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PROTAC Sirt2 Degrader-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PROTAC Sirt2 Degrader-1图片
CAS NO:2098487-75-1
包装与价格:
包装价格(元)
5mg询价
10mg询价

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
Cas No.2098487-75-1
Canonical SMILESO=C(N(C(CCC1=O)C(N1)=O)C2=O)C(C2=CC=C3)=C3OCC(NCCCCN4C=C(COC5=CC(CC6=CN=C(NC(CSC7=NC(C)=CC(C)=N7)=O)S6)=CC=C5)N=N4)=O
分子式C40H40N10O8S2
分子量852.94
溶解度DMSO : ≥ 100 mg/mL (117.24 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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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