MDI-117740 is a dual LIMK1/2 inhibitor. MDI-117740 shows effective cellular target engagement with LIMK1 (pIC50 = 6.73) and LIMK2 (pIC50 = 7.18) in HEK293 cells. MDI-117740 exerts significant anti-migratory activity in MDA-MB-231 cells. MDI-117740 can be used for the study of diseases associated with LIMK dysregulation, such as cancers and neurodegenerative disorders.

SM311 (Compound 10), a chemical probe, is a potent selective irreversible LIMK1 inhibitor (EC50=0.045 μM, >30-fold selective over LIMK2). SM311 blocks cofilin phosphorylation and actin cytoskeleton regulation. SM311 is promising for research of neurodegenerative diseases like Fragile X syndrome (FXS) and Alzheimer’s disease, as well as tumor invasion.

MDI-114215 (compound 85) is an allosteric LIMK1/2 dual inhibitor with good in vivo tolerance. MDI-114215 can inhibit cofilin phosphorylation in mouse brain region-induced pluripotent stem cells (iPSCs), which can be used for Fragile X Syndrome (FXS) research.

LIJTF500025 is a potent and selective LIMK inhibitor, with pIC50 values of 6.77 and 7.03 for LIMK1 and LIMK2, respectively, as determined by NanoBRET. LIJTF500025 can be used for the research of cancer.

T56-LIMKi is a LIMK2 inhibitor that reduces phosphorylated cofilin, and induces disassembly of actin stress fibers in NF1-/- MEFs cells.

BMS-5 is a potent inhibitor of the LIM kinase. It has IC50 values of 7nM and 8 nM for LIMK1 and LIMK2 respectively.

BMS-3 is a potent inhibitor of the LIM kinase. It has IC50's of 5nM and 6 nM for LIMK1 and LIMK2 respectively.

TH470 is a highly selective LIMK1/2 (LIM kinase1/2) inhibitor (LIMK1 IC50=9.8 nM; LIMK2 IC50=13 nM), and can be used in orphan disease research.

A potent, selective inhibitor of human LIMK1 with IC50 of 38 nM .