1700693-96-4
1700693-96-4 structure
- Name: ARN5187 trihydrochloride
- Chemical Name: 4-({[1-(2-Fluorophenyl)cyclopentyl]amino}methyl)-2-[(4-methyl-1-piperazinyl)methyl]phenol trihydrochloride
- CAS Number: 1700693-96-4
- Molecular Formula: C24H35Cl3FN3O
- Molecular Weight: 506.91
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2018-07-07 14:02:03
- Modify Date: 2024-01-16 08:38:40
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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 |
|---|---|
| Synonyms |
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) |
| 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 | |
| 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 |
| Molecular Formula | C24H35Cl3FN3O |
|---|---|
| Molecular Weight | 506.91 |
| Exact Mass | 505.182983 |