530352 CD40-TRAF6 Signaling Inhibitor, 6877002 - Calbiochem

530352
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₁₇NO

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30352.0001
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          Glass bottle 25 mg
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          Description
          OverviewA cell-permeable, bioavailable propenone compound that specifically targets TNF receptor-associated factor 6 (TRAF6; Kd = 97 µM for TRAF6 C-domain) and disrupts its functional coupling with CD40. A six-week treatment of C57BL/6 mice fed high fat diet (HFD) with this compound show significant improvement in insulin sensitivity and hepatosteatosis without affecting HFD-induced weight gain. Also reported to reduce gonadal adipose tissue inflammation and diminish the number of CD11b+F4/80+CD11c+ M1 macrophages. Inhibits NF-κB activation in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells (IC50 15.9 µM) and reduce IL-1β and IL-6 expression in anti-CD40 antibody FGK45-stimulated primary bone marrow-derived macrophages.
          Catalogue Number530352
          Brand Family Calbiochem®
          Synonyms3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one, (2E)-3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one
          References
          ReferencesChatzigeorgiou, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2686.
          Product Information
          FormYellow powder
          Hill FormulaC₁₇H₁₇NO
          Chemical formulaC₁₇H₁₇NO
          Applications
          Biological Information
          Primary TargetTRAF6
          Purity≥95% by NMR
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          CD40-TRAF6 Signaling Inhibitor, 6877002 - Calbiochem SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Chatzigeorgiou, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2686.
          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.

          Revision30-May-2014 JSW
          Synonyms3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one, (2E)-3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one
          DescriptionA cell-permeable propenone compound that disrupts TNF receptor-associated factor 6 (TRAF6) and CD40 coupling by targeting TRAF6 via direct affinity interaction (Kd = 97 µM), effectively inhibiting LPS-induced NF-κB activation in murine macrophage RAW264.7 (IC50 15.9 µM; drug treatment starts 1 h prior to 2 h CD40 expression induction by LPS) as well as anti-CD40 antibody FGK45-stimulated IL-1β expression (IC50 < 10 µM; drug treatment starts 1 h prior to 6 h antibody stimulation). Daily intraperitoneal injection in vivo (10 µmol/kg/d = 2.513 mg/kg/d) during the last 6 weeks of a 12-week murine high fat diet-induce obesity (DIO) study is reported to improve insulin sensitivity, reduce hepatosteatosis, and prevent obesity-related inflammation in fat tissue (AT), as evidenced by a 40% less CD11b+F4/80+CD11c+ M1 macrophages in the stromal vascular fraction (SVF) of gonadal AT (gonAT) than the control DIO mice. Genetic studies likewise reveal that disruption of TRAF6-mediated CD40 signaling ameliorates obesity related complications, while CD40 knockout or deficit in TRAF2/3/5-CD40 interaction exacerbates metabolic complications in DIO mice.
          FormYellow powder
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₁₇H₁₇NO
          Purity≥95% by NMR
          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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesChatzigeorgiou, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2686.