| 產(chǎn)品描述： | SGC707 is a potent, selective, and non-competitive PRMT3 (protein arginine methyltransferase 3) inhibitor (IC50=31 nM, Kd=53 nM). |
| 靶點(diǎn)： |
PRMT3:31 nM (IC50);HistoneMethyltransferase |
| 體外研究： |
SGC707 (0-10 μM; 6 h) binds to PRMT3 in both HEK293 and A549 cells. Cell Viability Assay Cell Line: HEK293 and A549 cells Concentration: 0-10 μM Incubation Time: 6 hours Result: Stabilized PRMT3 in both HEK293 and A549 cells with EC50 values of 1.3 μM and 1.6 μM, respectively. |
| 體內(nèi)研究： |
SGC707 (intraperitoneal injection; 10 mg/kg; 3 times per week; 3 w) treatment reduces hepatic steatosis and plasma triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Animal Model: Western-type diet-fed LDL (lipoprotein) receptor knockout mice Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; 3 times per week; 3 weeks Result: Exhibited 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels. |
| 參考文獻(xiàn)： |
1. Kaniskan Hü, 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. de Jong LM, et al. PRMT3 inhibitor SGC707 reduces triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. Sci Rep. 2022 Jan 10;12(1):483. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.352 ml |
16.759 ml |
33.519 ml |
| 5 mM |
0.67 ml |
3.352 ml |
6.704 ml |
| 10 mM |
0.335 ml |
1.676 ml |
3.352 ml |
| 50 mM |
0.067 ml |
0.335 ml |
0.67 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京