SGC707
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货号：A165657
SGC707 is a chemical probe of PRMT3 with IC50 of 31 nM.
SGC707 化学结构
SGC707 3D分子结构
规格
价格
会员价
库存
数量
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SGC707 质控信息
BRD4770
✔
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UNC1999
+++
EZH1, IC50: 45 nM
EZH2, IC50: 2 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
+++
EZH1, IC50: 240 nM
EZH2, IC50: 4 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。
SGC707 生物活性
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] 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]
SGC707 动物研究
Dose
Mice: 10 mg/kg, 30 mg/kg[3]
Administration
i.p.
SGC707 参考文献
[1] Kaniskan HÜ, Szewczyk MM, et al. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70.
[2] Hoekstra M, Nahon JE, et al. Inhibition of PRMT3 activity reduces hepatic steatosis without altering atherosclerosis susceptibility in apoE knockout mice. Biochim Biophys Acta Mol Basis Dis. 2019 Jun 1;1865(6):1402-1409.
[3] Kaniskan HÜ, Szewczyk MM, Yu Z, Eram MS, Yang X, Schmidt K, Luo X, Dai M, He F, Zang I, Lin Y, Kennedy S, Li F, Dobrovetsky E, Dong A, Smil D, Min SJ, Landon M, Lin-Jones J, Huang XP, Roth BL, Schapira M, Atadja P, Barsyte-Lovejoy D, Arrowsmith CH, Brown PJ, Zhao K, Jin J, Vedadi M. A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Angew Chem Int Ed Engl. 2015 Apr 20;54(17):5166-70. doi: 10.1002/anie.201412154. Epub 2015 Feb 27. PMID: 25728001; PMCID: PMC4400258.
[4] Hoekstra M, Nahon JE, de Jong LM, Kröner MJ, de Leeuw LR, Van Eck M. Inhibition of PRMT3 activity reduces hepatic steatosis without altering atherosclerosis susceptibility in apoE knockout mice. Biochim Biophys Acta Mol Basis Dis. 2019 Jun 1;1865(6):1402-1409. doi: 10.1016/j.bbadis.2019.02.012. Epub 2019 Feb 15. PMID: 30776415.
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SGC707 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
3.35mL
0.67mL
0.34mL
16.76mL
3.35mL
1.68mL
33.52mL
6.70mL
3.35mL
SGC707 技术信息
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