SB 203580；152121-47-6

產(chǎn)品描述：

SB203580是一種p38 MAPK抑制劑，在THP-1細(xì)胞中IC50為0.3-0.5μM，對(duì)SAPK3(106T)和SAPK4(106T)選擇性低10倍，且阻斷PKB磷酸化，IC50為3-5μM。SB203580是第一個(gè)被報(bào)道的p38抑制劑。

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.

別名：

Adezmapimod；RWJ 64809

外觀：

white to off-white powder

可溶性/溶解性：

DMSO：43 mg/mL (113.92 mM)

靶點(diǎn)：

p38 MAPK；PKB

In vitro(體外研究)：

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.

In vivo(體內(nèi)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).

分子結(jié)構(gòu)圖：