产品
编 号:F743804
分子式:C24H32FN3O
分子量:397.53
产品类型
结构图
CAS No: 1287451-26-6
联系客服
产品详情
生物活性:
ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis.
体外研究:
ARN5187 (compound 1) (0-100 μM; 48 h) shows cytotoxicity with EC50 of 23.5 μM in BT-474 cells and IC50 of 30.14 μM, >100 μM for BT-474 and HMEC cells, respectively.ARN5187 (0-100 μM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells.ARN5187 (25, 50 μM) is a lysosomotropic-independent REV-ERB antagonistic activity.ARN5187 (50 μM; 24 h) shows autophagy inhibition.ARN5187 (50 μM; 2, 8, 24 h) effects autophagy formation and maturation.