PD 151746

PD 151746 is an inhibitor of calpain 1/μ-calpain (K_i = 0.26 µM).¹ It is 20-fold selective for calpain 1 over calpain 2/m-calpain (K_i = 5.33 µM). It is also selective over cathepsin B, papain, trypsin, and thermolysin, (K_is = >200, >500, >500, and >500 µM, respectively) and does not inhibit basal calcineurin activity (K_i = >200 µM) but does inhibit calmodulin-induced calcineurin activity (K_i = 84.54 µM). It reduces glycogen synthesis induced by insulin in HepG2 cells when used at a concentration of 5.33 µM.² PD 151746 (10 µM) also increases intracellular calcium in isolated human neutrophils and HEK293 cells expressing human formyl peptide receptor-like 1 (hFPRL1).³

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1. Wang, K.K.W., Nath, R., Posner, A., et al. An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective. Proc. Natl. Acad. Sci. USA 93, 6687-6692 (1996).

2. Meier, M., Klein, H.H., Kramer, J., et al. Calpain inhibition impairs glycogen syntheses in HepG2 hepatoma cells without altering insulin signaling. J. Endocrinol. 193(1), 45-51 (2007).

3. Fujita, H., Kato, T., Watanabe, N., et al. Calpain inhibitors stimulate phagocyte functions via activation of human formyl peptide receptors. Arch. Biochem. Biophys. 513(1), 51-60 (2011).