SR 12813

A PXR agonist and cholesterol biosynthesis inhibitor

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
10mg

￥762.00

610.00

- +
50mg

￥2500.00

2000.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci4426
CAS: 126411-39-0
别名: GW 485801
分子式: C24H42O7P2
分子量: 504.53
纯度: >98%
溶解度: DMF: 15 mg/mL,DMSO: 1 mg/mL,Ethanol: 5 mg/mL
储存: Store at -20°C
库存: 现货

Background

SR12813 is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, with an IC50 value of 0.85 μM.

SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC50 of 1.2 μM but has no effect on fatty acid synthesis. Furthermore, SR-12813 reduces cellular 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase activity with an IC50 of 0.85 μM[1]. Both 25-HC and SR-12813 can kill mammalian cells through blocking the synthesis of cholesterol, thereby they are ideal regents for lethal selection. SR-12813 kills HeLa cells at concentration range from 8 μM to 16 μM. SR-12813 kills wild type cells and mutant cells infected by Ad-Cre (SL-5+Cre), but the mutant SL-5 survives this condition. SR-12813 or 25-HC promotes the degradation of the 95-KDa full-length HMG-CoA reductase in wild type HeLa and SL-5 mutant cells[1].

参考文献:
[1]. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.
[2]. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.

Protocol

Kinase experiment:

Briefly, compounds are added to the cells in Me2SO (final concentration, 0.1%). After the experiment cells are lysed by the addition of 0.1 mL of 0.25% Brij 96, 0.1 M sucrose, 0.1 M KF, 50 mM KCl, 40 mM potassium dihydrophosphate, 30 mM EDTA, 5 mM dithiothreitol, pH 7.4 at room temperature. In some experiments KF is omitted to measure “total” HMG-CoA reductase activity. HMG-CoA reductase activity in the cell lysate is further determined.

参考文献:

[1]. Berkhout T, et al. The novel cholesterol-lowering drug SR-12813 inhibits cholesterol synthesis via an increased degradation of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. J Biol Chem. 1996 Jun 14;271(24):14376-82.
[2]. Jiang W, et al. Forward genetic screening for regulators involved in cholesterol synthesis using validation-based insertional mutagenesis. PLoS One. 2014 Nov 26;9(11):e112632.