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GSK2807 Trifluoroacetate
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。
GSK2807 Trifluoroacetate图片
包装与价格:
包装价格(元)
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GSK2807 Trifluoroacetate 是一种有效的、选择性的、SAM 竞争性的 SMYD3 抑制剂,Ki 为 14 nM,IC50 为 130 nM。
Canonical SMILESNC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(CC[C@H](N)C(O)=O)CCCN(C)C)O3)C=N2)=NC=N1.OC(C(F)(F)F)=O
分子式C21H33F3N8O7
分子量566.53
溶解度Water : ≥ 50 mg/mL (88.26 mM)
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

GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a Ki of 14 nM.

A high-resolution crystal structure reveals that GSK2807 bridges the gap between the SAM-binding pocket and the substrate lysine tunnel of SMYD3. GSK2807 is 24-fold selective for SMYD3 in comparison with the closely related enzyme SMYD2 (Ki=14±6 nM and 345±36 nM, respectively)[1].

References:
[1]. Van Aller GS, et al. Structure-Based Design of a Novel SMYD3 Inhibitor that Bridges the SAM-and MEKK2-Binding Pockets. Structure. 2016 May 3;24(5):774-781.

 
 
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