SR12813

SR12813 (GW 485801) is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC₅₀ value of 0.85 μM^[1][2]. SR12813 is also an efficient agonist of human pregnane X receptor (hPXR). SR12813 can strongly bind to hPXR but not to mouse PXR (mPXR)^[3]. IC50 & Target: IC50: 0.85 μM (HMG-CoA Reductase) In Vitro: SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC₅₀ of 1.2 μM but has no effect on fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC₅₀ of 0.85 μM^[1]. Both 25-HC and SR-12813 can kill mammalian cells through blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection. SR-12813 kills HeLa cells at concentration range from 8 µM to 16 µM. SR-12813 kills wild type cells and mutant cells infected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotes the degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and SL-5 mutant cells^[1].