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SGC707 {[allProObj[0].p_purity_real_show]}

货号:A165657

SGC707 is a chemical probe of PRMT3 with IC50 of 31 nM.

SGC707 化学结构 CAS号:1687736-54-4
SGC707 化学结构
CAS号:1687736-54-4
SGC707 3D分子结构
CAS号:1687736-54-4
SGC707 化学结构 CAS号:1687736-54-4
SGC707 3D分子结构 CAS号:1687736-54-4
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SGC707 纯度/质量文件 产品仅供科研

货号:A165657 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

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]. 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]

SGC707 动物研究

Dose Mice: 10 mg/kg, 30 mg/kg[3] (i.p.)
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.

SGC707 实验方案

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

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
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