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Description: PD 151746 (PD-151746) is a novel, potent, selective, and cell-permeable calpain inhibitor with important biological activity. It inhibits calpain with a Ki of 0.26 uM for u-Calpain, and has about 20-fold higher selectivity for u-calpain (Ki = 0.26 +/- 0.03 uM) over m-calpain (Ki = 5.33 +/- 0.77 uM). PD151746 significantly inhibited NMDA-induced alpha-spectrin breakdown product (SBDP) of 145 kDa and completely inhibited the fragmentation of calmodulin-dependent protein kinase II-alpha (CaMPK-IIalpha) and nitric oxide synthase (nNOS), which were cleaved by calpain. The u-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity.
References: Proc Natl Acad Sci U S A. 1996 Jun 25; 93(13):6687-92; Biochem J. 2003 Sep 1; 374(Pt 2):403-11.
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