Biochem/physiol Actions

Reversible: yes

Primary TargetHMG-CoA reductase

Cell permeable: yes

General description

Carboxylate form of Lovastatin (Cat. No. 438185) that is active in whole cells and cell-free assays. Lovastatin is reported to be an anti-hypercholesterolemic agent that acts as a reversible competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and blocks a series of biological events including activation of p21^ras by insulin in 3T3-L1 fibroblasts and 3T3-L1 adipocytes, farnesylation of p21^ras, 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. Shown to inhibit the stimulation of MAP kinase by insulin in HIRcB cells and block the transcription of the type-I SCR gene in THP-1-derived macrophages. Also blocks PDGF receptor tyrosine phosphorylation and MAP kinase activation by PDGF.

Carboxylate form of Lovastatin (Cat. No. 438185) that is active in whole cells and cell-free assays. Lovastatin is reported to be an anti-hypercholesterolemic agent that acts as a reversible competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase and blocks a series of biological events including activation of p21^ras by insulin in 3T3-L1 fibroblasts and 3T3-L1 adipocytes, farnesylation of p21^ras, 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. Shown to inhibit the stimulation of MAP kinase by insulin in HIRcB cells and block the transcription of the type-I SCR gene in THP-1-derived macrophages. Also blocks PDGF receptor tyrosine phosphorylation and MAP kinase activation by PDGF.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Rao, S., et al. 1999. Proc. Natl. Acad. Sci. USA96, 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. Acta1303, 199.Xu, X.Q., et al. 1996. Arch. Biochem. Biophys.326, 233.Reusch, J.E.-B., et al. 1995. J. Biol. Chem.270, 2036.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 10 mM (5 mg/1.13 ml) solution of Lovastatin, Sodium Salt (Cat. No. 438186) in H₂O.

Reconstitution

Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.

Warning

Toxicity: Harmful (C)