ARN5187 trihydrochloride 是一种亲溶酶体REV-ERBβ配体，抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 trihydrochloride 显示出溶酶体效力和细胞毒性。ARN5187 trihydrochloride 诱导细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。

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 EC 50 of 23.5 μM in BT-474 cells and IC 50 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: BT-474 cells Concentration: 0-100 μM Incubation Time: 48 h Result: Showed cytotoxicity with EC 50 of 23.5 μM. Western Blot Analysis [1] Cell Line: BT-474 cells Concentration: 50 μM Incubation Time: 24 h Result: Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP. RT-PCR [1] Cell Line: BT-474 cells Concentration: 25, 50 μM Incubation Time: Result: Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.

1700693-96-4

C24H35Cl3FN3O

506.91

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years