LIM Kinase (LIMK)(LIM激酶)

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.

Products for LIM Kinase (LIMK)

Cat.No. 产品名称 Information
GC73353 TH470 TH470是一种高度选择性的LIMK1/2（LIM激酶1/2）抑制剂（LIMK1 IC50=9.8 nM；LIMK2 IC50=13 nM），可用于孤儿疾病研究。
GC71011 DB0614 DB0614（实施例21）是一种靶向激酶蛋白质降解的双功能化合物。
GC68913 Curcolonol Curcolonol 是一种呋喃型倍半萜。Curcolonol 可以从几种草药中分离出来。Curcolonol 对 LIM 激酶 1 具有抑制活性。Curcolonol 可用于乳腺癌的研究。
GC65207 R-10015 R-10015 is a potent, selective inhibitor of LIM domain kinase (LIMK) with IC50 of 38 nM for human LIMK1. R-10015 binds to the ATP-binding pocket and acts as a broad-spectrum antiviral compound for HIV infection.
GC62675 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 MKNK2、MAP2K1/2/3/4/6/7、GAK、AAK1、BMP2K、MAP3K7、MAPKAPK5、GSK3A/B、MAPK1/3、SRC、YES1、FGFR1、ZAK (MLTK)、MAP3K1、LIMK1 和 RSK2。SM1-71 在体外抑制多种癌细胞系的增殖。
GC50404 CRT 0105950 CRT 0105950 是一种有效的 LIMK 抑制剂，对 LIMK1 和 LIMK2 的 IC50 分别为 0.3 nM 和 1 nM。 CRT 0105950 可用于癌症研究。
GC50219 SR 7826 SR 7826 是一类双芳基脲衍生的强效、选择性和口服活性 LIM 激酶 (LIMK) 抑制剂，对 LIMK1 的 IC50 为 43 nM。
GC38860 TH-257 An inhibitor of LIMK1 and LIMK2
GC44094 LX7101 (hydrochloride) A LIMK and ROCK inhibitor
GC19076 BMS-3 An inhibitor of LIMK1 and LIMK2
GC16355 T 5601640
T5601640
An inhibitor of LIMK2
GC15511 LIMKi 3
LIMKi 3
An inhibitor of LIMK1 and LIMK2