CAS:2093393-05-4TC13172

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TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2±0.6 nM for HT-29 cells.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

2093393-05-4

储存条件

分子式

C17H16N4O5S

运输

蓝冰

分子量

388.40

别名

溶解度

DMSO	25.0 mg/mL (64.4 mM) warming
Water	Insoluble

动物实验配方

生物活性

描述Mixed lineage kinase domain-like protein (MLKL) is a necroptosis executor that mediates ion influx and causes cell structure disruption. TC13172 is a MLKL inhibitor that shows anti-necroptosis potency with an EC₅₀ value of 2  0.6 nM in TNF-a/Smac mimetic/Z-VAD-fmk-treated HT-29 cells. In HT-29 cells pre-incubated with 100 nM TC13172 for 2 hours and then treated with another MLKL inhibitor with a propyne group at the dose of 1 μM for additional 2 hours, TC13172 efficiently outcompeted the other inhibitor in binding to MLKL. Treatment of HT-29 cells with 100 nM TC13172 for 8 hours blocked the oligomerization and translocation of MLKL from the cytoplasm to the cell membrane but did not disrupt the phosphorylation of MLKL.
作用机制TC13172 potently inhibits MLKL by directly binding to Cys-86. The hydrogen bond formation between the 3-OH of TC13172 and an acceptor residue on MLKL may contribute to the high potency of TC13172 towards MLKL.