Mevastatin (Compactin) inhibits HMGCR (HMG-CoA reductase) (Ki for acid form is 1 nM) which in turn inhibits isoprenoid biosynthesis and therefore blocks protein isoprenylation and reduces plasma cholesterol levels in humans. Mevastatin causes cells to arrest early in the G1 phase. Mevastatin is a close structural analog of lovastatin (sc-200850) and both agents have the same biochemical and pharmacological activities. Mevastatin is inactive in cell-free assays. In cells however, it is hydrolyzed to the active free acid form by intracellular esterases.
1. Quesney-Huneeus, V., et al. 1979. Proc. Natl. Acad. Sci. U.S.A. 76: 5056-5060. PMID: 291922 2. Quesney-Huneeus, V., et al. 1983. J. Biol. Chem. 258: 378-385. PMID: 6848509 3. Evangelopoulos, M.E., et al. 2009. J. Neurosci. Res. 87: 2138-2144. PMID: 19224573 4. Sugazaki, M., et al. 2010. Connect. Tissue Res. 51: 105-112. PMID: 20109072
Soluble in water (Partly miscible), acetone, DMSO (20 mg/ml), 100% ethanol (25 mg/ml), 1:1 ethanol:PBS(pH7.2) (0.5 mg/ml), and DMF (~5 mg/ml).
Rated 5 out of
Vukelic et alVukelic et al. (PubMed ID 19903814) found that Mevastatin (Compactin) decreased the amount of farnesyl pyrophosphate (FPP) available to bind with glucocorticoid receptor (GR) and reversed zaragozic acid A-mediated inhibitory effects, promoting epithelialization and would healing. -SCBT Publication Review
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