420129
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.
别名:
JNK Inhibitor V, SAPK Inhibitor V, 1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile, AS601245
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关于此项目
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
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
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.
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
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.
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
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
存储类别
11 - Combustible Solids
wgk
WGK 1
Biju Bhargavan et al.
Molecular neurobiology, 55(7), 5976-5992 (2017-11-13)
HIV-1-associated neurocognitive disorders (HAND) is associated with blood-brain-barrier (BBB) inflammation, and inflammation involves toll-like receptors (TLRs) signaling. It is not known whether primary human brain microvascular endothelial cells (HBMEC), the major BBB component, express TLRs or whether TLRs are involved
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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