ARN5187
Based on 1 publication(s) in Google Scholar
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.
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- CAS No.: 1287451-26-6
- Formule: C24H32FN3O
- Masse moléculaire:397.53
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) ARN5187
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Activité biologique
REV-ERBβ[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-474 | EC50 |
9.5 μM
Compound: 148
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Inhibition of autophagy in human BT-474 cells
Inhibition of autophagy in human BT-474 cells
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[PMID: 36283182] |
| BT-474 | IC50 |
10 μM
Compound: 1, ARN5187
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Lysosomotropic activity in human BT474 cells assessed as reduction in lysosomal pH incubated for 24 hrs by lysosomotropy assay
Lysosomotropic activity in human BT474 cells assessed as reduction in lysosomal pH incubated for 24 hrs by lysosomotropy assay
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[PMID: 26135471] |
| BT-474 | IC50 |
23.5 μM
Compound: 40; ARN5187
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Cytotoxicity against human BT474 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human BT474 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 29211480] |
| BT-474 | IC50 |
30.14 μM
Compound: 1, ARN5187
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Cytotoxicity against human BT474 cells assessed as reduction in cell number incubated for 72 hrs
Cytotoxicity against human BT474 cells assessed as reduction in cell number incubated for 72 hrs
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[PMID: 26135471] |
| HEK293 | IC50 |
17.5 μM
Compound: 1, ARN5187
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Inhibition of REV-ERBbeta (unknown origin) expressed in HEK293 cells incubated for 24 hrs assessed as inhibition of receptor-mediated transcriptional repression by REV-ERB luciferase reporter assay
Inhibition of REV-ERBbeta (unknown origin) expressed in HEK293 cells incubated for 24 hrs assessed as inhibition of receptor-mediated transcriptional repression by REV-ERB luciferase reporter assay
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[PMID: 26135471] |
| HMEC | IC50 |
>100 μM
Compound: 1, ARN5187
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Cytotoxicity against HMEC cells assessed as reduction in cell number incubated for 72 hrs
Cytotoxicity against HMEC cells assessed as reduction in cell number incubated for 72 hrs
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[PMID: 26135471] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT-474 cells
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Concentration:0-100 µM
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Incubation Time:48 h
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Result:Showed cytotoxicity with EC50 of 23.5 µM.
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Cell Line:BT-474 cells
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Concentration:25, 50 µM
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Incubation Time:
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Result:Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.
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Cell Line:BT-474 cells
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Concentration:50 µM
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Incubation Time:24 h
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Result:Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.
Chemical Information
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CAS No. 1287451-26-6
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Masse moléculaire 397.53
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Formule C24H32FN3O
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SMILES
OC1=CC=C(CNC2(C3=CC=CC=C3F)CCCC2)C=C1CN4CCN(C)CC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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J Clin Endocrinol Metab
2025 Mar 17;110(4):991-1002. PMID: 39359072
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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