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
- UPC:
- 51286505
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 420129-5MG