ARN5187

Cat. No.: HY-103691: FAQs
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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

CAS No. : 1287451-26-6

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Other Forms of ARN5187:

ARN5187 trihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

REV-ERBβ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
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.

Molecular Weight

397.53

Formula

C₂₄H₃₂FN₃O

CAS No.

1287451-26-6

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.

Purity & Documentation

Handling Instructions (2659 KB)

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. [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]

ARN5187 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARN51871287451-26-6ARN 5187ARN-5187AutophagyApoptosisapoptosisBT-474 cellslysosomotropicchloroquineanticancerα-p62HEK-293 cellsInhibitorinhibitorinhibit

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