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SR12813研究進展

發(fā)布日期:2017-10-27   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/SR12813.htmlSR12813/a產(chǎn)品描述:SR12813 is an inhibitor of b3-hydroxy-3-methylgluta
<a href="https://www.medchemexpress.com/SR12813.html">SR12813</a>產(chǎn)品描述:SR12813 is an inhibitor of <b>3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase</b>, with an IC<sub>50</sub> value of 0.85 μM.

IC50 & Target: IC50: 0.85 μM (HMG-CoA Reductase)

<i><b>In Vitro:</b></i> SR-12813 inhibits incorporation of tritiated water into cholesterol with an IC<sub>50</sub> 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 IC<sub>50</sub> of 0.85 μM<sup>[1]</sup>. 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<sup>[1]</sup>.

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