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475964 MK-2 Inhibitor IV, MK-25 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₂₇H₂₅ClN₄O₂, HCl

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475964-10MG
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      Description
      OverviewA cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC50 = 110 nM; EC50 = 350 nM for pHSP27 in IL-1β-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µM against human CK2, Haspin, Arg and CK1γ3 = 40, 40, 42 and > 70, respectively). Shown to efficiently suppress the secretions of TNFα, IL6 (IC50 = 4.4 and 5.2 µM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50 = 5.7 and 2.2 µM in IL1β-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50 > 20 µM for 3A4, 2D6 and 2C9).
      Catalogue Number475964
      Brand Family Calbiochem®
      Synonyms5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
      References
      ReferencesHuang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.
      Product Information
      FormBeige solid
      Hill FormulaC₂₇H₂₅ClN₄O₂, HCl
      Chemical formulaC₂₇H₂₅ClN₄O₂, HCl
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      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 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      MK-2 Inhibitor IV, MK-25 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      MK-2 Inhibitor IV, MK-25 - Calbiochem Certificates of Analysis

      TitleLot Number
      475964

      References

      Reference overview
      Huang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.
      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.

      Revision28-September-2012 JSW
      Synonyms5-(4-Chlorophenyl)-N-(4-(piperazin-1-yl)phenyl)-N-(pyridin-2-ylmethyl)furan-2-carboxamide, HCl, MAPKAP-K2 Inhibitor IV, MK-25
      DescriptionA cell-permeable furanylcarboxamide compound that acts as a potent, reversible and non-ATP-competitive inhibitor of MK-2/MAPKAP-K2 activity (IC50 = 110 nM; EC50 = 350 nM for pHSP27 in IL-1β-stimulated SW1353 cells) with excellent selectivity over 150 kinases (% activity inhibition at 10 µM against human CK2, Haspin, Arg and CK1γ3 = 40, 40, 42 and > 70, respectively). Shown to efficiently suppress the secretions of TNFα, IL6 (IC50 = 4.4 and 5.2 µM in LPS-stimulated THP1 cell, respectively) and MMP-13 (IC50 = 5.7 and 2.2 µM in IL1β-stimulated SW1353 and in primary osteoarthritis-derived chondrocytes, respectively). Exhibits desirable bioavailability and weakly inhibits a panel of cytochrome P450 isozymes (IC50 > 20 µM for 3A4, 2D6 and 2C9).
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₇H₂₅ClN₄O₂, HCl
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (25 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 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesHuang, X., et al. 2011. ACS Med. Chem. Lett. 2, 632.