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CAS No.: 2244678-29-1

TH-257 Catalog No. CSN24750

Synonyms: TH 257

TH 257 is a potent inhibitor of both LIMK1 and 2 with IC50 values of 84 and 39nM, respectively.

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400-920-2911

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实验方案

技术信息

生物活性

描述LIM kinase (LIMK) 1 and 2 are cytoplasmic tyrosine-like kinases involved in various physiological processes related to viral infection, tumor progression and metastasis. TH 257 is a potent inhibitor of both LIMK1 and 2 with IC50 values of 84 and 39nM, respectively^[1]. In live cell NanoBRET assay, TH-257 exhibited an inhibitory effect against ectopically expressed full-length LIMK1 and 2 with IC50 values of 250 and 150nM, respectively. TH 257 showed no significant activity against the wider kinome that has been observed in the KINOMEscan assay at 1μM^[1].
作用机制TH 257 is a potent, allosteric inhibitor of LIMK1/2 and can be used as a chemical probe for these enzymes. It targets a binding pocket induced by an αC and DFG-out conformation^[1].
参考文献

[1] Manetti F. Recent advances in the rational design and development of LIM kinase inhibitors are not enough to enter clinical trials. Eur J Med Chem. 2018 Jul 15;155:445-458. doi: 10.1016/j.ejmech.2018.06.016. Epub 2018 Jun 8. PMID: 29908439.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3666 mL
- 11.8332 mL
- 23.6664 mL
- 5 mM
- 0.4733 mL
- 2.3666 mL
- 4.7333 mL
- 10 mM
- 0.2367 mL
- 1.1833 mL
- 2.3666 mL

技术信息

CAS号

2244678-29-1

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H26N2O3S

运输

蓝冰

分子量

422.54

别名

TH 257

溶解度

DMSO	135.0 mg/mL (319.5 mM)
Water	insoluble

动物实验配方

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TH-257 Catalog No. CSN24750

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