Lovastatin
别名: Mevinolin, MK-803 中文名称：洛伐他汀
Lovastatin是一种HMG-CoA还原酶抑制剂，无细胞试验中IC50为3.4 nM，用于降胆固醇（降脂药）。Lovastatin 可触发自噬。
Lovastatin Chemical Structure
CAS: 75330-75-5
产品质控
批次：
纯度：
99.99%
99.99
Lovastatin相关产品
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相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Lovastatin是一种HMG-CoA还原酶抑制剂，无细胞试验中IC50为3.4 nM，用于降胆固醇（降脂药）。Lovastatin 可触发自噬。 | ||
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| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在大鼠原代星形胶质细胞中，Lovastatin抑制了LPS-和细胞因子介导的NO产生以及iNOS的表达。在大鼠原代星形胶质细胞，小胶质细胞和巨噬细胞中，Lovastatin抑制了LPS-诱导的TNF-α，IL-1β和IL-6的表达。[1] Lovastatin导致超过95％的DNA合成的抑制，这通过[3H]胸苷与DNA的结合测定。Lovastatin使细胞同步在G1，而不是在细胞周期的G0期。Lovastatin对RAS的依赖性以及RAS无关的细胞系有相似的生长抑制活性。[2] Lovastatin使载脂蛋白-B的含脂蛋白显著减少，特别是低密度脂蛋白胆固醇，以及血浆甘油三酯erides，以及高密度脂蛋白胆固醇的少量增加。[3] Lovastatin通过抑制蛋白酶体使细胞停滞，这导致p21和p27蛋白的积累，使细胞阻滞在G1期。Lovastatin是羟甲基戊二酰基（HMG)-CoA还原酶，是胆固醇合成的限速酶。Lovastatin可用于阻止培养细胞在细胞周期的G1期，导致细胞周期蛋白依赖性激酶抑制剂（CKIs）p21和p27蛋白的稳定化。[4] 在表达激活p21ras的人膀胱癌T24细胞中，Lovastatin（2-10 mM）使细胞停留在G1期和并延长-或使一小部分细胞停滞-在细胞周期中的G2期。的G2期。在人膀胱癌T24细胞中，Lovastatin（50 mM）表现细胞毒性。[5] |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-AKT / AKT / p-GSK3β / GSK3β / p-β-catenin / β-catenin / TAZ HMGR |
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30975976 | |
| Immunofluorescence | β-catenin |
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30975976 | |
| Growth inhibition assay | Cell viability |
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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 |
化学信息&溶解度
| 分子量 | 404.54 | 分子式 | C24H36O5 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 80 mg/mL ( (197.75 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 35 mg/mL (86.51 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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