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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。 |
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. |
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 |
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 |