ホームページ Metabolism HMG-CoA Reductase inhibitor - Autophagy activator Lovastatin For research use only.

Lovastatin

別名：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化学構造

CAS No. 75330-75-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 40500 国内在庫あり
JPY 88500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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文献中Selleckの製品使用例（54）

製品安全説明書

現在のバッチを見る： 純度： 99.99%
99.99

Lovastatin関連製品

シグナル伝達経路

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductaseシグナル伝達経路

HMG-CoA Reductase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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
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-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
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
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
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 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
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
SW480 Growth inhibition assay 96 hrs Growth inhibition of human SW480 cells after 96 hrs by MTS assay, IC50=7.1μM. 17472962
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
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
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-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
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
PC3 Cytotoxicity assay 48 hrs Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by SRB assay, IC50=5.4μM. 27756564
HEK293 Function assay TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells, IC50=28μM. 15616150
MDCK Function assay TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells, IC50=10μM. 15616150
NIH-3T3-G185 Function assay TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50=32.7μM. 11716514
3T3-G185 Function assay TP_TRANSPORTER: inhibition of Daunorubicin transport in 3T3-G185 cells, IC50=26μM. 11474784
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
HEP G2 Function assay Tested for inhibition of cholesterol biosynthesis in HEP G2 cells, IC50=0.029μM. 7932551
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 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 the incorporation of sodium [14C]acetate into cholesterol in HEP G2 cells., IC50=0.05μM. 1656041
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
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
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
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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生物活性

製品説明 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]
細胞実験 細胞株 Astrocytes
濃度 10 μM
反応時間 8 h
実験の流れ

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.
実験結果図 Methods Biomarkers 結果図 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

化学情報

分子量 404.54 化学式

C24H36O5
CAS No. 75330-75-5 SDF Download Lovastatin SDFをダウンロードする
Smiles CCC(C)C(=O)OC1CC(C=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O)C
保管

In vitro
Batch:

DMSO : 80 mg/mL ( (197.75 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 35 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Tags: Lovastatinを買う | Lovastatin ic50 | Lovastatin供給者 | Lovastatinを購入する | Lovastatin費用 | Lovastatin生産者 | オーダーLovastatin | Lovastatin化学構造 | Lovastatin分子量 | Lovastatin代理店