation.
SB 590885 is frequently used in a combination of five compounds, including inhibitors of MEK, GSK-3β, BRAF, ROCK, and SRC, which support the expansion of viable OCT4-ΔPE-GFP+ human pluripotent cells after exogenous transcription factor expression has been removed:
Axon 2504
SB 590885
BRAF inhibitor
Axon 2511
IM 12
GSK-3β inhibitor
Axon 1408
PD 0325901
MEK inhibitor
Axon 1683
Y 27632
ROCK inhibitor
Axon 2381
WH4-023
Lck/Src inhibitor
(alternatively, CHIR 99021 (Axon 1386) could be used as GSK-3β inhibitor)
Naive Stem Cell 5i inhibitor Set is commercially available (Axon 5011)
KEYWORDS: SB 590885 | Supplier | BRAF inhibitor | SB590885 | CAS [405554-55-4] | MEK | RAF | Inhibitor | pluripotent | ESC | stem cell | proliferation | MAPK | cancer | tumor | | axonmedchem |
| EHop 016 | Axon 2351
CAS [1380432-32-5]
MF C25H30N6OMW 430.55
Purity:
99%
Soluble in DMSO
Description
EHop 016 is a Rac GTPase inhibitor (IC50 value 1.1 µM) specific for Rac1 and Rac3 at concentrations of 5 µM, and inhibits the interaction of Vav2 with Rac1 at physiologically relevant concentrations. Moreover, EHop-016 inhibits the activation of the Rac downstream effector p21-activated kinase (PAK), extension of motile actin-based structures, and cell migration. EHop-016 is ~100 times more potent than NSC 23766 (Axon 1578) and 10–50 times more potent than other currently available Rac inhibitors.
References
Certificates
Categories
Extra info
B.L. Montalvo-Ortiz et al. Characterization of EHop-016, novel small molecule inhibitor of Rac GTPase. J. Biol. Chem. 2012, 287, 13228-13238.
S. Dharmawardhane et al. Development of EHop-016: a small molecule inhibitor of Rac. In Enzymes 2013, 33, 117-146. Ed. F. Tamanoi.
Certificate of Analysis
Material Safety Data Sheet
Cell Cycle Regulation
Cell Signaling & Oncology
Stem Cell
EC 3.6.5.2
Rac
PAK
Rac GTPase inhibitor specific for Rac1 and Rac3
Chemical name
N4-(9-ethyl-9H-carbazol-3-yl)-N2-(3-morpholinopropyl)pyrimidine-2,4-diamine
Parent CAS No.
[1380432-32-5]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| SP 600125 - NSC 75890 | Axon 2519
CAS [129-56-6]
MF C14H8N2OMW 220.23
Purity:
98%
Soluble in DMSO
Description
Reversible ATP-competitive JNK inhibitor (IC50 values 40 nM, 40 nM, and 90 nM for JNK1, JNK2 and JNK3, respectively) with >20-fold selectivity vs. a range of kinases and enzymes tested. SP600125 caused G2/M cell cycle arrest and elevation of cyclin B1 and p27(kip), thereby inhibiting cell proliferation and increasing apoptosis in multiple cell lines. Moreover, SP600125 dose dependently inhibits phosphorylation of c-Jun, the expression of inflammatory genes COX-2, IL-2, IFN-γ, TNF-α, and prevents activation and differentiation of primary human CD4 cell cultures; SP600125 has proven to be a useful tool for isolation, generation, derivatization and stabilization of naive human pluripotent stem cells in so called NHSM conditions developed at the Weizmann Institute of Science.
*Promotion | | axonmedchem |
| RAF709 | Axon 2817
CAS [1628838-42-5]
MF C28H29F3N4O4MW 542.55
Purity:
99%
Soluble in DMSO
Recently added | | axonmedchem |
| BT2 | Axon 2334
CAS [34576-94-8]
MF C9H4Cl2O2SMW 247.10
Purity:
99%
Soluble in DMSO
Description
Allosteric inhibitor of branched-chain α-ketoacid dehydrogenase (BCKDC) kinase (BDK; IC50 value 3.19 μM). BT 2 binding to BDK results in the dissociation of BDK from the BCKDC accompanied by accelerated degradation of the released kinase in vivo. BT 2 is also known to inhibit the Bcl-2 family member Mcl-1 (Ki value 59 µM).
