ARN5187 trihydrochloride

Modify Date: 2024-01-16 08:38:40

ARN5187 trihydrochloride structure	Common Name	ARN5187 trihydrochloride
	CAS Number	1700693-96-4	Molecular Weight	506.91
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₂₄H₃₅Cl₃FN₃O	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of 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].

Name	4-({[1-(2-Fluorophenyl)cyclopentyl]amino}methyl)-2-[(4-methyl-1-piperazinyl)methyl]phenol trihydrochloride
Synonym	More Synonyms

Description	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].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> Autophagy >> Autophagy
Target	REV-ERBβ[1]
In Vitro	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]. Cell Cytotoxicity Assay[1] Cell Line: BT-474 cells Concentration: 0-100 µM Incubation Time: 48 h Result: Showed cytotoxicity with EC50 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.
References	[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.

Molecular Formula	C₂₄H₃₅Cl₃FN₃O
Molecular Weight	506.91
Exact Mass	505.182983

4-({[1-(2-Fluorophenyl)cyclopentyl]amino}methyl)-2-[(4-methyl-1-piperazinyl)methyl]phenol trihydrochloride

Phenol, 4-[[[1-(2-fluorophenyl)cyclopentyl]amino]methyl]-2-[(4-methyl-1-piperazinyl)methyl]-, hydrochloride (1:3)

ARN5187 trihydrochloride

Use of ARN5187 trihydrochloride

Names

ARN5187 trihydrochloride Biological Activity

Chemical & Physical Properties

Synonyms