Hymeglusin (29066-42-0) is an inhibitor of eukaryotic mevalonate biosynthesis via inhibition of HMG-CoA synthase, IC50=0.12 μM.1 Acts via covalent modification of the active site Cys129.1,2 Inhibits cholesterol biosynthesis in rats (45% at 25 mg/Kg).1 Also inhibits bacterial HMG-CoA synthase.3 Inhibits dengue virus replication.4
1) Greenspan et al. (1987), Inhibition of hydroxymethylglutaryl-coenzyme A synthase by L-659,699; Proc. Natl. Acad. Sci. USA, 84 7488
2) Tomoda et al. (2004), Binding site for fungal beta-lactone hymeglusin on cytosolic 3-hydroxy-3-methylglutaryl coenzyme A synthase; Biochem. Biophys. Acta, 1636 22
3) Skaff et al. (2012), Biochemical and structural basis for inhibition of Enterococcis faecalis hydroxymethylglutaryl-CoA synthase, mvaS, by hymeglusin; Biochemistry, 51 4713
4) Rothwell et al. (2009), Cholesterol biosynthesis modulation regulates dengue viral replication; Virology, 389 8
