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TC13172 {[allProObj[0].p_purity_real_show]}

货号:A157358

TC13172是一种混合谱系激酶样蛋白 (MLKL) 抑制剂,对 HT-29 细胞的 EC50 值为 2±0.6 nM。

TC13172 化学结构 CAS号:2093393-05-4
TC13172 化学结构
CAS号:2093393-05-4
TC13172 3D分子结构
CAS号:2093393-05-4
TC13172 化学结构 CAS号:2093393-05-4
TC13172 3D分子结构 CAS号:2093393-05-4
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TC13172 纯度/质量文件 产品仅供科研

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TC13172 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.

TC13172 细胞实验

Cell Line
Concentration Treated Time Description References
Yeast cells 20 µM 24 hours TC13172 significantly restored the growth rate of yeast cells expressing RIPK1, RIPK3VQVG/AAAA, and MLKL, demonstrating its efficacy as an MLKL inhibitor. Biomolecules. 2021 Jan 25;11(2):153

TC13172 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.

TC13172 实验方案

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

TC13172 技术信息

CAS号2093393-05-4
分子式C17H16N4O5S
分子量 388.4
SMILES Code O=C(N1C)N(CC#CC2=CC=CC(O)=C2)C3=C(N(C)C(S(=O)(C)=O)=N3)C1=O
MDL No. N/A
别名
运输蓝冰
InChI Key ZTQLCNOQWGSELY-UHFFFAOYSA-N
Pubchem ID 134691750
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

请根据您的动物给药指南选择适当的溶解方案。
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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