BMS-5

BMS-5 is a potent inhibitor of the LIM kinase. It has IC₅₀ values of 7nM and 8 nM for LIMK1 and LIMK2 respectively. LIMK1/2 activity was measured via TCA precipitation assay using a biotinylated ADF (actin depolymization factor) as the protein substrate and the kinase domains of LlMKl and LIMK2 as the enzyme sources in the presence of 1 μM ATP.

Kinases, such as LIM kinase 1 (LMK1) and LIM kinase 2 (LMK2), have been identified as participating in signal pathways affecting actin dynamics by deactivating cofilin. Over expression of LIMKl has been found in invasive breast and prostate cancer cell lines and suppression of LIMK 2 expression has been found to limit migration of human fibrosarcoma cells. Thus, the inhibition of LIMKl and/or LIMK2 enzymes have been suggested as targets for treating cancer, including reduction or prevention of metastasis.