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TH-257

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Chemical Structure| 2244678-29-1 同义名 : -
CAS号 : 2244678-29-1
货号 : A1193405
分子式 : C24H26N2O3S
纯度 : 98%
分子量 : 422.54
MDL号 : MFCD31697753
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 250 mg/mL(591.66 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 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.83mL

2.37mL

1.18mL

23.67mL

4.73mL

2.37mL

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.