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GSK5182

CAS No. : 877387-37-6

MCE 国际站：GSK5182

产品活性：GSK5182 是一种高效选择性，具有口服活性的 ERRγ 反向激动剂，其 IC₅₀ 值为 79 nM。GSK5182 不与其他核受体相互作用，包括 ERRα 和 ERα。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。

研究领域：Vitamin D Related/Nuclear Receptor  |  Metabolic Enzyme/Protease  |  Immunology/Inflammation  |  NF-κB

作用靶点：Estrogen Receptor/ERR  |  Reactive Oxygen Species

In Vitro: GSK5182 (0-20 μM; 0-hours; PLC/PRF/5 cells) treatment leads to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.
GSK5182 (0-20 μM; 24 hours; PLC/PRF/5 cells) treatment also causes a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of phosphorylated retinoblastoma protein (p-pRb).
GSK5182 (10-20 μM; PLC/PRF/5 cells) treatment induces cell cycle arrest at G1 phase, which in turn induces a corresponding dose-dependent reduction in the percentage of cells in S phase.

In Vivo: GSK5182 (40 mg/kg; intraperitoneal injection; every day; 25 or 30 days; db/db mice, diet-induced obesity mice) specifically inhibits the transcriptional activity of ERRγ, and suppresses hepatic glucose production through inhibition of hepatic gluconeogenesis. GSK5182 elicits anti-diabetic effects in mouse models via negative regulation of the hepatic gluconeogenesis program. GSK5182 normalizes hyperglycemia mainly through inhibition of hepatic glucose production.

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