References
Certificates
Categories
Extra info
A. Friberg et al. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J. Med. Chem. 2013, 56, 15-30.
S.C. Tso et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J. Biol. Chem. 2014, 289, 20583-20593.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Diabetes & Metabolism
BDK
Mcl-1
EC 2.7.11.4
Allosteric inhibitor of BCKDC kinase (BDK) and Mcl-1 inhibitor
Chemical name
3,6-dichlorobenzo[b]thiophene-2-carboxylic acid
Parent CAS No.
[34576-94-8]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| MBQ-167 | Axon 2777
CAS [2097938-73-1]
MF C22H18N4MW 338.41
Purity:
98%
Soluble in DMSO
Description
MBQ-167 is an effective Rac and Cdc42 inhibitor with IC50 values of 78 nM and 103 nM, respectively. MBQ-167 significantly decreases Rac and Cdc42 downstream effector p21-activated kinase (PAK) signaling and the activity of STAT3, without affecting Rho, MAPK, or Akt activities. MBQ-167 also inhibits breast cancer cell migration, viability, and mammosphere formation.
KEYWORDS: MBQ-167 | supplier | Rac/Cdc42 inhibitor | MBQ167 | MBQ 167 | CAS [2097938-73-1] | Cytoskeleton | Rac | CDC42 | Inhibitor | Enzymes | PAK | STAT3 | Breast Cancer | | axonmedchem |
| GW 5074 | Axon 1984
CAS [220904-83-6]
MF #N/AMW #N/A
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Potent, brain-permeable inhibitor of c-Raf (IC50 value 9 nM) when tested in vitro with no effect on the activities of CDK1/2/5/6, JNK1/2/3, c-Src, MEK1, p38 MAP kinase, VEGFR2, and c-fms. In contrast to its effect in vitro, treatment of neurons with GW 5074 causes c-Raf activation (when measured in vitro inthe absence of the drug) and stimulates the Raf-MEK-ERK pathway. GW 5074 protects neurons from death in culture and in an in vivo paradigm of neurodegeneration.
KEYWORDS: GW 5074 | supplier | C-Raf inhibitor | GW5074 | CAS [220904-83-6] | MEK | RAF | Inhibitor | Raf-1 | cell-permeable | activation | Raf-MEK-ERK | pathway | CNS | neurodegeneration | neuroprotection | | axonmedchem |
| AZ13705339 | Axon 2669
CAS [2016806-57-6]
MF C33H36FN7O3SMW 629.75
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
AZ13705339 is a potent and selective PAK1 inhibitor (IC50 value of 0.33 nM). In vitro probe compound.
KEYWORDS: AZ13705339 | supplier | PAK1 inhibitor | AZ 13705339 | AZ-13705339 | CAS [2016806-57-6] | Non Selective (Phosphorylation Substrates) | PAK | Inhibitor | Enzymes | | axonmedchem |
| ML 311 | Axon 2823
CAS [315698-17-0]
MF C23H24F3N3OMW 415.45
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of the protein-protein interaction of Mcl-1 and Bim with an IC50 value of 0.31 µM for Mcl-1. ML 311 displayed significant activity in a number of cell lines, with EC50 values in the range of 0.3–15 M. Useful tool for studying lymphoid tumorigenesis and to demonstrate the potential for using this strategy in therapies intended to bypass apoptosis resistance pathways that are activated in drug-resistant tumors.
