1. Autophagy
    Apoptosis
  2. Autophagy
    Apoptosis
  3. ARN5187

ARN5187 

Cat. No.: HY-103691
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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.

For research use only. We do not sell to patients.

ARN5187 Chemical Structure

ARN5187 Chemical Structure

CAS No. : 1287451-26-6

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Description

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].

IC50 & Target

REV-ERBβ[1]

In Vitro

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.

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.

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.

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.
Molecular Weight

397.53

Formula

C24H32FN3O

CAS No.
SMILES

OC1=CC=C(CNC2(C3=CC=CC=C3F)CCCC2)C=C1CN4CCN(C)CC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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ARN5187
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HY-103691
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