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Submit ReviewLovastatin
说明： Potent HMG-CoA reductase inhibitor
别名： Mevinolin
化学名： (2S)-(1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-Hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl-2-methyl butanoate
纯度： ≥97% (HPLC)
生物活性 for Lovastatin
Lovastatin is a potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.6 nM) therefore decreases cholesterol biosynthesis, in vitro and in vivo. Indirectly inhibits Rho-GTPase activity by depleting intracellular pool of isoprene residues. Decreases CDK2, 4, 6 and cyclin E levels and induces G1 arrest and apoptosis in tumor cell lines in vitro. Inactive lactam prodrug of lovastatin hydroxy acid, naturally bioactivated in vivo following oral administration.
化合物库 for Lovastatin
Lovastatin is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
技术数据 for Lovastatin
| 分子量 | 404.54 |
| 公式 | C24H36O5 |
| 储存 | Store at +4°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 75330-75-5 |
| PubChem ID | 53232 |
| InChI Key | PCZOHLXUXFIOCF-BXMDZJJMSA-N |
| Smiles | [H][C@]12[C@H](C[C@@H](C)C=C1C=C[C@H](C)[C@@H]2CC[C@@H]1C[C@@H](O)CC(=O)O1)OC(=O)[C@@H](C)CC |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Lovastatin
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 20.23 | 50 温和加热 | |
| DMSO | 40.45 | 100 |
制备储备液 for Lovastatin
以下数据基于产品分子量 404.54。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.47 mL | 12.36 mL | 24.72 mL |
| 5 mM | 0.49 mL | 2.47 mL | 4.94 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.47 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.49 mL |
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产品说明书 for Lovastatin
参考文献 for Lovastatin
参考文献是支持产品生物活性的出版物。
Alberts (1988) Discovery, biochemistry and biology of lovas. Am.J.Cardiol. 62 10J PMID: 3055919
Alberts et al (1980) Mevinolin: a highly potent competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase and a cholesterol-lowering agent. Proc.Natl.Acad.Sci.U.S.A. 77 3957 PMID: 6933445
Park et al (1999) Lovastatin-induced inhibition of HL-60 cell proliferation via cell cycle arrest and apoptosis. Anticancer Res. 19 3133 PMID: 10652602
Ziegler et al (2017) Rho inhibition by lovas. affects apoptosis and DSB repair of primary human lung cells in vitro and lung tissue in vivo following fractionated irradiation. Cell Death Dis. 8 e2978 PMID: 28796249
If you know of a relevant reference for Lovastatin, please let us know.
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关键词: Lovastatin, Lovastatin supplier, HMG-CoA, reductases, inhibitors, inhibits, statins, Mevinolin, Reductase, 1530, Tocris Bioscience
⚠ WARNING: This product can expose you to chemicals including Lovastatin, which is known to the State of California to cause reproductive toxicity with developmental effects. For more information, go to www.P65Warnings.ca.gov
11 篇 Lovastatin 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Lovastatin 的部分引用包括：
Roche et al (2018) Trafficking of cholesterol to the ER is required for NLRP3 inflammasome activation. J Cell Biol 217 3560 PMID: 30054450
Ibrahim et al (2015) The Effects of Targeted Deliveries of lovas. and Tocotrienol on Ossification-Related Gene Expressions in Fracture Healing in an Osteoporosis Rat Model. Int J Environ Res Public Health 12 12958 PMID: 26501302
Buchovecky et al (2013) A suppressor screen in Mecp2 mutant mice implicates cholesterol metabolism in Rett syndrome. Nat Genet 45 1013 PMID: 23892605
Kah et al (2012) Selective induction of apoptosis by HMG-CoA reductase inhibitors in hepatoma cells and dependence on p53 expression. Oncol Rep 28 1077 PMID: 22710979
Park et al (2016) Pyrin inflammasome activation and RhoA signaling in the autoinflammatory diseases FMF and HIDS. Nat Immunol 17 914 PMID: 27270401
Leznicki et al (2018) Expansion of DUB functionality generated by alternative isoforms - USP35, a case study. J Cell Sci 131 PMID: 29685892
Saqcena et al (2015) Apoptotic effects of high-dose rapamycin occur in S-phase of the cell cycle. Oncotarget 14 2285 PMID: 25945415
Rojo-Arreola et al (2014) Chemical and genetic validation of the statin drug target to treat the helminth disease, schistosomiasis. PLoS One 9 e87594 PMID: 24489942
Horlbeck et al (2018) Mapping the Genetic Landscape of Human Cells. Cell 174 953 PMID: 30033366
Nölting et al (2014) Combination of 13-Cis retinoic acid and lovastatin: marked antitumor potential in vivo in a pheochromocytoma allograft model in female athymic nude mice. Endocrinology 155 2377 PMID: 24762141
Vainio et al (2011) Phospholipase PLA2G7, associated with aggressive prostate cancer, promotes prostate cancer cell migration and invasion and is inhibited by STAT. J Neurosci 2 1176 PMID: 22202492
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Lovastatin 的评论
平均评分: 5 (Based on 1 Review.)
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Filter by:
GTPase inhibitor.
By
Mengxi Lv on 03/26/2018
分析类型： In Vitro
种属： Other
细胞系/组织： chondrocyte
used as Rho GTPase activity inhibitor
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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