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抑制剂描述:

产品名称:SP600125

产品别名:见爱必信官网

英文别名:SP600125

靶点:JNK;Autophagy

CAS:129-56-6

纯度:>98 %

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

SP600125是一种广谱JNK抑制剂,作用于JNK1,JNK2和JNK3,无细胞试验中IC50分别为40nM,40nM和90nM,比作用于MKK4选择性高10倍,比作用于MKK3,MKK6,PKB,和PKCα选择性高25倍,比作用于ERK2,p38,Chk1,EGFR等选择性高100倍。

溶解性:DMSO: ≥ 44 mg/mL

体外研究:

SP600125 is originally characterized as a selective ATP-competitive inhibitor of c-Jun N-terminal kinase JNK. In Jurkat T cells, SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM. However, later studies reveal that SP600125 also suppresses aryl hydrocarbon receptor (AhR) , Mps1 , and a panel of other serine/threonine kinases, including Aurora kinase A, FLT3, MELK, and TRKA .In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation. In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1.

体内研究:In mice, SP600125 (15 mg/kg or 30 mg/kg) significantly inhibits lipopolysaccharide (LPS)-induced TNF-α expression and anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes.

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