2699724-40-6
Chemical Structure
(E/Z)-GSK5182
- CAS No.: 2699724-40-6
- Formula:C27H31NO3
- Molecular Weight:417.54
IUPAC Name: (Z)-4-(1-(4-(2-(dimethylamino)ethoxy)phenyl)-5-hydroxy-2-phenylpent-1-en-1-yl)phenol
InChIKey: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
SMILES: OCCC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)OCCN(C)C)\C3=CC=C(C=C3)O
Biological Activity: (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM[1]. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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(E/Z)-GSK5182 | 98.90% | (E/Z)-GSK5182 is a racemic compound of (E)-GSK5182 and (Z)-GSK5182 isomers. GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM. GSK5182 also induces reactive oxyen species (ROS) generation in hepatocellular carcinoma. | ||||||||||||||||||||
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- [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. [Content Brief]
- [2]. Misra J, et al. ERRγ: a Junior Orphan with a Senior Role in Metabolism. Trends Endocrinol Metab. 2017 Apr;28(4):261-272. [Content Brief]
- [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. [Content Brief]
Keywords
