Catalog No.S2061 Synonyms: MK-803
Molecular Weight(MW): 404.54
Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent).
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To evaluate the role of cell cycle progression in androgen induced DSB formation, LAPC4 cells were either treated with solvent control or 50 μM lovastatin for 36 h prior to stimulation with 100 nM DHT for 6 h. Note that androgen induced γH2A.X foci formation was not different between control and lovastatin pre-treated cells.
Clin Cancer Res, 2016. doi:10.1158/1078-0432.CCR-15-1147.. Lovastatin purchased from Selleck.
Purity & Quality Control
Choose Selective HMG-CoA Reductase Inhibitors
|Description||Lovastatin is an inhibitor of HMG-CoA reductase with IC50 of 3.4 nM in a cell-free assay, used for lowering cholesterol (hypolipidemic agent).|
Lovastatin inhibits LPS- and cytokine-mediated production of NO and expression of iNOS in rat primary astrocytes. Lovastatin inhibits LPS-induced expression of TNF-alpha, IL-1beta, and IL-6 in rat primary astrocytes, microglia, and macrophages.  Lovastatin results in over 95% inhibition of DNA synthesis as measured by incorporation of [3H]thymidine into DNA. Lovastatin synchronizes cells in the G1 and not in the G0 phase of the cell cycle. Lovastatin has a similar growth-inhibitory activity against ras-dependent as well as ras-independent cell lines.  Lovastatin produces a profound reduction of apolipoprotein-B-containing lipoproteins, especially LDL cholesterol and, to a lesser extent, plasma triglyc- erides, and a small increase in HDL cholesterol.  Lovastatin arrests cells by inhibiting the proteasome, which results in the accumulation of p21 and p27, leading to G1 arrest. Lovastatin is an inhibitor of hydroxymethyl glutaryl (HMG)-CoA reductase, the rate-limiting enzyme in cholesterol synthesis. Lovastatin can be used to arrest cultured cells in the G1 phase of the cell cycle, resulting in the stabilization of the cyclin-dependent kinase inhibitors (CKIs) p21 and p27.  Lovastatin (2-10 mM) arrests cells in G1 and also prolonged--or arrested a minor fraction of cells in--the G2 phase of the cell cycle in human bladder carcinoma T24 cell line expressing activated p21ras. Lovastatin (50 mM) is cytotoxic in human bladder carcinoma T24 cell line expressing activated p21ras. 
-  Pahan K, et al. J Clin Invest, 1997, 100(11), 2671-2679.
-  Keyomarsi K, et al. Cancer Res, 1991, 51(13), 3602-3609.
-  Tobert JA, et al. Nat Rev Drug Discov, 2003, 2(7), 517-526.
|In vitro||DMSO||8 mg/mL (19.77 mM)|
|Ethanol||6 mg/mL (14.83 mM)|
|In vivo||Add solvents individually and in order:
30% PEG400+0.5% Tween80+5% propylene glycol
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02964884||Not yet recruiting||Neurofibromatosis Type 1|Learning Disability||Vanderbilt University|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)||November 2016||Phase 2|
|NCT02680379||Recruiting||Fragile X Syndrome||Université de Sherbrooke|FRAXA Research Foundation||March 2016||Phase 2|
|NCT02642653||Recruiting||Fragile X Syndrome|Genetic Diseases||Randi J. Hagerman, MD|University of California, Davis||January 2016||Phase 4|
|NCT02998151||Enrolling by invitation||Fragile X Syndrome||Childrens Hospital Medical Center, Cincinnati|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)||January 2016||Phase 2|
|NCT02603770||Completed||Lipid Metabolism Disorder||Luye Pharma Group Ltd.||November 2015||Phase 1|
|NCT02563860||Completed||Rett Syndrome||Montefiore Medical Center|Rett Syndrome Research Trust||July 2015||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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