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].

Product Specifications

CAS Number

[1700693-96-4]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; Autophagy; REV-ERB

Type

Reference compound

Related Pathways

Apoptosis; Autophagy; Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

COVID-19-immunoregulation

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/arn5187-trihydrochloride.html

Purity

99.54

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

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

Molecular Formula

C24H35Cl3FN3O

Molecular Weight

506.91

Precautions

H315, H319, H335

References & Citations

[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.