Lovastatin
Chemical Name: (2S)-(1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl-2-methyl butanoate
Purity: ≥97%
Biological Activity
Lovastatin is a potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM) therefore decreases cholesterol biosynthesis, in vitro and in vivo. Indirectly inhibits Rho-GTPase activity by depleting intracellular pool of isoprene residues. Decreases CDK2, 4, 6 and cyclin E levels and induces G1 arrest and apoptosis in tumor cell lines in vitro. Inactive lactam prodrug of lovastatin hydroxy acid, naturally bioactivated in vivo following oral administration.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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SCAP/SREBP pathway is required for the full steroidogenic response to cyclic AMP
Proc Natl Acad Sci USA, 2016;113(38):E5685-E5693. -
Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent.
Alberts et al.
Proc.Natl.Acad.Sci.U.S.A., 1980;77:3957 -
Lovastatin-induced inhibition of HL-60 cell proliferation via cell cycle arrest and apoptosis.
Park et al.
Anticancer Res., 1999;19:3133 -
Rho inhibition by lovas. affects apoptosis and DSB repair of primary human lung cells in vitro and lung tissue in vivo following fractionated irradiation.
Ziegler et al.
Cell Death Dis., 2017;8:e2978 -
Discovery, biochemistry and biology of lovas.
Alberts
Am.J.Cardiol., 1988;62:10J
Product Datasheets
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Citations for Lovastatin
The citations listed below are publications that use Tocris products. Selected citations for Lovastatin include:
11 Citations: Showing 1 - 10
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Trafficking of cholesterol to the ER is required for NLRP3 inflammasome activation.
Authors: Roche Et al.
J Cell Biol 2018;217:3560
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Mapping the Genetic Landscape of Human Cells.
Authors: Horlbeck Et al.
Cell 2018;174:953
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Expansion of DUB functionality generated by alternative isoforms - USP35, a case study.
Authors: Leznicki Et al.
J Cell Sci 2018;131
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Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS.
Authors: Park Et al.
Nat Immunol 2016;17:914
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Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle.
Authors: Saqcena Et al.
Oncotarget 2015;14:2285
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The Effects of Targeted Deliveries of lovas. and Tocotrienol on Ossification-Related Gene Expressions in Fracture Healing in an Osteoporosis Rat Model.
Authors: Ibrahim Et al.
Int J Environ Res Public Health 2015;12:12958
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Chemical and genetic validation of the statin drug target to treat the helminth disease, schistosomiasis.
Authors: Rojo-Arreola Et al.
PLoS One 2014;9:e87594
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Combination of 13-Cis retinoic acid and lovastatin: marked antitumor potential in vivo in a pheochromocytoma allograft model in female athymic nude mice.
Authors: Nölting Et al.
Endocrinology 2014;155:2377
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A suppressor screen in Mecp2 mutant mice implicates cholesterol metabolism in Rett syndrome.
Authors: Buchovecky Et al.
Nat Genet 2013;45:1013
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Selective induction of apoptosis by HMG-CoA reductase inhibitors in hepatoma cells and dependence on p53 expression.
Authors: Kah Et al.
Oncol Rep 2012;28:1077
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Phospholipase PLA2G7, associated with aggressive prostate cancer, promotes prostate cancer cell migration and invasion and is inhibited by STAT.
Authors: Vainio Et al.
J Neurosci 2011;2:1176
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