| 产品描述： | GSK4112 (SR6452) is a Rev-erbα agonist with an EC50 value of 0.4 μM. GSK4112 can be used as a chemical tool to probe the function of Rev-erbα in transcriptional repression, regulation of circadian biology, and metabolic pathways |
| 靶点： |
Rev-ErbBα;Autophagy |
| 体外研究： |
GSK4112 (0-100 μM; 1 h) interacts with Rev-erbα with an EC50 value of 0.4 μM. GSK4112 (10 μM; 6 h) represses expression of bmal1 and the target genes associated with the pathway of gluconeogenesis, recruits HDAC3 and modulates the effect of Rev-erbα on oscillation of hepatic gene expression. GSK4112 (10 μM; 16 h) reduces glucose output in murine hepatocytes. RT-PCR Cell Line: HepG2 cell line Concentration: 10 μM Incubation Time: 6 hours Result: Repressed mRNA levels of bmal1, G6 Pase, PEPCK and PGC1α. |
| 体内研究： |
GSK4112 (25 mg/kg; i.p. 0.5 h before Jo2 exposure) attenuates Fas-induced hepatic damage. Animal Model: Male C57BL/6 mice with Fas-induced acute hepatic damage Dosage: 25 mg/kg Administration: Intraperitoneal injection; 25 mg/kg; 0.5 h before Jo2 exposure Result: Obviously ameliorated the degree of liver damage, suppressed Jo2-induced ALT and AST increasing, improved the survival rate of mice and suppressed Fas-induced hepatocyte apoptosis. |
| 参考文献： |
1. Grant D, et al. GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. ACS Chem Biol. 2010 Oct 15;5(10):925-932. 2. Shao R, et al. REV-ERBα Agonist GSK4112 attenuates Fas-induced Acute Hepatic Damage in Mice. Int J Med Sci. 2021 Oct 25;18(16):3831-3838. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.52 ml |
12.598 ml |
25.196 ml |
| 5 mM |
0.504 ml |
2.52 ml |
5.039 ml |
| 10 mM |
0.252 ml |
1.26 ml |
2.52 ml |
| 50 mM |
0.05 ml |
0.252 ml |
0.504 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京