生物活性 | |||
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描述 | Sirtuins are protein deacylases that regulate metabolism and stress responses and are implicated in aging-related diseases[1]. SIRT5 has drawn extensive attention due to its specific catalytic activity for low deacetylation activity but significant desuccinylation, demalonylation and deglutarylation activities[2]. SIRT5 inhibitor 1 (compound 49) is a very potent human sirtuin 5 deacylase inhibitor, with an IC50 of 0.11 μM, >100-fold from compound 1[3]. In vivo rat model of ischemia/reperfusion injury, SIRT5 inhibitor 1 (compound 49) reduced the ischemic area, showing a cardioprotective effect against myocardial injury that was higher than that exerted by diazoxide, used as reference cardioprotective drug, and maximum with compound 49[4]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.48mL 0.30mL 0.15mL |
7.41mL 1.48mL 0.74mL |
14.82mL 2.96mL 1.48mL |
参考文献 |
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