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.

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

Packaged under inert gas

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

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

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

Toxicity: Harmful (C)