Keywords: ML 311 | supplier | Mcl-1-Bim interaction inhibitor | ML311 | ML-311 | CAS [315698-17-0] | Non Selective | Mcl-1 | Inhibitor | Proteins | Lymphoid Tumorigenesis | Bim | | axonmedchem |
| BQU 57 | Axon 2397
CAS [1637739-82-2]
MF C16H13F3N4OMW 334.30
Purity:
99%
Soluble in DMSO
Description
Inhibitor of the RAS-like small GTPases RalA and RalB (Kd value 7.7 µM for RalB-GDP; IC50 values 2.0 mM and 1.3 mM for growth inhibition in H358 and H2122 tumor xenografts, respectively). BQU57 shows selectivity for Ral relative to the GTPases Ras and RhoA. Mechanistically, BQU-57 inhibits the binding of Ral proteins in their GDP-bound form to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. Close analogue of RBC 8 (Axon 2396)
References
Certificates
Categories
Extra info
C. Yan et al. Small molecules inhibit the RAS-like small GTPases RALA and RALB. Cancer Discov. 2014 Nov;4(11):1251.
C. Yan et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-7.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
MAPK
EC 3.6.5.2
RalA
RalB
Inhibitor of the RAS-like small GTPases RalA and RalB
Chemical name
6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
Parent CAS No.
[1637739-82-2]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| RBC 8 | Axon 2396
CAS [361185-42-4]
MF C25H20N4O3MW 424.45
Purity:
99%
Soluble in DMSO
Description
Inhibitor of the RAS-like small GTPases RalA and RalB (IC50 values 3.5 μM and 3.4 μM for growth inhibition in H2122 and H358 tumor xenografts, respectively). RBC8 shows selectivity for Ral relative to the GTPases Ras and RhoA. Mechanistically, RBC8 inhibits the binding of Ral proteins in their GDP-bound form to its effector RALBP1, as well as inhibiting Ral-mediated cell spreading of murine embryonic fibroblasts and anchorage-independent growth of human cancer cell lines. Close analogue of BQU 57 (Axon 2397)
KEYWORDS: RBC 8 | supplier | RalA/B inhibitor | RBC8 | CAS [361185-42-4] | GTP | RalA | RalB | Inhibitor | Enzymes | Ral | Ras-like | GTPase | xenograft | RALBP1 | GDP | GTP | switch | cancer | fibroblasts | | axonmedchem |
| CID 1067700 | Axon 2184
CAS [314042-01-8]
MF C18H18N2O4S2MW 390.48
Purity:
99%
Soluble in DMSO
Description
First inhibitor of Rab7 GTPase exhibiting significant inhibitory potency on Rab7 nucleotide binding with nanomolar inhibitor (Ki) values and an inhibitory response of ≥97% for BODIPY-GTP and BODIPYGDP binding (Ki values 13 nM and 19 nM, and EC50 values 11 and 21 nM, respectively). CID 1067700 is a competitive guanine nucleotide binding inhibitor characterized for the Ras-super family of GTPases.
References
Certificates
Categories
Extra info
J.O. Agola et al. A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition. ACS Chem. Biol. 2012, 7, 1095-1108.
Certificate of Analysis
Material Safety Data Sheet
Apoptosis
Cell Cycle Regulation
Cell Signaling & Oncology
Epigenetics
Immunology
MAPK
EC 3.6.5.2
Rab7
First inhibitor of Rab7 GTPase
Chemical name
2-(3-benzoylthioureido)-5,5-dimethyl-5,7-dihydro-4H-thieno[2,3-c]pyran-3-carboxylic acid
Parent CAS No.
[314042-01-8]
Order
Size
Unit Price
Stock
10 mg
€125.00
In Stock | | axonmedchem |
| PLX 4032 - RG 7204 | Vemurafenib | RO 5185426 | Axon 1624
CAS [918504-65-1]
MF C23H18ClF2N3O3SMW 489.92
Purity:
98%
Soluble in DMSO
Description
Selective inhibitor of protein kinase, targeting B-Raf (V600E) (IC50: 44 nM); PLX4032 has been shown to cause programmed cell death in melanoma cell lines; a potential anti-tumor agent under clinical trials
References
Certificates
Categories
Extra info
G Bollag et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010, 467, 596–599.
