產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 10mg 50mg 100mg
CAS	129-56-6
別名	N/A
化學(xué)名	dibenzo[cd,g]indazol-6(2H)-one
分子式	C14H8N2O
分子量	220.23
溶解度	≥ 11mg/mL in DMSO, ≥ 2.56 mg/mL in EtOH with gentle warming
儲(chǔ)存條件	Desiccate at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

SP600125 is a selective, reversible and ATP-competitive inhibitor of Jun N-terminal kinase (JNK) with IC50 values of 40, 40 and 90 nM for JNK1, 2 and 3, respectively [1].

SP600125 was screened out from a time-resolved f luorescence assay using the GST-c-Jun and recombinant human JNK2. In this assay, SP600125 showed a Ki value of 190 nM. SP600125 was also found to inhibit JNK1, 2 and 3 isoforms in the selectivity tests. The selectivity of SP600125 for JNK is 300-fold greater than that for ERK1 and p38-2. In Jurkat T cells, SP600125 suppressed the phosphorylation of c-Jun with IC50 of 5-10 μM. SP600125 also inhibited the expression of IL-2 and IFN-γ in cells stimulated with PMA and phytohemagglutinin, since JNK had been reported to regulate the transcription of IL-2. Besides that, SP600125 exerted differential inhibition of cytokines in CD4+ cells as well as inflammatory genes in monocytes. Moreover, SP600125 administration significantly inhibited TNF-α expression induced by LPS in a mouse model, suggesting that it had efficacy in endotoxin-induced inf lammation in vivo [1].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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