506190 p97 ATPase Activity Inhibitor, DBeQ - Calbiochem

506190
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₂H₂₀N₄

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      506190-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable quinazolinamine compound that inhibits the AAA (ATPase associated with diverse cellular activities) ATPase p97 (IC50 = 1.6 µM against WT or C522A p97) in a reversible and ATP-competitive (Ki = 3.2 µM) manner, while being at least 50-fold less potent against AAA ATPase NSF (N-methylmaleimide-sensitive factor) or the ATP-dependent chymotrypsin-like activity of proteasome 20S, and exhibiting no significant activity against a panel of ~170 kinases. Shown to effectively suppress p97-dependent cellular processes, including ERAD (ER-associated degradation) reporter TCRα-GFP degradation (92.59% vs. 33.33% degradation in 2 h, respectively, with DMSO or 10 µM DBeQ in HEK293 cultures), autophagic degradation of LC3-II (LC3-II/LC3-I = 0.04 vs. 1.0, respectively, after 3 h DMSO or 10 µM DBeQ treatment in HeLa cultures), UFD (ubiquitin fusion degradation) pathway-mediated UbG76V-GFP reporter degradation (IC50 = 2.3 µM in HeLa cells), but not the degradation of p97-independent proteasome substrates ODC (ornithine decarboxylase) and ODD (oxygen-dependent degradation domain of HIF-1α) luciferase fusion reporters (IC50 = 45 and 56 µM, respectively, in HeLa cells). Also demonstrated to display selective antiproliferative activity against RPMI8226, HeLa, and HEK293 over non-cancerous human fetal lung fibroblasts MRC5 (GI50 = 1.2, 3.1, 4.0, and 6.6 µM, respectively) by inducing cellular DEVD-like (caspase-3/7), but not VEID-like (caspase-6), activity (by 4- to 6-fold in 4 h in HeLa cells) via a yet unknown mechanism.
          Catalogue Number506190
          Brand Family Calbiochem®
          SynonymsCID676352, CID16472035, N²,N⁴-Dibenzylquinazolinine-2,4-diamine, KUC105555N, ERAD Inhibitor I, p97 Inhibitor I, Valosin-containing Protein Inhibitor I, VCP Inhibitor I
          References
          ReferencesChou, T.F., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 4834.
          Product Information
          FormWhite solid
          Hill FormulaC₂₂H₂₀N₄
          Chemical formulaC₂₂H₂₀N₄
          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
          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
          506190

          References

          Reference overview
          Chou, T.F., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 4834.
          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.

          Revision08-December-2011 RFH
          SynonymsCID676352, CID16472035, N²,N⁴-Dibenzylquinazolinine-2,4-diamine, KUC105555N, ERAD Inhibitor I, p97 Inhibitor I, Valosin-containing Protein Inhibitor I, VCP Inhibitor I
          DescriptionA cell-permeable quinazolinamine compound that inhibits the AAA (ATPase associated with diverse cellular activities) ATPase p97 (IC50 = 1.6 µM against WT or C522A p97) in a reversible and ATP-competitive (Ki = 3.2 µM) manner, while being at least 50-fold less potent against AAA ATPase NSF (N-methylmaleimide-sensitive factor) or the ATP-dependent chymotrypsin-like activity of proteasome 20S, and exhibiting no significant activity against a panel of ~170 kinases. Shown to effectively suppress p97-dependent cellular processes, including ERAD (ER-associated degradation) reporter TCRα-GFP degradation (92.59% vs. 33.33% degradation in 2 h, respectively, with DMSO or 10 µM DBeQ in HEK293 cultures), autophagic degradation of LC3-II (LC3-II/LC3-I = 0.04 vs. 1.0, respectively, after 3 h DMSO or 10 µM DBeQ treatment in HeLa cultures), UFD (ubiquitin fusion degradation) pathway-mediated UbG76V-GFP reporter degradation (IC50 = 2.3 µM in HeLa cells), but not the degradation of p97-independent proteasome substrates ODC (ornithine decarboxylase) and ODD (oxygen-dependent degradation domain of HIF-1α) luciferase fusion reporters (IC50 = 45 and 56 µM, respectively, in HeLa cells). Also demonstrated to display selective antiproliferative activity against RPMI8226, HeLa, and HEK293 over non-cancerous human fetal lung fibroblasts MRC5 (GI50 = 1.2, 3.1, 4.0, and 6.6 µM, respectively) by inducing cellular DEVD-like (caspase-3/7), but not VEID-like (caspase-6), activity (by 4- to 6-fold in 4 h in HeLa cells) via a yet unknown mechanism.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₂H₂₀N₄
          Structure formulaStructure formula
          Purity≥95% by HPLC
          SolubilityDMSO (50 mg/ml) or Ethanol (2.5 mg/ml)
          Storage -20°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 6 months at -20°C.
          Toxicity Regulatory Review
          ReferencesChou, T.F., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 4834.