GSK5182

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

GSK5182 

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。

GSK5182

GSK5182 Chemical Structure

CAS No. : 877387-37-6

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生物活性

GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 does not interact with other nuclear receptors, including ERRα or ERα. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma (HCC)[1][2][3].

IC50 & Target

ERRγ

79 nM (IC50)

Reactive Oxygen Species

 

体外研究
(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[1].
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)[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 0 hour, 24 hours, 48 hours, 72 hours
Result: Led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells.

Western Blot Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 0 μM, 10 μM, 20 μM
Incubation Time: 24 hours
Result: Caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb.

Cell Cycle Analysis[1]

Cell Line: The human hepatoma cell line PLC/PRF/5
Concentration: 10 μM, 20 μM
Incubation Time:
Result: Induced cell cycle arrest.

体内研究
(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[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: db/db mice (male, 7-12-week-old), diet-induced obesity (DIO) mice[3]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; every day; 30 days for db/db mice, 25 days for DIO mice
Result: Inhibited the transcriptional activity of ERRγ, suppressed hepatic glucose production through inhibition of hepatic gluconeogenesis.

分子量

417.54

Formula

C27H31NO3
CAS 号

877387-37-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kim JH, et al. Estrogen-related receptor γ is upregulated in liver cancer and its inhibition suppresses livercancer cell proliferation via induction of p21 and p27. Exp Mol Med. 2016 Mar 4;48:e213.

    [2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272.

    [3]. Kim DK, et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes. 2013 Sep;62(9):3093-102.

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