SIRT5 inhibitor 1

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Chemical Structure| 2166487-21-2 同义名 : -
CAS号 : 2166487-21-2
货号 : A1176889
分子式 : C31H39FN6O6S2
纯度 : 99%+
分子量 : 674.81
MDL号 : MFCD31746885
存储条件:

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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

[1]Kalbas D, Liebscher S, Nowak T, et al. Potent and Selective Inhibitors of Human Sirtuin 5. J Med Chem. 2018;61(6):2460-2471.

[2]Yingying Wang, Hui Chen, Xiaoming Zha. Overview of SIRT5 as a potential therapeutic target: Structure, function and inhibitors, European Journal of Medicinal Chemistry. 2022; 236: 114363.

[3]Rajabi N, et al. Mechanism-Based Inhibitors of the Human Sirtuin 5 Deacylase: Structure-Activity Relationship, Biostructural, and Kinetic Insight. Angew Chem Int Ed Engl. 2017 Nov 20;56(47):14836-14841.

[4]Nicola Mautone, Clemens Zwergel, Antonello Mai & Dante Rotili (2020) Sirtuin modulators: where are we now? A review of patents from 2015 to 2019, Expert Opinion on Therapeutic Patents, 30:6, 389-407.