GSK2807 Trifluoroacetate

目录号: PL13110 纯度: ≥98%
GSK2807 Trifluoroacetate 是 SMYD3 有效的、有选择性的,SAM 竞争性抑制剂,其Ki 值为 14 nM,IC50 为 130 nM。
CAS No. :2245255-66-5
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中文名称
GSK2807 Trifluoroacetate
英文名称
GSK2807 Trifluoroacetate
英文别名
GSK2807 Trifluoroacetate;GSK2807Trifluoroacetate;GSK2807 (Trifluoroacetate);GSK2807;GSK2807 TFA;(S)-2-amino-4-((((2R,3S,4R,5R)-5-(6-amino-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(3-(dimethylamino)propyl)amino)butanoic acid compound with 2,2,2-trifluoroacetic acid (1:1)
Cas No.
2245255-66-5
分子式
C21H33F3N8O7
分子量
566.53
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述
GSK2807 Trifluoroacetate 是 SMYD3 有效的、有选择性的,SAM 竞争性抑制剂,其Ki 值为 14 nM,IC50 为 130 nM。
产品详情
GSK2807 Trifluoroacetate 是 SMYD3 有效的、有选择性的,SAM 竞争性抑制剂,其Ki 值为 14 nM,IC50 为 130 nM。
生物活性
GSK2807 Trifluoroacetate is a potent, selective and SAM-competitive inhibitor of SMYD3, with a K i of 14 nM and an IC 50 of 130 nM.
性状
Solid
IC50 & Target[1][2]
SMYD3 14 nM (Ki) SMYD3 130 nM (IC50)
体外研究(In Vitro)
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). has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
[2]. Kaniskan Hü, et al. Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev. 2018 Feb 14;118(3):989-1068.
溶解度数据
In Vitro: DMSO : 100 mg/mL (176.51 mM; Need ultrasonic)H2O : ≥ 50 mg/mL (88.26 mM)
搜索质检报告(COA)
[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.
[2]. Kaniskan Hü, et al. Inhibitors of Protein Methyltransferases and Demethylases. Chem Rev. 2018 Feb 14;118(3):989-1068.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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