AS601245
1,3-Benzothiazol-2-yl-(2-((2-(3-pyridinyl)ethyl)amino)-4-pyrimidinyl)acetonitrile
SAPK Inhibitor V Yellow solid. PROTECT FROM LIGHT. HYGROSCOPIC. PACKAGED UNDER INERT GAS. A cell-permeable pyrimidinyl compound that displays anti-inflammatory properties. Acts as a potent 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. Purity: ≥95% by HPLC (sum of two isomers). CAS 345987-15-7. Ref.: 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. |
