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
538355
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₄H₃₂FN₃O • 3HCl

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.38355.0001
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          		 Glass bottle 10 mg
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          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

          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 -20°C
          Hygroscopic
          Protect from light
          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.