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GSK2807 Trifluoroacetate {[allProObj[0].p_purity_real_show]}

货号:A912563

GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM.

GSK2807 Trifluoroacetate 化学结构 CAS号:2245255-66-5
GSK2807 Trifluoroacetate 化学结构
CAS号:2245255-66-5
GSK2807 Trifluoroacetate 3D分子结构
CAS号:2245255-66-5
GSK2807 Trifluoroacetate 化学结构 CAS号:2245255-66-5
GSK2807 Trifluoroacetate 3D分子结构 CAS号:2245255-66-5
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GSK2807 Trifluoroacetate 纯度/质量文件 产品仅供科研

货号:A912563 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Histone Methyltransferase 其他靶点 纯度
BRD4770 99%+
UNC1999 +++

EZH2, IC50: 2 nM

EZH1, IC50: 45 nM

99%+
EPZ005687 ++

EZH2, Ki: 24 nM

98+%
EPZ015666 +++

PRMT5, Ki: 5 nM

99%+
3-Deazaneplanocin A HCl ++++

S-adenosylhomocysteine hydrolase, Ki: 50 pM

99%+
Tazemetostat +++

EZH2, IC50: 11 nM

EZH2, Ki: 2.5 nM

98%
GSK126 ++

EZH2, IC50: 9.9 nM

99%+
MI-3 +

Menin-MLL, IC50: 648 nM

98%
MM-102 ++

MLL1, IC50: 0.4 μM

99%
EI1 ++

EZH2 (Y641F), IC50: 13 nM

Ezh2 (wild-type), IC50: 15 nM

98%
SGC0946 ++++

DOT1L, IC50: 0.3 nM

99%+
PFI-2 HCl ++++

SETD7, Ki: 0.33 nM

SETD7, IC50: 2 nM

99%+
Pinometostat ++++

DOT1L, Ki: 80 pM

99%+
EPZ004777 +++

DOT1L, IC50: 0.4 nM

99%+
Entacapone ++

COMT, IC50: 151 nM

95%
UNC0379 +

SETD8, IC50: 7.9 μM

99%+
Menin-MLL inhibitor MI-2 +

Menin-MLL, IC50: 446 nM

98%
GSK343 +++

EZH2, IC50: 4 nM

EZH1, IC50: 240 nM

99%+
BIX-01294 3HCl +

G9a, IC50: 2.7 μM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

GSK2807 Trifluoroacetate 生物活性

描述 SMYD3 is a lysine methyltransferase implicated as an oncogene in human malignancies, which is found to be overexpressed in colorectal, breast, prostate, and hepatocellular tumors. Methylation of its target, MEKK2, is important for regulation of the MEK/ERK pathway. GSK2807 Trifluoroacetate is the trifluoroacetate form of GSK2807. GSK2807 is a potent and selective, SAM-competitive inhibitor of SMYD3 with Ki value of 14nM, with selectivity to SMYD3 over a panel of protein methyltransferases including SMYD2, PRMT1, PRMT4, PRMT5, NSD2, NSD3, DOT1L, G9a and ASH1L. GSK2807 could form a dead-end ternary complex with SMYD3 and MEKK2.

GSK2807 Trifluoroacetate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.83mL

1.77mL

0.88mL

17.65mL

3.53mL

1.77mL

GSK2807 Trifluoroacetate 技术信息

CAS号2245255-66-5
分子式C21H33F3N8O7
分子量 566.531
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 105 mg/mL(185.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(88.26 mM)

动物实验配方
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