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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 Specifications 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
      Catalog 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.