PI Poulikakos et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010, 464, 427-430.
E Sala et al. BRAF Silencing by Short Hairpin RNA or Chemical Blockade by PLX4032 Leads to Different Responses in Melanoma and Thyroid Carcinoma Cells. Mol. Cancer Res. 2008, 6(5), 751-759.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.1
RAF
B-Raf protein kinase inhibitor
Chemical name
N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide
Parent CAS No.
[918504-65-1]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| Locostatin - UIC 1005 | Axon 2590
CAS [90719-30-5]
MF C14H15NO3MW 245.27
Purity:
100%
Optical purity:
Optically pure
Soluble in DMSO and Ethanol
Description
Non-toxic Raf kinase inhibitory protein (RKIP) inhibitor; disrupts the interaction of RKIP, not only with Raf-1 kinase, but also with GRK2; Locostatin is an inhibitor of cell sheet migration and cell growth in an epithelial cell proliferation assay, and it induced T cell anergy by blocking cytokine production after Ag recall. Other evidence suggested that Locostatin’s effects on cytoskeletal structure and migration are caused through mechanisms independent of its binding to RKIP and Raf/MAP kinase signaling.
KEYWORDS: Locostatin | supplier | RKIP/Raf inhibitor | UIC 1005 | UIC1005 | (N-crotonyl)-(4S)-isopropyl-2-oxazolidinone | (S)-(+)-4-benzyl-3-crotonyl-2-oxazolidinone | CAS [90719-30-5] | MAPK | MEK | RAF | Inhibitor | PEBP1 | Phosphatidylethanolamine Binding Protein | cell sheet migration | NF-kB | NIK | PKC | GPCR kinase 2 | | axonmedchem |
| AZ 628 | Axon 1545
CAS [878739-06-1]
MF C27H25N5O2MW 451.52
Purity:
99%
Soluble in DMSO
Description
Selective RAF inhibitor, showing strong selectivity for RAF kinases among a panel of 150 tested kinases; IC50 values: ca 30 nM for BRAF V600E and wild-type CRAF and 100 nM for wild-type BRAF
References
Certificates
Categories
Extra info
C Montagut et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res. 2008, 68(12), 4853–4861.
G Hatzivassiliou et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature 2010, 464, 431-435.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.1
RAF
B-Raf and C-Raf protein kinase inhibitor
Chemical name
3-(Cyano-dimethyl-methyl)-N-[4-methyl-3-(3-methyl-4-oxo-3,4-dihydro-quinazolin-6-ylamino)-phenyl]-benzamide
Parent CAS No.
[878739-06-1]
Order
Size
Unit Price
Stock
5 mg
€80.00
In Stock | | axonmedchem |
| PLX 4720 | Axon 1474
CAS [918505-84-7]
MF C17H14ClF2N3O3SMW 413.83
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of protein kinase, targeting B-Raf (V600E)
References
Certificates
Categories
Extra info
J Tsai et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci USA. 2008, 105(8), 3041-3046.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.1
RAF
B-Raf protein kinase inhibitor
Chemical name
Propane-1-sulfonic acid [3-(5-chloro-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide
Parent CAS No.
[918505-84-7]
Order
Size
Unit Price
Stock
2 mg
€60.00
In Stock | | axonmedchem |
| GDC 0879 | Axon 1459
CAS [905281-76-7]
MF C19H18N4O2MW 334.37
Purity:
99%
Soluble in DMSO
Description
Selective inhibitor of protein kinase, targeting B-Raf (V600E)
References
Certificates
Categories
Extra info
KP Hoeflich et al. Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/MAPK pathway suppression. Cancer Res. 2009, 69(7), 3042-3051.
H Wong et al. Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3- (pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor. J. Pharmacol. Exp. Ther. 2009, 329(1), 360-367.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
EC 2.7.11.1
RAF
B-Raf protein kinase inhibitor
Chemical name
5-[1-(2-Hydroxy-ethyl)-3-pyridin-4-yl-1H-pyrazol-4-yl]-indan-1-one oxime
Parent CAS No.
