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Sigma-Aldrich

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.

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Synonym(s):
JNK Inhibitor V, SAPK Inhibitor V, 1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile, AS601245
Empirical Formula (Hill Notation):
C20H16N6S
CAS Number:
Molecular Weight:
372.45

Quality Level

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

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

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
Product competes with ATP.
Reversible: yes
Target IC50: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively

Packaging

Packaged under inert gas

Warning

Toxicity: Harmful (C)

Reconstitution

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.
Soluble in DMSO, aliquot & store at -20*C; stable for 3 months

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 1


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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
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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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