PROTACSirt2Degrader-1是一种基于SirReal的PROTAC，为Sirt2的降解剂，由一个高效、同种型选择性的Sirt2抑制剂，一个连接物和thalidomide(E3泛素化连接酶的配体)组成。PROTACSirt2Degrader-1对Sirt2的IC50值为0.25μM，而对Sirt1/Sirt3(IC50>100μM)无作用
PROTAC Sirt2 Degrader-1 is a SirReal-based PROTAC, acts as a Sirt2 degrader, composed of a highly potent and isotype-selective Sirt2 inhibitor, a linker and thalidomide, a bona fide cereblon ligand for E3 ubiquitin ligase. PROTAC Sirt2 Degrader-1 shows an IC50 of 0.25 μM for Sirt2, with no effect on Sirt1/Sirt3 (IC50s > 100 μM)[1].
PROTAC Sirt2 Degrader-1 (Compound 12; 10 µM, 1-6 hours) induces Sirt2 degradation in HeLa cells[1].|| Western Blot Analysis[1]||Cell Line:|HeLa cells|Concentration:|10 µM|Incubation Time:|1-6 hours|Result:|Caused Sirt2 degradation, but showed no effect on Sirt1 levels.
[1]. Schiedel M, et al. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J Med Chem. 2018 Jan 25;61(2):482-491.
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