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Cell Cycle/DNA Damage——LIM Kinase (LIMK)

LIM kinases (LIMKs) are important cell cytoskeleton regulators that play a prominent role in cancer manifestation and neuronal diseases. The LIMK family consists of two homologues, LIMK1 and LIMK2, which differ from one another in expression profile, intercellular localization, and function. The main substrate of LIMK is cofilin, a member of the actin-depolymerizing factor (ADF) protein family. When phosphorylated by LIMK, cofilin is inactive. LIMKs play a contributory role in several neurodevelopmental disorders and in cancer growth and metastasis.

LIM domain kinases (LIMK1 and 2) are substrate for Cdc42/Rac-PAK, and modulate actin dynamics by phosphorylating cofilin at serine-3. This modification inactivates cofilin’s actin severing and depolymerizing activity. LIMKs also translocate into the nucleus and regulate cell cycle progression. LIMKs are potential therapeutic targets for NF2 and other merlin-deficient tumors.

Cell Cycle/DNA Damage——LIM Kinase (LIMK)(7)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM17756 BMS-3

BMS-3 是一种高效的 LIMK 抑制剂,抑制 LIMK1LIMK2IC50 分别为 5 nM 和 6 nM。

1338247-30-5 98%
KM17768 BMS-5

BMS-5 (LIMKi 3) 是一种高效的 LIMK 抑制剂,抑制 LIMK1LIMK2IC50 分别为 7 nM 和 8 nM。

1338247-35-0 99%
KE9523 LIMK-IN-22j 1116571-01-7 ≥95%
KM6998 R-10015

R-10015 是一种用于 HIV 感染的广谱抗病毒化合物,是高效选择性的 LIMK 抑制剂,通过结合 ATP 结合口袋阻断 LIMK,抑制人 LIMK1 的 IC50 值为 38 nM。

2097938-51-5 99%
KM5185 SM1-71

SM1-71 是一种有效的 TAK1 抑制剂,Ki 值为 160 nM,同时可以共价抑制 MKNK2MAP2K1/2/3/4/6/7GAKAAK1BMP2KMAP3K7MAPKAPK5GSK3A/BMAPK1/3SRCYES1FGFR1ZAK (MLTK)MAP3K1LIMK1RSK2。SM1-71 在体外抑制多种癌细胞系的增殖。

2088179-99-9 96%
KM14437 T56-LIMKi

T56-LIMKi是选择性的LIMK2抑制剂。抑制Panc-1细胞生长的IC50值为35.2 μM。

924473-59-6 98%
KM4108 TH-257

TH-257 是一种有效的 LIMK1LIMK2 抑制剂,对 LIMK1LIMK2IC50 值分别为 84 nM 和 39 nM,是 LIMK1LIMK2 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。

2244678-29-1 98%
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