MDI-114215

MDI-114215 is an allosteric inhibitor of LIM kinase 1 (LIMK1) and LIMK2 (IC50s = 19. and 26. nM, respectively). It is selective for LIMK1 and LIMK2 in a panel of 468 kinases but does bind to cyclin-dependent kinase 7 (Cdk7), MAP kinase kinase 7 (MKK7), vaccinia-related kinase 2 (VRK2), and phosphorylated Abl1 at 300 nM. MDI-114215 is also selective for LIMK1 and LIMK2 in a panel of 44 receptors, ion channels, transporters, and enzymes but does bind to cannabinoid 1 (CB1) receptor at 10 µM. It reduces the levels of cofilin phosphorylated by p21-activated kinase 1 (PAK1) in SH-SY5Y cells (IC50 = 50. nM). MDI-114215 (3 µM) enhances long-term potentiation (LTP) in hippocampal slices from Fmr1 knockout mice, which lack the gene encoding fragile X mental retardation 1 protein (FMRP).. Solulibility: DMSO: Soluble: = 10 mg/ml: Ethanol: Soluble: = 10 mg/ml.