产品说明书

SGC707

Print
Chemical Structure| 1687736-54-4 同义名 : -
CAS号 : 1687736-54-4
货号 : A165657
分子式 : C16H18N4O2
纯度 : 99%+
分子量 : 298.34
MDL号 : MFCD28411624
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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]
实验方案
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
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.