For research use only. Not for therapeutic Use.
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].
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].
Catalog Number | I011912 |
CAS Number | 264206-85-1 |
Synonyms | 1-benzyl-3-(4-methoxyanilino)-4-phenylpyrrole-2,5-dione |
Molecular Formula | C24H20N2O3 |
Purity | ≥95% |
InChI | InChI=1S/C24H20N2O3/c1-29-20-14-12-19(13-15-20)25-22-21(18-10-6-3-7-11-18)23(27)26(24(22)28)16-17-8-4-2-5-9-17/h2-15,25H,16H2,1H3 |
InChIKey | HLZMYWLMBBLASX-UHFFFAOYSA-N |
SMILES | COC1=CC=C(C=C1)NC2=C(C(=O)N(C2=O)CC3=CC=CC=C3)C4=CC=CC=C4 |
Reference | [1]. HepG2 cells, ABCA1, SREBP-1c, cellular cholesterol, macrophages, triglyceride accumulation |