| Bioactivity | 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]. | |||||||||
| Target | EC50: 50 nM (LXRα); 40 nM (LXRβ) | |||||||||
| Invitro | 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: | |||||||||
| Name | GSK3987 | |||||||||
| CAS | 264206-85-1 | |||||||||
| Formula | C24H20N2O3 | |||||||||
| Molar Mass | 384.43 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. HepG2 cells, ABCA1, SREBP-1c, cellular cholesterol, macrophages, triglyceride accumulation |