Gambogenic acid binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination.
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产品名称 | Histone Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BRD4770 | ✔ | 99%+ | |||||||||||||||||
UNC1999 |
+++
EZH1, IC50: 45 nM EZH2, IC50: 2 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 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 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 |
+++
EZH1, IC50: 240 nM EZH2, IC50: 4 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。 |
靶点 |
|
描述 | Gambogenic acid binds to Cys668 within the EZH2-SET domain, triggering EZH2 degradation through COOH terminus of Hsp70‐interacting protein (CHIP)‐mediated ubiquitination. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.59mL 0.32mL 0.16mL |
7.93mL 1.59mL 0.79mL |
15.85mL 3.17mL 1.59mL |
CAS号 | 173932-75-7 |
分子式 | C38H46O8 |
分子量 | 630.77 |
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(166.46 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 |
动物实验配方 |