264206-85-1

264206-85-1 structure

Name: GSK3987
Chemical Name: GSK3987
CAS Number: 264206-85-1
Molecular Formula: C₂₄H₂₀N₂O₃
Molecular Weight: 384.427
Catalog: Signaling Pathways Metabolic Enzyme/Protease LXR
Create Date: 2021-08-23 09:10:47
Modify Date: 2025-08-25 16:24:21
GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation[1].

Name	GSK3987
Synonyms	1-Benzyl-3-[(4-methoxyphenyl)amino]-4-phenyl-1H-pyrrole-2,5-dione 1-BENZYL-3-(4-METHOXYPHENYLAMINO)-4-PHENYLPYRROLE-2,5-DIONE 1H-Pyrrole-2,5-dione, 3-[(4-methoxyphenyl)amino]-4-phenyl-1-(phenylmethyl)-

Description	GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation[1].
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> LXR Research Areas >> Metabolic Disease
Target	EC50: 50 nM (LXRα); 40 nM (LXRβ)[1]
In Vitro	GSK3987 (compound 4) shows activity with EC50s of 0.08 µM, 50 nM, 40 nM for ABCA1, LXRα-SRC1, LXRβ-SRC1, respectively[1]. GSK3987 (30, 100, 300, 1000 nM) increases the expression of ABCA1 and induces cellular cholesterol efflux to apoA1 particles in a dose-dependent manner in primary human macrophages[1]. GSK3987 (6-1500 nM) increases the expression of SREBP-1c and induces triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner[1]. RT-PCR[1] Cell Line: HepG2 cells Concentration: 6-1500 nM Incubation Time: Result: Increased the expression of SREBP-1c and induced triglyceride accumulation in human hepatoma (HepG2) cells in a dose-dependent manner.
References	[1]. HepG2 cells, ABCA1, SREBP-1c, cellular cholesterol, macrophages, triglyceride accumulation