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Description: Ruboxistaurin hydrochloride (LY333531) is a novel, potent and specific inhibitor of PKCbeta (protein kinase C). It competitively and reversibly inhibits PKCbeta1 and PKCbeta2 with IC50 values of 4.7 and 5.9 nM respectively. It has the usefulness to treat diabetic nephropathy and diabetic macular edem. LY333531 strikingly decreases the chance of HUVEC survival and the effect of LY333531 on apoptotic cell death in HUVEC significantly increases compared with the AGEs group. Blockade of PKC-beta up-regulates the expression of Bax and Bad proteins and down-regulates the expression of Bcl-2 protein. Moreover, LY333531 reduces the ratio of Bcl-2/Bax.
References: J Med Chem. 1996 Jul 5; 39(14):2664-71; Diabetes. 2013 Jul; 62(7):2318-28; Pharmazie. 2011 Nov; 66(11):881-7.
Related CAS#: 169939-94-0 (free base); 202260-21-7 (mesylate hydrate); 192050-59-2 (mesylate) 169939-93-9 (HCl)
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