480073 | MLKL Inhibitor, Necrosulfonamide - CAS 432531-71-0 - Calbiochem

480073
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      Overview

      Replacement Information

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      480073-25MG
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable acrylamide compound that inhibits human, but not murine, MLKL adaptor function via covalent modification of Cys86 and is more potent than Nec-1 (Cat. No. 480065) in preventing necrotic/necroptotic death in human HT-29 (IC50 = 124 nM and 2 µM, respectively), being ineffective against necrosis/necroptosis in murine L929 or apoptosis in human RIP3-null Panc-1 cells. Unlike Nec-1, which prevents necrosome formation by blocking RIP1-RIP3 interaction, MLKL prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with further downstream effectors.
          Catalogue Number480073
          Brand Family Calbiochem®
          SynonymsNecrosis Inhibitor III, Mixed Lineage Kinase Domain-Like Protein Inhibitor, Necrosome Inhibitor II, Necrosulfonamide, (E)-N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide
          References
          ReferencesDunai, Z.A., et al. 2012. PLoS One 7, e41945.
          Sun, L., et al. 2012. Cell 148, 213.
          Product Information
          CAS number432531-71-0
          FormDark yellow solid
          Hill FormulaC₁₈H₁₅N₅O₆S₂
          Chemical formulaC₁₈H₁₅N₅O₆S₂
          ReversibleN
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Primary Targethuman MLKL
          Purity≥95% 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 +2°C to +8°C
          Protect from Light Protect from light
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks 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
          480073

          References

          Reference overview
          Dunai, Z.A., et al. 2012. PLoS One 7, e41945.
          Sun, L., et al. 2012. Cell 148, 213.
          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.

          Revision12-April-2013 JSW
          SynonymsNecrosis Inhibitor III, Mixed Lineage Kinase Domain-Like Protein Inhibitor, Necrosome Inhibitor II, Necrosulfonamide, (E)-N-(4-(N-(3-Methoxypyrazin-2-yl)sulfamoyl)phenyl)-3-(5-nitrothiophene-2-yl)acrylamide
          DescriptionA cell-permeable acrylamide compound that inhibits human, but not murine, MLKL adaptor function via covalent modification of Cys86 through Michael addition and is more potent than the RIP1 inhibitor Nec-1 (Cat. No. 480065) in preventing necrotic/necroptotic death in human HT-29 (IC50 = 124 nM and 2 µM with respective drug against 20 ng/mL TNF-&alpha/100 nM Smac mimetic/20 µM Z-VAD-induced death) and FADD-null Jurkat cultures (80% protection against 200 ng/mL TNF-&alpha-induced death by 0.5 µM NSA or 10 µM Nec-1), being ineffective against blocking necrosis/necroptosis in murine L929 or apoptosis in human RIP3-null Panc-1 cells even at concentrations as high as 5 µM. Unlike Nec-1, which prevents necrosome formation by blocking RIP1-RIP3 interaction, MLKL prevents the MLKL-RIP1-RIP3 necrosome complex from interacting with further downstream effectors.
          FormDark yellow solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number432531-71-0
          Chemical formulaC₁₈H₁₅N₅O₆S₂
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 weeks at -20°C.
          Toxicity Standard Handling
          ReferencesDunai, Z.A., et al. 2012. PLoS One 7, e41945.
          Sun, L., et al. 2012. Cell 148, 213.