OSC Inhibitor, Ro 48-8071-CAS 189197-69-1-Calbiochem

C₂₃H₂₇BrFNO₂ · xC₄H₄O₄

448.37 (free base basis)

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).

Toxicity: Regulatory Review (Z)

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

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.

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

100

≥95% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

off-white

water: 5 mg/mL

ambient

2-8℃

1S/C23H27BrFNO2/c1-3-14-26(2)15-6-4-5-7-16-28-20-12-13-21(22(25)17-20)23(27)18-8-10-19(24)11-9-18/h3,8-13,17H,1,4-7,14-16H2,2H3

CMYCCJYVZIMDFU-UHFFFAOYSA-N

10 mg in Glass bottle

11 - Combustible Solids

WGK 3