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TC13172

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Chemical Structure| 2093393-05-4 同义名 : -
CAS号 : 2093393-05-4
货号 : A157358
分子式 : C17H16N4O5S
纯度 : 98%+
分子量 : 388.398
MDL号 : N/A
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

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
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[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.
实验方案
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
参考文献

[1]Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein.

[2]Yan B, Liu L, Huang S, Ren Y, Wang H, Yao Z, Li L, Chen S, Wang X, Zhang Z. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein. Chem Commun (Camb). 2017 Mar 28;53(26):3637-3640. doi: 10.1039/c7cc00667e. PMID: 28267172.