For research use only. Not for therapeutic Use.
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].
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].
| Catalog Number | I002775 |
| CAS Number | 1700693-96-4 |
| Synonyms | 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methylpiperazin-1-yl)methyl]phenol;trihydrochloride |
| Molecular Formula | C24H35Cl3FN3O |
| Purity | ≥95% |
| InChI | InChI=1S/C24H32FN3O.3ClH/c1-27-12-14-28(15-13-27)18-20-16-19(8-9-23(20)29)17-26-24(10-4-5-11-24)21-6-2-3-7-22(21)25;;;/h2-3,6-9,16,26,29H,4-5,10-15,17-18H2,1H3;3*1H |
| InChIKey | DCJGIMILIULIAL-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)CC2=C(C=CC(=C2)CNC3(CCCC3)C4=CC=CC=C4F)O.Cl.Cl.Cl |
| Reference | [1]. De Mei C, et al. Dual inhibition of REV-ERBβ and autophagy as a novel pharmacological approach to induce cytotoxicity in cancer cells. Oncogene. 2015 May 14;34(20):2597-608. [2]. Torrente E, et al. Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. J Med Chem. 2015 Aug 13;58(15):5900-15. |
