ARN5187 

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].

REV-ERBβ^[1]

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].

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

397.53

C₂₄H₃₂FN₃O

1287451-26-6

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]