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TC13172 Sale

目录号 : GC34140

TC13172是MLKL的抑制剂,作用于HT-29细胞,其EC50值为2nM。

TC13172 Chemical Structure

Cas No.:2093393-05-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,436.00
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5mg
¥3,124.00
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10mg
¥4,909.00
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50mg
¥14,726.00
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100mg
¥23,651.00
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Sample solution is provided at 25 µL, 10mM.

Description

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

The anti-necroptosis potency of TC13172 is evaluated in the HT-29 cell line, the EC50 value is 2±0.6 nM. TC13172 has an inhibition potency of 2 nM against cell necroptosis. TC13172 inhibits MLKL by directly binding to Cys-86. TC13172 does not disrupt the phosphorylation of MLKL, but do decrease the level of MLKL in the membrane phase, demonstrating that these MLKL inhibitors block the translocation of MLKL to the cell membrane, thereby protecting cells from necroptosis[1].

[1]. Bo Yan, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein.ChemCommun (Camb). 2017 Mar 28;53(26):3637-3640.

实验参考方法

Cell experiment:

Human colorectal adenocarcinoma (HT)-29 cells are incubated with compound 12 (1 mM) or DMSO for 2 h. For the binding competition experiment samples, cells are pre-incubated with 5 mM NSA or 100 nM TC13172 for 2 h, 1 mM compound 12 is then added and incubated for an additional 2 h. The click reaction (Biotin-C2H4-N3 10 mM, TBTA 10 mM, CuSO4 50 mM, Sodium ascorbate 50 mM) is carried out with cell lysates for 2 h. The biotinmodified proteins are enriched and analysed by western blotting using antibodies against flag and GAPDH[1].

References:

[1]. Bo Yan, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein.ChemCommun (Camb). 2017 Mar 28;53(26):3637-3640.

化学性质

Cas No. 2093393-05-4 SDF
Canonical SMILES O=C1C2=C(N=C(S(C)(=O)=O)N2C)N(CC#CC3=CC(O)=CC=C3)C(N1C)=O
分子式 C17H16N4O5S 分子量 388.4
溶解度 DMSO : 25 mg/mL (64.37 mM);Water : < 0.1 mg/mL (insoluble) 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.5747 mL 12.8733 mL 25.7467 mL
5 mM 0.5149 mL 2.5747 mL 5.1493 mL
10 mM 0.2575 mL 1.2873 mL 2.5747 mL
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