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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[2]. |
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. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.87mL 2.57mL 1.29mL |
25.75mL 5.15mL 2.57mL |
CAS号 | 2093393-05-4 |
分子式 | C17H16N4O5S |
分子量 | 388.398 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,2-8°C |
溶解方案 |
DMSO: 25 mg/mL(64.37 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |