T 5601640 is a selective LIMK2 inhibitor which can inhibit cofilin phosphorylation in cells that overexpress LIMK2 but not LIMK1.
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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[3]. T5601640 is a selective inhibitor of LIMK2 and efficiently inhibits the growth of ST88-14, U87, Panc-1 cells, A549 lung cancer cells with IC50 values of 18.3, 7.4, 35.2 and 90 μM, respectively. T5601640 decreases phosphorylated cofilin (p-cofilin) levels and thus inhibits growth of several cancerous cell lines, including those of pancreatic cancer, glioma and schwannoma[3]. T5601640 (10-50 μM) reduces p-cofilin in a dose-dependent manner in NF1−/−MEFs with an IC50 of 30 μM. Notably, the inhibitor does not affect the amounts of total cofil. 50 μM T5601640 causes a statistically significant reduction in the number of cells exhibiting stress fibers[4]. T5601640 can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T5601640 (60 mg/kg) shows a significant decrease in tumor volume compared to control[3].
作用机制
T5601640, as a potential LIMK2 inhibitor, occupies both the ATP-binding and the substrate-binding sites.
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