| Bioactivity | 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[1][2]. |
| Invitro | 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[1][2].ARN5187 (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells[1].ARN5187 (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity[1].ARN5187 (50 µM; 24 h) shows autophagy inhibition[1].ARN5187 (50 µM; 2, 8, 24 h) effects autophagy formation and maturation[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| Name | ARN5187 |
| CAS | 1287451-26-6 |
| Formula | C24H32FN3O |
| Molar Mass | 397.53 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |