Synonym: Compactin, ML-236B
|Related Categories||Antibacterial, Antibiotics, Antibiotics A to Z, Antibiotics G-M, Approved Therapeutics/Drug Candidates,|
|solubility||DMSO: soluble20 mg/mL|
|ethanol: soluble25 mg/mL|
human ... HMGCL(3155), HMGCR(3156)|
rat ... Hmgcr(25675)
HMG-CoA reductase inhibitor. Cholesterol lowering drug. Inhibits myoblast formation. An antibiotic shown to cause apoptosis, apparently by inhibiting post-translational prenylation of proteins such as Ras. Similarly, mevastatin increases eNOS mRNA and protein levels by blocking the geranylgeranylation of Rho.
Bottomless glass bottle. Contents are inside inserted fused cone.
Certificate of Analysis
Certificate of Origin
Download BioFiles v7 n5 (3.18 Mb PDF) Back to Pharmaceutical Drugs and Drug Candidates homepage
BioFiles v7 n5, 2012, 21–24
Keywords: Anti-inflammatory agents, Cardiovascular, Chemical vapor deposition, Clinical, Diabetes, Inflammation, Oxidations, Pharmaceutical, Transcription
The amount of cholesterol that is synthesized in the liver is tightly regulated by dietary cholesterol levels. When dietary intake of cholesterol is high, synthesis is decreased and when dietary inta...
BioFiles 2007, 2.7, 6.
Keywords: Gene expression, Transcription
Terpenes comprise the largest and most diverse class of secondary metabolites; approximately 55,000 compounds have been identified to date.1 While the enzymes responsible for terpene synthesis are fo...
BioFiles 2008, 3.9, 4.
Keywords: Anti-inflammatory agents, Antimicrobials, Antiparasitics, Apoptosis, Building blocks, Cancer, Carcinogens, Cell division, Condensations, Detergents, Gene expression, Hormones, Insecticides, Isomerizations, Metabolites, Neurotransmitters, Poisons, Pollination, Reproduction, Vitamins
Induction of 3-hydroxy-3-methylglutaryl coenzyme A reductase activity in human fibroblasts incubated with compactin (ML-236B), a competitive inhibitor of the reductase. Brown, M.S., et al. J. Biol. Chem. 253, 1121, (1978)
Novel synthetic inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity that inhibit tumor cell proliferation and are structurally unrelated to existing statins. JEAN-PIERRE H. PERCHELLET et al Int. J. Mol. Med. 24, 633-43, (2010)
Complete mitochondrial genome of compactin-producing fungus Penicillium solitum and comparative analysis of Trichocomaceae mitochondrial genomes. Eldarov MA, Mardanov AV, Beletsky AV, et al. FEMS Microbiol. Lett. 329(1), 9-17, (2012)
Construction of a novel expression vector in Pseudonocardia autotrophica and its application to efficient biotransformation of compactin to pravastatin, a specific HMG-CoA reductase inhibitor. Fujii Y, Norihisa K, Fujii T, et al. Biochem. Biophys. Res. Commun. 404(1), 511-6, (2011)
IL-2 costimulation enables statin-mediated activation of human NK cells, preferentially through a mechanism involving CD56+ dendritic cells. Gruenbacher G, Gander H, Nussbaumer O, et al. Cancer Res. 70(23), 9611-20, (2010)
Lipophilic statins prevent matrix metalloproteinase-mediated cartilage collagen breakdown by inhibiting protein geranylgeranylation. Barter MJ, Hui W, Lakey RL, et al. Ann. Rheum. Dis. 69(12), 2189-98, (2010)
A role for the mevalonate pathway in the induction of subtype cross-reactive immunity to influenza A virus by human gammadelta T lymphocytes. Jameson JM, Cruz J, Costanzo A, et al. Cell. Immunol. 264(1), 71-7, (2010)
A novel statin-mediated "prenylation block-and-release" assay provides insight into the membrane targeting mechanisms of small GTPases. Ali BR, Nouvel I, Leung KF, et al. Biochem. Biophys. Res. Commun. 397(1), 34-41, (2010)
The transcription factor KLF2 mediates hepatic endothelial protection and paracrine endothelial-stellate cell deactivation induced by statins. Marrone G, Russo L, Rosado E, et al. J. Hepatol. 58(1), 98-103, (2013)
The association of statins plus LDL receptor-targeted liposome-encapsulated doxorubicin increases in vitro drug delivery across blood-brain barrier cells. Pinzón-Daza M, Garzón R, Couraud P, et al. Br. J. Pharmacol. 167(7), 1431-47, (2012)
Efficient bioconversion of compactin to pravastatin by the quinoline-degrading microorganism Pseudonocardia carboxydivorans isolated from petroleum-contaminated soil. Lin CL, Tang YL, and Lin SM Bioresour. Technol. 102(22), 10187-93, (2011)
Three-dimensional quantitative structure (3-D QSAR) activity relationship studies on imidazolyl and N-pyrrolyl heptenoates as 3-hydroxy-3-methylglutaryl-CoA reductase (HMGR) inhibitors by comparative molecular similarity indices analysis (CoMSIA). Ramasamy Thilagavathi et al Bioorg. Med. Chem. Lett. 15, 1027-32, (2005)
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