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530352 CD40-TRAF6 Signaling Inhibitor, 6877002 - CAS 433249-94-6 - Calbiochem

A cell-permeable compound that specifically targets TRAF6 (Kd = 97 µM for TRAF6 C-domain) and disrupts its functional coupling with CD40.

Ficha de datos de seguridad (MSDS o SDS), certificado de análisis y de calidad (CoA y CoQ), expedientes, folletos y otros documentos disponibles.

Sinónimos: 3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one, (2E)-3-((2,5-Dimethylphenyl)amino)-1-phenyl-2-propen-1-one

Primary Target: TRAF6
530352
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Descripción

Replacement Information

Tabla espec. clave

CAS #Empirical Formula
433249-94-6C₁₇H₁₇NO

Products

Número de referenciaEmbalaje Cant./Env.
5303520001 Frasco de vidrio 25 mg
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
CAS number433249-94-6
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
Global Trade Item Number
Número de referencia GTIN
5303520001 04055977260748

Documentation

CD40-TRAF6 Signaling Inhibitor, 6877002 - CAS 433249-94-6 - Calbiochem Ficha datos de seguridad (MSDS)

Título

Ficha técnica de seguridad del material (MSDS) 

Referencias bibliográficas

Visión general referencias
Chatzigeorgiou, A., et al. 2014. Proc. Natl. Acad. Sci. USA 111, 2686.
Ficha técnica

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
CAS number433249-94-6
Chemical formulaC₁₇H₁₇NO
Purity≥95% by NMR
SolubilityDMSO (100 mg/ml). Use only fresh DMSO for reconstitution.
Storage Protect from light
+2°C to +8°C
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.