PD150606

PD 150606 is a selective, cell-permeable non-peptide calpain inhibitor (Ki values for ν and m-calpains are 0.21 and 0.37 μM respectively).target:calpain[1]In vitro: PD150606 also against tetrafluoroethyl-l-cysteine-, bromohydroquinone-, oxidant (t-butylhydroperoxide)- and calcium ionophore (ionomycin)-induced cell death. PD150606 inhibits calpains by binding to the calcium-binding domain of the enzyme. [2] high specificity for calpains relative to other proteases, uncompetitive inhibition with respect to substrate.[3]

Signaling Pathways >> Metabolic Enzyme/Protease >> Proteasome

Research Areas >> Cancer

[1]. Squier MK et al. Calpain and calpastatin regulate neutrophil apoptosis. J Cell Physiol. 1999 Mar;178(3):311-9.

[2]. Waters SL et al. Calpains mediate calcium and chloride influx during the late phase of cell injury. J Pharmacol Exp Ther. 1997 Dec;283(3):1177-84.

[3]. Wang KK et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6687-92.

MG-132 | Celastrol | ONX-0914 (PR-957) | Pepstatin | Epoxomicin | Ixazomib (MLN2238) | Calpain Inhibitor I | Oprozomib (ONX 0912) | CEP-18770 (Delanzomib) | RA190 | Capzimin | Gabexate mesylate | PI 1840 | VR23 | PD 151746