GSK2807 Trifluoroacetate
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货号：A912563
GSK2807 Trifluoroacetate is a SMYD3 SAM-competitive inhibitor with Ki of 14 nM.
GSK2807 Trifluoroacetate 化学结构
GSK2807 Trifluoroacetate 3D分子结构
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GSK2807 Trifluoroacetate 质控信息
BRD4770
✔
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UNC1999
+++
EZH2, IC50: 2 nM
EZH1, IC50: 45 nM
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EPZ005687
++
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EPZ015666
+++
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3-Deazaneplanocin A HCl
++++
S-adenosylhomocysteine hydrolase, Ki: 50 pM
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EPZ6438
+++
EZH2, IC50: 11 nM
EZH2, Ki: 2.5 nM
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GSK126
++
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MI-3
+
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MM-102
++
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EI1
++
Ezh2 (wild-type), IC50: 15 nM
EZH2 (Y641F), IC50: 13 nM
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SGC0946
++++
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PFI-2 HCl
++++
SETD7, IC50: 2 nM
SETD7, Ki: 0.33 nM
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Pinometostat
++++
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EPZ004777
+++
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Entacapone
++
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UNC0379
+
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Menin-MLL inhibitor MI-2
+
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GSK343
+++
EZH2, IC50: 4 nM
EZH1, IC50: 240 nM
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BIX-01294 3HCl
+
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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
摩尔计算器
总药量计算器
工作液计算器
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
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