Home Metabolism HMG-CoA Reductase inhibitor - Autophagy activator Lovastatin For research use only.

Lovastatin

Synonyms: Mevinolin, MK-803

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 triggers autophagy.

Lovastatin Chemical Structure

Lovastatin Chemical Structure

CAS: 75330-75-5

Selleck's Lovastatin has been cited by 50 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

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Choose Selective HMG-CoA Reductase Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HES 9 cell line Function assay Concentration required to inhibit HMG-CoA reductase by 50% was determined in HES 9 cell line, IC50=0.013 μM 1527791
HEP G2 Function assay Inhibition of the incorporation of sodium [14C]acetate into cholesterol in HEP G2 cells., IC50=0.05μM. 1656041
HEP G2 Function assay Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line), IC50=0.00005μM. 2153213
HEP G2 Function assay Inhibition of cellular HMG-CoA reductase in cultures of human HEP G2 cells, determined by decreased incorporation of sodium [14C]acetate into cholesterol., IC50=0.05μM. 2296036
HEP G2 Function assay Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029μM. 7932551
HEP-G2 Function assay Tested for ability to inhibit incorporation of [14C]acetate into cholesterol in cultured human hepatoma (HEP-G2) cells; 0.061-0.10, IC50=0.079μM. 8246237
3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin transport in 3T3-G185 cells, IC50=26μM. 11474784
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=32.7μM. 11716514
MDCK Function assay TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells, IC50=10μM. 15616150
HEK293 Function assay TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells, IC50=28μM. 15616150
Huh-7/3-1 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b in human Huh-7/3-1 cells assessed as inhibition of HCV replication after 72 hrs by luciferase assay 16408072
SW480 Growth inhibition assay 96 hrs Growth inhibition of human SW480 cells after 96 hrs by MTS assay, IC50=7.1μM. 17472962
LS180 Growth inhibition assay 96 hrs Growth inhibition of human LS180 cells after 96 hrs by MTS assay, IC50=25.3μM. 17472962
HT29 Growth inhibition assay 96 hrs Growth inhibition of human HT29 cells after 96 hrs by MTS assay, IC50=46.8μM. 17472962
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by MTS assay in presence of >50 uM mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Decrease in survivin expression in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis 17472962
SW480 Function assay 20 uM 48 hrs Reversal of reduction in survivin expression in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of 100 uM mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of reduction in survivin mRNA expression in human SW480 cells at 20 uM after 48 hrs by RT-PCR technique in presence of 100 uM mevalonate 17472962
LS180 Function assay 20 uM Inhibition of survivin expression in parent human LS180 cells at 20 uM by immunoblot analysis 17472962
LS180 Function assay 20 uM Inhibition of survivin expression in survivin gene transfected human LS180 cells at 20 uM immunoblot analysis 17472962
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of farnesyl pyrophosphate 17472962
SW480 Growth inhibition assay 20 uM 48 hrs Reversal of growth inhibition of human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of geranylgeranyl pyrophosphate 17472962
SW480 Function assay 20 uM 48 hrs Decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of mevalonate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of farnesyl pyrophosphate 17472962
SW480 Function assay 20 uM 48 hrs Reversal of decrease in isoprenylated Ras level in human SW480 cells at 20 uM after 48 hrs by immunoblot analysis in presence of geranylgeranyl pyrophosphate 17472962
SW480 Function assay 20 uM Inhibition of FBS-stimulated increase in Ras protein expression in human SW480 cells assessed as GTP-bound protein at 20 uM by immunoblot analysis 17472962
SW480 Function assay 20 uM Reversal of inhibition of FBS-stimulated increase in Ras protein expression in human SW480 cells assessed as GTP-bound protein at 20 uM by immunoblot analysis 17472962
SW480 Function assay 20 uM Inhibition of FBS-stimulated increase in Akt phosphorylation in human SW480 cells at 20 uM by immunoblot analysis 17472962
LS180 Growth inhibition assay 72 hrs Blockade of growth inhibition of human LS180 cells after 72 hrs by MTS method 17472962
K562 Function assay 48 hrs Inhibition of GGTase1 in human K562 cells assessed as reduction of Rap1a protein geranylgeranylation after 48 hrs by Western blotting 20832326
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50=11.4μM. 23570542
A549 Function assay 5 mins Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis, IC50=19.8μM. 23570542
HS68 Cytotoxicity assay 72 hrs Cytotoxicity against human HS68 cells after 72 hrs by MTT assay, IC50=23.2μM. 23570542
MEF Cytotoxicity assay 72 hrs Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay, IC50=35μM. 23570542
MDA-MB-231 Function assay 1 to 10 uM 24 hrs Induction of p21 expression in human PR, ER, HER2-negative human MDA-MB-231 cells at 1 to 10 uM after 24 hrs by western blot analysis 24556504
MDA-MB-361 Growth inhibition assay 48 hrs Growth inhibition of ER-positive, HER2-positive human MDA-MB-361 cells after 48 hrs by WST-1 assay 24556504
MDA-MB-468 Growth inhibition assay 48 hrs Total growth inhibition of PR, ER, HER2-negative human MDA-MB-468 cells after 48 hrs by WST-1 assay 24556504
AU565 Growth inhibition assay 48 hrs Growth inhibition of ER-negative, HER2-positive human AU565 cells after 48 hrs by WST-1 assay 24556504
MCF7 Growth inhibition assay 48 hrs Total growth inhibition of ER-positive, HER2-negative human MCF7 cells after 48 hrs by WST-1 assay 24556504
MDA-MB-231 Growth inhibition assay >10 uM 48 hrs Total growth inhibition of PR, ER, HER2-negative human MDA-MB-231 cells at >10 uM after 48 hrs by WST-1 assay 24556504
RPMI-8226 Function assay 10 uM 48 hrs Inhibition of HMG-coA reductase in human RPMI-8226 cells assessed as disruption of Rap1a geranylgeranylation at 10 uM after 48 hrs by western blot analysis 24726306
HepG2 Function assay 1 uM 6 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced lipid accumulation at 1 uM after 6 hrs by oil-red O staining based spectrophotometry 25304895
HepG2 Function assay 10 uM 24 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced total cholesterol accumulation at 10 uM after 24 hrs by oil-red O staining based spectrophotometry 25304895
HepG2 Function assay 10 uM 24 hrs Lipid-lowering effect in human HepG2 cells assessed as reduction in oleic acid-induced triglyceride accumulation at 10 uM after 24 hrs by oil-red O staining based spectrophotometry 25304895
RPMI8226 Apoptosis assay 20 uM 48 hrs Induction of apoptosis in human RPMI8226 cells assessed as increase in PARP cleavage at 20 uM incubated for 48 hrs by immunoblot method 25935643
RPMI8226 Apoptosis assay 20 uM 48 hrs Induction of apoptosis in human RPMI8226 cells assessed as increase in caspase-3 cleavage at 20 uM incubated for 48 hrs by immunoblot method 25935643
HepG2 Function assay 6 hrs Lipid lowering activity in human HepG2 cells assessed as decrease in oleic acid elicited lipid accumulation after 6 hrs by oil-red O staining method, IC50=8.3μM. 26169125
A549 Antiviral assay 48 hrs Antiviral activity against Dengue virus 2 NGC infected in human A549 cells assessed as reduction in virus replication after 48 hrs by renilla luciferase reporter gene assay, EC50=1.82μM. 26771861
Neuro2a Function assay 1 uM Inhibition of HMGCoA reductase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Vero Cytotoxicity assay Cytotoxicity against African green monkey Vero cells, IC50=2.2μM. 27228159
KB Cytotoxicity assay Cytotoxicity against human KB cells by resazurin microplate assay, IC50=15.6μM. 27228159
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50=5.4μM. 27756564
MDA-MB-231 Function assay 30 uM 24 hrs Induction of reactive oxygen species in human MDA-MB-231 cells at 30 uM after 24 hrs by DCFH-DA probe-based flow cytometric method 27756564
MDA-MB-231 Function assay 10 uM 6 to 24 hrs Induction of CHK1/2 phosphorylation in human MDA-MB-231 cells assessed as increase in p53 phosphorylation at 10 uM after 6 to 24 hrs by Western blot method 27756564
MDA-MB-231 Function assay 10 uM 6 to 24 hrs Induction of ATM phosphorylation in human MDA-MB-231 cells at 10 uM after 6 to 24 hrs by Western blot method 27756564
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
RPMI8226 Function assay 0.5 uM 48 hrs Inhibition of FTase in human RPMI8226 cells assessed as disruption of H-ras farnesylation at 0.5 uM after 48 hrs by immunoblot analysis 31699606
RPMI8226 Function assay 0.5 uM 48 hrs Inhibition of GGtase-1 in human RPMI8226 cells assessed as disruption of Rap1a geranylgeranylation at 0.5 uM after 48 hrs by immunoblot analysis 31699606
A549 Function assay Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, IC50=0.0295μM. ChEMBL
HepG2 Function assay Compound was evaluated for inhibitory activity against HMG-CoA reductase in HepG2 cells, IC50=0.039μM. ChEMBL
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Biological Activity

