ARN5187 trihydrochloride 

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].

REV-ERBβ^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

506.91

C₂₄H₃₅Cl₃FN₃O

1700693-96-4

OC1=CC=C(CNC2(C3=CC=CC=C3F)CCCC2)C=C1CN4CCN(C)CC4.Cl[H].Cl[H].Cl[H]

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]