662140 DUB Inhibitor IV, b-AP15 - CAS 1009817-63-4 - Calbiochem

662140
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₁₇N₃O₆ 1009817-63-4

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      662140-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo.
          Catalogue Number662140
          Brand Family Calbiochem®
          SynonymsUSP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II, NSC687852, 3,5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one
          References
          ReferencesD'Arcy, P., et al. 2011. Nat. Med. 17, 1636.
          Product Information
          CAS number1009817-63-4
          FormYellow powder
          Hill FormulaC₂₂H₁₇N₃O₆
          Chemical formulaC₂₂H₁₇N₃O₆
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥97% 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 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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          DUB Inhibitor IV, b-AP15 - CAS 1009817-63-4 - Calbiochem Certificates of Analysis

          TitleLot Number
          662140

          References

          Reference overview
          D'Arcy, P., et al. 2011. Nat. Med. 17, 1636.
          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.

          Revision09-December-2013 JSW
          SynonymsUSP14 Inhibitor III, UCH-L5/UCH37 Inhibitor II, NSC687852, 3,5-bis((4-Nitrophenyl)methylidene)-1-prop-2-enoylpiperidin-4-one, (3E,5E)-1-Acryloyl-3,5-bis(4-nitrobenzylidene)piperidin-4-one
          DescriptionA cell-permeable bis-nitrobenzylidene-piperidinone that inhibits 19S deubiquitinase (DUB) activity (IC50 = 2.1 µM against Ub-AMC hydrolysis) in a reversible manner by directly targeting UCH37/UCH-L5 and USP14, while exhibiting little or no activity toward BAP1, UCH-L1, UCH-L3, USP2, USP7, USP8 (IC50 >100 µM), or POH1/PRN11. Dual UCH37 and USP14 inhibition by a-AP15 results in increased bulk cellular protein ubiquitination level and a blockage of protein proteasomal degradation (Effective conc. ≥770 nM in HCT-116 cells), exactly opposite to the effects seen with USP14 inhibition alone by IU1 (Cat. No. 662210). Effectively suppresses the growth of various tumors in mice (2.5 to 5 mg/kg, i.p. or s.c.) in vivo.
          FormYellow powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1009817-63-4
          Chemical formulaC₂₂H₁₇N₃O₆
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml; clear, yellow solution)
          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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesD'Arcy, P., et al. 2011. Nat. Med. 17, 1636.