Mevinolin MK-803 White to off-white powder. PROTECT FROM LIGHT. An anti-hypercholesterolemic agent that inhibits the activity of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. Has been shown to block a series of biological events including: the activation of p21ras by insulin in 3T3-L1 fibroblasts and 3T3-L1 adipocytes; the farnesylation of p21ras, which decreases the pool of intracellular Ras available for subsequent activation by growth factors (including insulin); and N-ras-induced neuronal differentiation. Causes cell cycle arrest in the late G1 phase through inhibition of proteasome. Has recently been shown to inhibit the stimulation of MAP kinase by insulin in HIRcB cells and to block the transcription of type-I SCR gene in THP-1-derived macrophages. Also blocks PDGF receptor tyrosine phosphorylation and MAP kinase activation by PDGF. This product requires activation for use in cell synchronization studies and in cell-free assay systems for HMG-CoA studies. Purity: ≥95% by HPLC. RTECS EK7907000, CAS 75330-75-5. Merck Index: 14, 5586 Ref.: Rao, S., et al. 1999. Proc. Natl. Acad. Sci. USA 96, 7197. Carel, K., et al. 1996. J. Biol. Chem. 271, 30625. McGuire, T.F., et al. 1996. J. Biol. Chem. 271, 27402. Umetani, N., et al. 1996. Biochim. Biophys. Acta 1303, 199. Xu, X.Q., et al. 1996. Arch. Biochem. Biophys. 326, 233. Reusch, J.E.-B., et al. 1995. J. Biol. Chem. 270, 2036. Jakobisiak, M., et al. 1991. Proc. Natl. Acad. Sci. USA 88, 3628. Keyomarsi, K., et al. 1991. Cancer Res. 51, 3602. Mendola, C.E., and Backer, J.M. 1990. Cell Growth Differ. 1, 499. R: 63; S: 22-24/25 |