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抑制剂描述:

产品名称:SB 203580

产品别名:见爱必信官网

英文别名:SB 203580

靶点:Mitophagy;p38 MAPK;Autophagy

CAS:152121-47-6

纯度:99%

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:

SB203580是一种p38 MAPK抑制剂,在THP-1细胞中IC50为0.3-0.5μM,对SAPK3(106T)和SAPK4(106T)选择性低10倍,且阻断PKB磷酸化,IC50为3-5μM。SB203580是第一个被报道的p38抑制剂。

溶解性:DMSO:43 mg/mL (113.92 mM)

体外研究:

SB203580 inhibits the IL-2-induced proliferation of primary human T cells, murine CT6 T cells, or BAF F7 B cells with an IC50 of 3–5 μm. SB203580 also inhibits IL-2-induced p70S6 kinase activation, although the concentration required is slightly higher with an IC50 above 10 μm. SB203580 also inhibits the activity of PDK1 in a dose-dependent manner with an IC50 in the 3–10 μm range. SB203580 inhibits p38-MAPK stimulation of MAPKAPK2 with an IC50 of approximately 0.07 μM, whereas inhibits total SAPK/JNK activity with an IC50 of 3–10 μM. SB203580 at higher concentrations activates the ERK pathway, which subsequently enhances NF-κB transcriptional activity. SB203580 induces autophagy in human hepatocellular carcinoma (HCC) cells.

体内研究:SB203580 protects pig myocardium against ischemic injury in an in vivo model. SB203580 is effective to prevent and treat the disease in MRL/lpr mice model of Systemic lupus erythematosus (SLE).

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