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 triggers autophagy.
Targets
HMG-CoA reductase [1]
(Cell-free assay)
3.4 nM
In vitro
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 Research Cell lines Astrocytes
Concentrations 10 μM
Incubation Time 8 h
Method

Cells preincubated in serum-free media with 10 µM lovastatin or 5 mM NaPA, or a combination of 2 µM lovastatin and 2 mM NaPA for 8 h received 1 µg/ml of LPS.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT / p-GSK3β / GSK3β / p-β-catenin / β-catenin / TAZ HMGR 30975976
Immunofluorescence β-catenin 30975976
Growth inhibition assay Cell viability 20205716
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01478828 Terminated Prostate Cancer Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Patrick C Walsh Prostate Cancer Research Fund July 13 2012 Not Applicable
NCT01527669 Completed Healthy Subjects National Taiwan University Hospital|National Science Council Taiwan February 2012 Phase 4
NCT01385020 Completed Healthy Subjects National Taiwan University Hospital|National Science Council Taiwan July 2011 Phase 4
NCT00700921 Completed Chronic Obstructive Pulmonary Disease (COPD) National Jewish Health|National Heart Lung and Blood Institute (NHLBI) April 2008 Phase 2

Chemical lnformation & Solubility

Molecular Weight 404.54 Formula

C24H36O5
CAS No. 75330-75-5 SDF Download Lovastatin SDF
Smiles CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (197.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 35 mg/mL

Water : Insoluble


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