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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 | SGC707 is a potent and selective PRMT3 inhibitor with IC50 value of 31nM. SGC707 stabilized PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3μm and 1.6μm in PRMT3 InCELL Hunter Assays. It reduced PRMT3-dependent H4R3me2a in dose-dependent manner[3]. Chronic treatment with SGC707, i.p., 3 times per week, developed less severe hepatic steatosis as exemplified by the 51% reduced liver triglyceride levels and led a body weight loss by 94% of 12-week old hyperlipidemic apolipoprotein E knockout mice mice fed a Western-type diet for six weeks to induce both hepatic steatosis and atherosclerosis. This may due to the inhibition of PRMT3 uncoupling two transcriptional pathways, of both cholesterol metabolism and hepatic lipogenesis, in vivo by acting as a specific lipogenic coactivator of LXR[4]. |
作用机制 | SGC707 binds an allosteric site at the interface of the two PRMT3 subunits that is distant from the site of methyl transfer.[3] |
Dose | Mice: 10 mg/kg, 30 mg/kg[3] (i.p.) |
Administration | i.p. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.35mL 0.67mL 0.34mL |
16.76mL 3.35mL 1.68mL |
33.52mL 6.70mL 3.35mL |
CAS号 | 1687736-54-4 |
分子式 | C16H18N4O2 |
分子量 | 298.34 |
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 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(351.95 mM),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 |