MG OSC Inhibitor; Ro 48-8071 1PC X 10MG

General description

An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC; IC₅₀ ~6.5 nM against mammalian) and reduces cholesterol synthesis (IC₅₀ ~1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC₅₀ ~10 µM).

An orally bioavailable benzofuranylallylamine compound that acts as a potent, active site targeting, competitive and reversible inhibitor of 2,3-oxidosqualene:lanosterol cyclase activity (OSC; IC₅₀ ~ 6.5 nM against mammalian) and reduces cholesterol synthesis (IC₅₀ ~ 1.5 nM in HepG2 cells) with minimal buildup of both dioxidosqualene and monooxidosqualene. Downregulates 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase mRNA and synthesis, and exerts less adverse effects in animal models than Statins. Shown to preferentially enhance the DNA-binding affinity of mutant p53 and arrest the growth of human breast cancer cells (IC₅₀ ~ 10 µM).

Legal Information

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

Other Notes

Thoma, R., et al. 2004. Nature432, 118.Peffley, D.M., et al. 1998. Biochem. Pharmacol.56, 439.Morand, O.H., et al. 1997. J. Lipid Res.38, 373.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Regulatory Review (Z)