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经验公式(希尔记法):
C20H16N6S
化学文摘社编号:
分子量:
372.45
MDL number:
UNSPSC Code:
12352202
NACRES:
NA.77
产品名称
JNK Inhibitor V, The JNK Inhibitor V, also referenced under CAS 345987-15-7, controls the biological activity of JNK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
SMILES string
[s]1c2c(nc1C(c3nc(ncc3)NCCc4cnccc4)C#N)cccc2
InChI
1S/C20H16N6S/c21-12-15(19-25-17-5-1-2-6-18(17)27-19)16-8-11-24-20(26-16)23-10-7-14-4-3-9-22-13-14/h1-6,8-9,11,13,15H,7,10H2,(H,23,24,26)
InChI key
RCYPVQCPYKNSTG-UHFFFAOYSA-N
assay
≥95% (sum of two isomers, HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
desiccated (hygroscopic)
protect from light
color
yellow
solubility
DMSO: 10 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
hJNK 1, hJNK 2, hJNK 3
hJNK 1, hJNK 2, hJNK 3
Product competes with ATP.
Reversible: yes
Target IC50: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively
Disclaimer
Toxicity: Harmful (C)
General description
A cell-permeable pyrimidinyl compound that displays anti-inflammatory properties. Acts as a potent, reversible, and ATP-competitive inhibitor of c-Jun N-terminal kinase (JNK, IC50 = 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively) with a 10- to 100-fold greater selectivity over a panel of 25 other commonly studied kinases (IC50 typically in the range of 1-10 µM or no effect at 10 µM). Its in vivo efficacy has been demonstrated in gerbils, mice, and rats via oral, i.v., or i.p. administration.
Other Notes
Gaillard, P., et al. 2005. J. Med. Chem.48, 4596.
Carboni, S., et al. 2005. J. Neurochem.92, 1054.
Ferrandi, C., et al. 2004. Br. J. Pharmacol.142, 953.
Carboni, S., et al. 2004. J. Pharm. Exp. Ther.310, 25.
Carboni, S., et al. 2005. J. Neurochem.92, 1054.
Ferrandi, C., et al. 2004. Br. J. Pharmacol.142, 953.
Carboni, S., et al. 2004. J. Pharm. Exp. Ther.310, 25.
Soluble in DMSO, aliquot & store at -20*C; stable for 3 months
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 1
Biju Bhargavan et al.
Molecular neurobiology, 55(7), 5976-5992 (2017-11-13)
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Alba Corman et al.
PLoS biology, 19(5), e3001263-e3001263 (2021-05-26)
We here conducted an image-based chemical screen to evaluate how medically approved drugs, as well as drugs that are currently under development, influence overall translation levels. None of the compounds up-regulated translation, which could be due to the screen being
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