[905281-76-7]
Order
Size
Unit Price
Stock
2 mg
€70.00
In Stock | | axonmedchem |
| Sorafenib tosylate - BAY 43-9006 | Nexavar | Axon 1397
CAS [475207-59-1]
MF C21H16ClF3N4O3.C7H8O3SMW 637.03
Purity:
99%
Soluble in DMSO
Description
Small molecule inhibitor of protein kinase, targeting the Raf/Mek/Erk pathway
References
Certificates
Categories
Extra info
DJ Panka et al. The Raf Inhibitor BAY 43-9006 (Sorafenib) Induces Caspase-Independent Apoptosis in Melanoma Cells. Cancer Res 2006, 66(3), 1611-1619.
SM Wilhelm et al. BAY 43-9006 Exhibits Broad Spectrum Oral Antitumor Activity and Targets the RAF/MEK/ERK Pathway and Receptor Tyrosine Kinases Involved in Tumor Progression and Angiogenesis. Cancer Res. 2004, 64, 7099-7109.
SM Wilhelm et al. The novel Raf inhibitor Bay 43-9006 blocks signaling and proliferation in BRAF mutant and wildtype melanoma and colorectal tumor cell lines. Proc. Am. Assoc. Cancer Res. 2003, 44, 106609.
S. S. Sridhar et al. Raf kinase as a target for anticancer therapeutics. Mol Cancer Ther. 2005, 4, 677-685.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
MAPK
PI3K-Akt-mTOR
EC 2.7.11.1
RAF
Protein kinase inhibitor of Raf/MEK/ERK pathway
Chemical name
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]phenoxy]-N-methyl-pyridine-2-carboxamide
Parent CAS No.
[284461-73-0]
Order
Size
Unit Price
Stock
10 mg
€80.00
In Stock | | axonmedchem |
| Cuspin-1 | Axon 2438
CAS [337932-29-3]
MF C13H10BrNOMW 276.13
Purity:
99%
Soluble in DMSO
Description
Small molecule upregulator of the Survival of Motor Neuron protein (SMN; EC50 value 18 μM in SMA patient fibroblast cells); a tool compound that revealed that increasing Ras signaling upregulates SMN protein levels by increased phosphorylation of Erk, an important member of the Ras-Raf-MEK signaling cascade.
KEYWORDS: Cuspin 1 | Supplier | SMN upregulator | Axon Medchem | Axon 2438 | Cuspin1 | CAS [337932-29-3] | GTP | RAS | RAF | MEK | ERK | Activator | Enzymes | Survival of Motor Neuron Protein | SMN | SMA | fibroblasts | Spliceosome | RNP | | axonmedchem |
| BIRB 796 - BIRB 0796 | Doramapimod | Axon 1358
CAS [285983-48-4]
MF C31H37N5O3MW 527.66
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Small molecule inhibitor of p38 mitogen-activated protein (MAP) kinase (MAPK); more potent than SB 203580 (Axon 1363) on p38α and p38β MAPKs; potential agent for the treatment of inflammatory diseases
*Promotion | | axonmedchem |
| WH-4-023 | Axon 2381
CAS [837422-57-8]
MF C32H36N6O4MW 568.67
Purity:
99%
Soluble in DMSO
Description
Orally active inhibitor of Lck and Src (IC50 values 2 nM and 6 nM for Lck and Src, respectively) with an >300-fold selectivity over p38α and KDR.
*Promotion | | axonmedchem |
| PD 0325901 | Axon 1408
CAS [391210-10-9]
MF C16H14F3IN2O4MW 482.19
Purity:
99%
Optical purity:
>98% ee
Soluble in DMSO
Description
Potent, highly specific non-ATP-competitive inhibitor of MEK (aka MKK) 1/2; a derivative of CI-1040 (Axon 1368) to improve bioavailability; clinical candidate and highly recommended tool to inhibit MKK1 or MKK1 plus MKK5 in cells.* PD 0325901 and CHIR 99021 (Axon 1386) from Axon Medchem are often used together as perfect 2i in stem cell research (Axon 2128).
