GSK5182

• Catalog Number: ACM877387376
• Product Name: GSK5182
• CAS: 877387-37-6
• Category: Agonists
• Description: GSK5182 is a specific inverse agonist for estrogen-related receptor γ.
• Synonyms: GSK5182; GSK 5182; GSK-5182
• IUPAC Name: 4-[(Z)-1-[4-(2-dimethylaminoethoxy)phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
• Molecular Weight: 417.55
• Molecular Formula: C27H31NO3
• Canonical SMILES: OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(C3=CC=CC=C3)\CCCO)C=C1
• InChI: InChI=1S/C27H31NO3/c1-28(2)18-20-31-25-16-12-23(13-17-25)27(22-10-14-24(30)15-11-22)26(9-6-19-29)21-7-4-3-5-8-21/h3-5,7-8,10-17,29-30H,6,9,18-20H2,1-2H3/b27-26-
• InChI Key: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Alternative CAS: 877387-37-6 (free base); 1936468-29-9 (HCl)
• Biological Target: GSK5182 is a highly selective and orally active inverse agonist of estrogen-related receptor γ (ERRγ) with an IC50 of 79 nM.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 77.67; H, 7.48; N, 3.35; O, 11.49
• Exact Mass: 417.2304
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Consistent with the results from experiments involving endogenous knockdown of ERRγ, this study found that treatment with GSK5182 led to a significant and dose-dependent reduction in the number of proliferating PLC/PRF/5 cells (Figure 4b). GSK5182 also caused a dose-dependent increase in the expression of p21 and p27 while at the same time reducing the level of p-pRb (Figure 4c). The results obtained from flow cytometry revealed that GSK5182 induced cell cycle arrest at G1 phase, which in turn induced a corresponding dose-dependent reduction in the percentage of cells in S phase (Figure 4d). Taken together, these data indicate that the antitumor effect of GSK5182 in HCC cells is mediated by the induction of cell cycle arrest at the G1/S checkpoint.; Reference: Exp Mol Med. 2016 Mar 4;48(3):e213. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4892874/
• In Vivo Activity: Interestingly, GSK5182 treatment improved the liver toxicity caused by diabetes progression in db/db mice, and there were no signs of kidney, muscle, or heart toxicity (Table 2 for BUN, CRE, and CK levels). Furthermore, GSK5182 treatment significantly decreased food intake and body weight and reduced hepatic fat accumulation as well as gonadal and inguinal fat mass (Fig. 5C-F).; Reference: Diabetes. 2013 Sep;62(9):3093-102. https://pubmed.ncbi.nlm.nih.gov/23775767/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).