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。
货号:ajcx11600
CAS:N/A
分子式:C21H33F3N8O7
分子量：566.53
溶解度:H2O : ≥ 50 mg/mL (88.26 mM)
纯度：98%
存储：Store at -20°C
库存： 现货

Background:

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].

参考文献:
[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.