T56-LIMKi (T5601640) is a selective inhibitor of LIMK2.

T56-LIMKi effectively suppresses the proliferation of various cancer cell lines, including ST88-14, U87, Panc-1, and A549 lung cancer cells, exhibiting IC50 values of 18.3, 7.4, 35.2, and 90 µM respectively. It significantly lowers phosphorylated cofilin (p-cofilin) levels, impairing the growth of pancreatic, glioma, and schwannoma cancer cells. This compound inhibits cofilin phosphorylation, crucial for actin disruption, thereby preventing tumor cell movement, proliferation, and the formation of colonies in soft agar without contact. At concentrations ranging from 10-50 µM, T56-LIMKi dose-dependently decreases p-cofilin in NF1−/− MEFs, with a 30 µM IC50, while not affecting total cofilin levels. Furthermore, a 50 µM dosage of T56-LIMKi significantly reduces the presence of stress fibers in cells.

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) display a significant decrease in tumor volume than controls[1].

T56-LIMKi can induce inhibition of cofilin phosphorylation and Panc-1 tumor shrinkage in vivo. Mice treated with T56-LIMKi (60 mg/kg) shows a significant decrease in tumor volume compared to control[1].