TH-257

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TH-257

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2244678-29-1

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

TH-257 是一种有效的 LIMK1 和 LIMK2 抑制剂，对 LIMK1 和 LIMK2 的 IC50 值分别为 84 nM 和 39 nM，是 LIMK1 和 LIMK2 的化学探针。TH-257 是一种变构抑制剂，靶向由 αC 和 DFG-out 构象诱导的结合口袋。TH257 具有极好的选择性，在 1 μM 浓度下未观察到针对更广泛的激酶组的显着活性。

Cas No.	2244678-29-1
Canonical SMILES	O=C(N(CCCC)CC1=CC=CC=C1)C2=CC=C(S(=O)(NC3=CC=CC=C3)=O)C=C2
分子式	C₂₄H₂₆N₂O₃S
分子量	422.54
溶解度	DMSO: 250 mg/mL (591.66 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM[1]. [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.