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538355 ARN5187 - Calbiochem

A cell-potent dual inhibitor of REV-ERBβ and autophagy. Relieves REV-ERB-mediated transcriptional repression and elicits stronger apoptotic induction in cancer cells.

ARN5187 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-(((1-(2-Fluorophenyl)cyclopentyl)-amino)methyl)-2-((4-methylpiperazin-1-yl)methyl)phenol, 3HCl

Primary Target: REV-ERBβ
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₄H₃₂FN₃O • 3HCl
Description
OverviewA cell-permeable piperazinylmethylphenol compound that exhibits dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. Shown to directly interact with the LBD of REV-ERBβ, activate the RevRE reporter (EC50 = 15.0 µM for REV-ERβ) and dose-dependently enhance BMAL1, PER1 and PEPCK expression. Disrupts lysosomal function, blocks autophagy at a late stage, and reduces cancer cell viability (EC50 = 23.5, 14.4 & 29.8 µM in BT-474, HEP-G2 & LNCaP cells, respectively). Elicits stronger apoptotic induction and significantly more cytotoxic than chloroquine.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Catalogue Number538355
Brand Family Calbiochem®
Synonyms4-(((1-(2-Fluorophenyl)cyclopentyl)-amino)methyl)-2-((4-methylpiperazin-1-yl)methyl)phenol, 3HCl
DescriptionARN5187
References
ReferencesDe Mei, C., et al. 2015. Oncogene. 34, 2597.
Product Information
FormOff-white solid
Hill FormulaC₂₄H₃₂FN₃O • 3HCl
Hygroscopic Hygroscopic
Quality LevelMQ100
Applications
Biological Information
Primary TargetREV-ERBβ
Purity≥98% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
538355 0

Documentation

ARN5187 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
De Mei, C., et al. 2015. Oncogene. 34, 2597.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision19-November-2016 JSW
Synonyms4-(((1-(2-Fluorophenyl)cyclopentyl)-amino)methyl)-2-((4-methylpiperazin-1-yl)methyl)phenol, 3HCl
DescriptionA cell-permeable piperazinylmethylphenol compound that exhibits dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. Shown to directly interact with the LBD of REV-ERBβ, activate the RevRE reporter (EC50 = 15.0 µM for REV-ERβ) and dose-dependently enhance BMAL1, PER1 and PEPCK expression. Disrupts lysosomal function, blocks autophagy at a late stage, and reduces cancer cell viability (EC50 = 23.5, 14.4 & 29.8 µM in BT-474, HEP-G2 & LNCaP cells, respectively). Elicits stronger apoptotic induction and significantly more cytotoxic than chloroquine.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
Purity≥98% by HPLC
SolubilityH₂O (50 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Standard Handling
ReferencesDe Mei, C., et al. 2015. Oncogene. 34, 2597.