PD 151746

PD 151746 is an inhibitor of calpain 1/µ-calpain (Ki = 0.26 µM). It is 20-fold selective for calpain 1 over calpain 2/m-calpain (Ki = 5.33 µM). It is also selective over cathepsin B, papain, trypsin, and thermolysin, (Kis = >200, >500, >500, and >500 µM, respectively) and does not inhibit basal calcineurin activity (Ki = >200 µM) but does inhibit calmodulin-induced calcineurin activity (Ki = 84.54 µM). It reduces glycogen synthesis induced by insulin in HepG2 cells when used at a concentration of 5.33 µM. PD 151746 (10 µM) also increases intracellular calcium in isolated human neutrophils and HEK293 cells expressing human formyl peptide receptor-like 1 (hFPRL1).Formal Name: 3-(5-fluoro-1H-indol-3-yl)-2-mercapto-2-propenoic acid. CAS Number: 179461-52-0. Molecular Formula: C11H8FNO2S. Formula Weight: 237.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 30 mg/ml, Methanol: 5 mg/ml. lambdamax: 226, 280, 338 nm. SMILES: FC1=CC=C2C(C(/C=C(C(O)=O)\S)=CN2)=C1. InChi Code: InChI=1S/C11H8FNO2S/c12-7-1-2-9-8(4-7)6(5-13-9)3-10(16)11(14)15/h1-5,13,16H,(H,14,15)/b10-3-. InChi Key: HWMQHECFXSVZGN-KMKOMSMNSA-N.