Lovastatin (MK-803)

Catalog No.S2061 Synonyms: Mevinolin,Mevacor

For research use only.

Lovastatin (MK-803, Mevinolin,Mevacor) 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 triggers autophagy.

Lovastatin (MK-803) Chemical Structure

CAS No. 75330-75-5

Selleck's Lovastatin (MK-803) has been cited by 36 publications

Purity & Quality Control

Choose Selective HMG-CoA Reductase Inhibitors

Biological Activity

Description Lovastatin (MK-803, Mevinolin,Mevacor) 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 triggers autophagy.
Targets
HMG-CoA reductase [1]
(Cell-free assay)
3.4 nM
In vitro

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. [1] 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. [2] 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. [3] 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. [4] 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. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HES 9 cell line NYPrTW0xTnWwY4Tpc44h[XO|YYm= Mo\KR49v[2WwdILheIlwdiC{ZYH1bZJm\CC2bzDpcohq[mm2IFjNS{1Ed0FicnXkeYN1[XOnIHL5JFUxLSC5YYOg[IV1\XKvaX7l[EBqdiCKRWOgPUBk\WyuIHzpcoUtKEmFNUC9NE4xOTNizszN MkDuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTV{N{e5NUc,OTV{N{e5NVww[T5?
HEP G2 M3XSXGZ2dmO2aX;uJIF{e2G7 M2PMPGlvcGmkaYTpc44hd2ZidHjlJIlv[2:{cH;yZZRqd25ib3[gd49lcXWvIGuxOGNe[WOndHH0[UBqdnSxIHPoc4xme3Sncn;sJIlvKEiHUDDHNkBk\Wyucz6sJGlEPTB;MD6wOe69VS5? MkXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ3NkC0NUc,OTZ3NkC0NVww[T5?
HEP G2 M2ri[mZ2dmO2aX;uJIF{e2G7 NVPTcY9kUW6qaXLpeIlwdiCxZjDj[YxtfWyjcjDIUWcuS2:DIILl[JVkfGG|ZTDpckBkfWy2dYLld{Bw\iCqZYDheIlkKGOnbHzzJEhJTVBiR{KsJIEhcHWvYX6gbIVx[XSxbXGgZ4VtdCCuaX7lLUwhUUN3ME2wMlAxODB3zszNMi=> M1m4elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUOyNVMoRjJzNUOyNVM9N2F-
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Rh18 MXTxTHRUKGG|c3H5 Mn\3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NXHpZVd3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M{DVeJFJXFNiYYPzZZk> M4\tfZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NFPqPYs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
MG 63 (6-TG R) M4O4fJFJXFNiYYPzZZk> MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? MnXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RPMI8226 MmHNSpVv[3Srb36gZZN{[Xl? NHzwfVMxNjVidV2= NHLVNnE1QCCqcoO= MYjJcohq[mm2aX;uJI9nKE[WYYPlJIlvKGi3bXHuJHJRVUl6MkK2JINmdGy|IHHzd4V{e2WmIHHzJIRqe3K3cITpc44hd2ZiSD3yZZMh\mG{bnXzfYxifGmxbjDheEAxNjVidV2gZYZ1\XJiNEigbJJ{KGK7IHntcZVvd2Kub4SgZY5idHm|aYO= NX3rNJM4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{G2PVk3ODZpPkOxOlk6PjB4PD;hQi=>
RPMI8226 NELVd|FHfW6ldHnvckBie3OjeR?= NH\rcVMxNjVidV2= M2m3b|Q5KGi{cx?= NYXSU5gzUW6qaXLpeIlwdiCxZjDHS5Rie2VvMTDpckBpfW2jbjDSVG1KQDJ{NjDj[YxteyCjc4Pld5Nm\CCjczDkbZNzfXC2aX;uJI9nKFKjcEHhJIdmemGweXzn[ZJidnmuYYTpc44h[XRiMD61JJVOKGGodHXyJFQ5KGi{czDifUBqdW23bn;icI91KGGwYXz5d4l{ MoPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF4OUm2NFYoRjNzNkm5OlA3RC:jPh?=
A549 MUnGeY5kfGmxbjDhd5NigQ>? MlzYVoVlfWO2YYPlJGFkfGm4aYT5JGF{e2G7OjDUbIUhUE2JUjDhZ5Rqfmm2eTD3ZZMheGW{Zn;ycYVlKHW|aX7nJGhOTy2Fb1GgdoVlfWO2YYPlJIF{e2G7IHvpeEBnem:vIGPp[41iNUGuZILpZ4ghf2m2aDD0bIUhcHWvYX6gdoVkd22kaX7hcpQheHKxdHXpckBweiBzMECg{txoKHSxdHHsJINmdGxibInzZZRmeyCocn;tJGE2PDliY3XscJMvKEyxdnHzeIF1cW5id3HzJJV{\WRiYYOgZUBxd3OrdHn2[UBkd262cn;sMEBKSzVyPUCuNFI6Pc7:TT6= NXG3RWVsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTB|Lze+R4hGVUKOPD;hQi=>
HepG2 NIe2dHVHfW6ldHnvckBie3OjeR?= NUjOZpNkS2:vcH;1coQhf2G|IHX2ZYx2[XSnZDDmc5IhcW6qaXLpeI9zgSCjY4Tpeol1gSCjZ3HpcpN1KEiPRz3Dc2EhemWmdXP0ZZNmKGmwIFjldGczKGOnbHzzMEBKSzVyPUCuNFM6|ryPLh?= NGXKU2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmw2ODNxJ{7DbGVOSkx:L3G+
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-GSK3β / GSK3β / p-β-catenin / β-catenin / TAZ ; HMGR 30975976 17412884
Immunofluorescence β-catenin 30975976
Growth inhibition assay Cell viability 20205716

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG 300+ 5% Tween80 + 50% ddH2O
For best results, use promptly after mixing.

2.5mg/mL

Chemical Information

Molecular Weight 404.54
Formula

C24H36O5

CAS No. 75330-75-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01478828 Terminated Drug: Lovastatin Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Patrick C Walsh Prostate Cancer Research Fund July 13 2012 Not Applicable
NCT01527669 Completed Drug: LipoCol Forte capsules|Drug: Lovastatin Tablet Healthy Subjects National Taiwan University Hospital|National Science Council Taiwan February 2012 Phase 4
NCT01385020 Completed Drug: Gemfibrozil & red yeast rice (LipoCol) Healthy Subjects National Taiwan University Hospital|National Science Council Taiwan July 2011 Phase 4
NCT00700921 Completed Drug: Lovastatin|Drug: Placebo Chronic Obstructive Pulmonary Disease (COPD) National Jewish Health|National Heart Lung and Blood Institute (NHLBI) April 2008 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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