Bioactivity | 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[1][2]. |
Invitro | 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[1][2].ARN5187 trihydrochloride (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells[1].ARN5187 trihydrochloride (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity[1].ARN5187 trihydrochloride (50 µM; 24 h) shows autophagy inhibition[1].ARN5187 trihydrochloride (50 µM; 2, 8, 24 h) effects autophagy formation and maturation[1]. Cell Cytotoxicity Assay[1] Cell Line: |
Name | ARN5187 trihydrochloride |
CAS | 1700693-96-4 |
Formula | C24H35Cl3FN3O |
Molar Mass | 506.91 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |