货号：S2230

储存条件：粉末-20°C可保存3年；液体-80°C可保存12月。 

产品描述

c-Jun N-terminal kinase (JNK) is a serine threonine protein kinase that belongs to the mitogen-activated protein kinase family. SP-600125 is an anthrapyrazolone inhibitor of JNK with IC50 values of 40, 40, and 90nM for JNK1, JNK2, and JNK3, respectively. SP-600125 also exhibits inhibitory activity against p56Lck, MMK3, MMK4, MMK6, MM7, PKB/AKT, and PKCα with IC50 values of 4.3, 1.5, 0.4, 1.0, 5.1, 1.0, and 1.5μM, respectively. SP-600125 inhibited JNK2 in an ATP-competitive manner with a Ki value of 0.19±0.06μM. It inhibited the phosphorylation of c-Jun in Jurkat T cells with an IC50 value of 5-10μM. In cells stimulated with PMA and phytohemagglutinin, SP-600125 inhibited both IL-2 and IFN-γ expression in a dose-dependent manner with IC50 values of 6 and 7μM, respectively. The incubation of Th1 cells with SP-600125 for 5 days potently inhibited the expression of IFN-γ, TNF-α, and IL-10 (IC50 = 7-12μM), but only weakly blocked the production of IL-1β and IL-6 (IC50 > 30μM). In primary human peripheral blood mononuclear cells stimulated with LPS (100 ng/ml) for 4 h, treatment with SP-600125 dose-dependently inhibited the mRNA expression of COX-2 and TNF-α with IC50 values of 5 and 10μM. In CD-1 mice induced with LPS, intravenous administration of SP-600125 significantly decreased the serum level of TNF-α at doses of 15 and 30mg/kg, while oral administration of 30mg/kg SP-600125 significantly inhibited TNF-α expression compared to the vehicle-treated group. 

作用机制

SP-600125 is a small-molecule, ATP-competitive inhibitor of JNK

产品信息