产品
编 号:F203557
分子式:C24H35Cl3FN3O
分子量:506.91
产品类型
结构图
CAS No: 1700693-96-4
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产品详情
生物活性:
ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.
体外研究:
ARN5187 trihydrochloride (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 trihydrochloride (0-100 μM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells.ARN5187 trihydrochloride (25, 50 μM) is a lysosomotropic-independent REV-ERB antagonistic activity.ARN5187 trihydrochloride (50 μM; 24 h) shows autophagy inhibition.ARN5187 trihydrochloride (50 μM; 2, 8, 24 h) effects autophagy formation and maturation.