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

475964
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₇H₂₅ClN₄O₂, HCl

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475964-10MG
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          Glass bottle 10 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.