Given the pivotal role of LIMKs in disease and their therapeuticpotential, there has been a growing number of reported LIMK inhibitors., The most characterized inhibitor is LIMKi3 (1, BMS-5, Figure ), a highly potent,type I dual LIMK1/2 inhibitor originally developed by Bristol-MyersSquibb.1 inhibits cellproliferation and motility in several cancer cell lines,,, reverses abnormal dendritic spinemorphology and normalizes anxiety-related behavior in the Fmr1 KO mouse model., Nevertheless, it haspromiscuous kinome selectivity and hasnot been progressed further. This evidence concerns the gene LIMK1 and cancer.