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Art. -Nr.: HY-103691

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ARN5187

Name: ARN5187
Brand: MedChemExpress
SKU: HY-103691
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1 Cited Publications

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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. Nr.: 1287451-26-6
Formel: C₂₄H₃₂FN₃O
Molecular Weight:397.53

Speicherung:

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

Data Sheet (272 KB)

ARN5187 Chemical Structure

CAS. Nr.: 1287451-26-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
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Biologische Aktivität

Beschreibung

IC₅₀ & Target

REV-ERBβ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
BT-474	EC₅₀	9.5 μM Compound: 148	Inhibition of autophagy in human BT-474 cells Inhibition of autophagy in human BT-474 cells	[PMID: 36283182]
BT-474	IC₅₀	10 μM Compound: 1, ARN5187	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	[PMID: 26135471]
BT-474	IC₅₀	23.5 μM Compound: 40; ARN5187	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	[PMID: 29211480]
BT-474	IC₅₀	30.14 μM Compound: 1, ARN5187	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	[PMID: 26135471]
HEK293	IC₅₀	17.5 μM Compound: 1, ARN5187	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	[PMID: 26135471]
HMEC	IC₅₀	>100 μM Compound: 1, ARN5187	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	[PMID: 26135471]

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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 1287451-26-6
Molecular Weight 397.53
Formel C₂₄H₃₂FN₃O
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Publications (1)

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Journal Impact Factor

J Clin Endocrinol Metab

Overexpression of NR1D1 Portends Disease Recurrence in Thyroid Cancer. [Abstract]

2025 Mar 17;110(4):991-1002. PMID: 39359072

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Keywords

ARN5187

1 Cited Publications

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Biologische Aktivität
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- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (1)
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ARN5187

Publications Citing Use of MedChemExpress (MCE) ARN5187

Biologische Aktivität

Chemical Information

Publications (1)

Reinheit & Dokumentation

Verweise

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ARN5187 Related Classifications

HY-103691 Related Classifications

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