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530352 CD40-TRAF6 Signaling Inhibitor, 6877002 - Calbiochem

530352
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₇NO

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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
      Quality LevelMQ100
      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.