Protein Kinase Inhibitor (PKI, SP600125Anthra[1,9-cd]pyrazol-6(2H)-one)

Novel, potent and selective JNK-1,-2, and -3 inhibitor (Ki=0.19uM). SP600125 is an ATP-competitive reversible inhibitor with >20-fold selectivity vs. a range of kinases and enzymes tested. In cells, SP600125 caused a dose-dependent inhibition of the phosphorylation of c-Jun, the expression of inflammatory genes IL-2, COX-2, TNF-a, IFN-gamma, and blocked the activation and differentiation of primary human CD4 cell cultures. In animal studies, SP600125 inhibited bacterial lipopolysaccharide-induced expression of tumor necrosis factor-a and prevented anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. Melting Point: 290.5-295.5°C, Solubility: Prepare initial stock solutions in DMSO (soluble at 65mg/ml) for in vitro use, solubility in ethanol or water is low. Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.