MG JNK Inhibitor V 1PC x 5MG

Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargethJNK 1, hJNK 2, hJNK 3

Cell permeable: yes

Target IC₅₀: 150, 220, and 70 nM for hJNK1, hJNK2, and hJNK3, respectively

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.

Legal Information

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

Other Notes

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

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.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Harmful (C)