*Promotion | | axonmedchem |
| BIX 02188 | Axon 1808
CAS [334951-92-7]
MF C26H26N4O2MW 426.51
Purity:
99%
Soluble in DMSO
Description
Selective dual MEK5 kinase inhibitor, with IC50 values of 4.3, 810, 1800, and >6300 nM for MEK5, ERK5, TGFbR1 and other closely related kinases respectively.
References
Certificates
Categories
Extra info
RJ Tatake et al. Identification of pharmacological inhibitors of the MEK5/ERK5 pathway. Biochem. Biophys. Res. Comm. 2008, 377(1), 120–125.
Y Obara and N Nakahata. The signaling pathway leading to extracellular signal-regulated kinase 5 (ERK5) activation via G-proteins and ERK5-dependent neurotrophic effects. Mol. Pharmacol. 2010, 77(1), 10-16.
BA Drew, ME Burowa , BS Beckman. MEK5/ERK5 pathway: The first fifteen years. Biochimica et Biophysica Acta (BBA) - Reviews on Cancer 2012, 1825 (1), 37-48.
E. Razumovskaya et al. Inhibition of MEK5 by BIX02188 induces apoptosis in cells expressing the oncogenic mutant FLT3-ITD. Biochem. Biophys. Res. Commun. 2011, 412, 307-312.
Certificate of Analysis
Material Safety Data Sheet
Cell Signaling & Oncology
Stem Cell
MAPK
EC 2.7.12.2
ERK
MEK
MEK5 inhibitor; ERK5 inhibitor
Chemical name
(Z)-3-((3-((dimethylamino)methyl)phenylamino)(phenyl)methylene)-N-methyl-2-oxoindoline-6-carboxamide
Parent CAS No.
[334951-92-7]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| CRT0066854 | Axon 2656
CAS [1438881-19-6]
MF C24H25N5SMW 415.55
Purity:
99%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Selective ATP-competitive inhibitor of the atypical PKC isoenzymes (IC50 values 639 nM and 132 nM, for full-length PKCζ, PKCι, respectively). CRT0066854 decreased colony formation in HeLa cells, inhibits LLGL2 phosphorylation and polarized epithelial morphogenesis, and impedes directed migration of NRK cells. A chemical tool to further dissect PKCζ and PKCι roles in establishing cell polarity and growth-factor-stimulated signalling pathways.
KEYWORDS: CRT0066854 | supplier | PKC inhibitor | CRT-0066854 | CAS [1438881-19-6] | Phosphorylation | protein kinase C | aPKC | AGC | PKCζ | PKCι | ATP | LLGL2 | colony | lumen formation | migration | zeta | iota | | axonmedchem |
| Squarunkin A | Axon 2778
CAS [2101958-02-3]
MF C25H32F3N5O4MW 523.55
Purity:
99%
Soluble in DMSO
Description
Squarunkin A selectively inhibits the binding of a myristoylated peptide representing the N-terminus of Src kinase to UNC119A with an IC50 value of 10 nM. It binds to UNC119 proteins in cell lysate and interferes with the activation of Src kinase.
KEYWORDS: Squarunkin A | supplier | UNC119–cargo interaction inhibitor | Squarunkin-A | CAS [2101958-02-3] | Non Selective | SRC | Inhibitor | Enzymes | Myristoyl | | axonmedchem |
| PH 797804, (±)- - rac-PH 797804 | rac-PH 797804 | Axon 2786
CAS [586379-66-0]
MF C22H19BrF2N2O3MW 477.30
Purity:
99%
Soluble in DMSO and ethanol
Description
Similar to the (-)-atropisomer PH 797804 (Axon 1837), racemic (±)-PH 797804 is a potent, selective and metabolically stable inhibitor of p38 MAPK (IC50 values of 2.5 and 15 nM in p38α cascade and hPBMC TNF assays, respectively).
KEYWORDS: PH 797804, (±)- | | axonmedchem |