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    NSC697923
    NSC697923

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1317
    CAS #: 343351-67-7Purity ≥98%

    Description: NSC697923 (NSC 697923; NSC-697923) is a potent, cell-permeable and selective inhibitor of the Ub-conjugating enzyme E2 (UBE2) complex Ubc13-Uev1A with potential anticancer activity. NSC697923 can inhibit proliferation and survival of diffuse large B-cell lymphoma cells (DLBCL). Importantly, NSC697923 is able to induce apoptosis. It can also induce nuclear accumulation of p53, which led to its increased transcriptional activity and tumor suppressor function.NSC697923 blocks the formation of the Ubc13-Uev1A by inhibiting the formation of the Ubc13_Ub conjugate while it is a key component for DLBCL grown. In the long term, the cell cannot survive without Ubc13 expression. In conclusion, compound NSC697923 is an efficient inhibitor of DLBAL survival.  

    References: Blood. 2012 Aug 23;120(8):1668-77; Cell Death Dis. 2014 Feb 20;5:e1079.

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    Molecular Weight (MW)267.26
    FormulaC11H9NO5S
    CAS No.343351-67-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (198.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeO=[N+](C1=CC=C(S(=O)(C2=CC=C(C)C=C2)=O)O1)[O-]
    SynonymsNSC 697923; NSC-697923; NSC697923


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    In Vitro

    In vitro activity: NSC697923 selectively inhibits PMA-induced NF-κB activation, and also inhibits IκBα phosphorylation by both RANKL and LPS. NSC697923 impedes the formation of the Ubc13 and ubiquitin thioester conjugate and suppresses constitutive NF-κB activity in ABC-DLBCL cells. In addition, NSC697923 inhibits the proliferation and survival of ABC-DLBCL cells and GCB-DLBCL cells, and also induces apoptosis of primary DLBCL cells. In neuroblastoma (NB) cell lines, NSC697923 shows cytotoxic effect, and inhibits both anchorage-dependent and -independent colony formation


    Kinase Assay: The reactions are carried out at 37°C for 40 minutes in a buffer containing 50mM Tris-HCl, pH 7.5, 5mM MgCl2, 200μM ATP, 120μM Ub (U-100H), and 0.1μM E1 (E-304). For Ubc13-mediated Ub chain synthesis, the reaction mixture includes 0.2 μM Ubc13 (E2-600) and 0.2 mM Uev1A (E2-662) with or without GST-TRAF6. For UbcH5c-catalyzed ubiquitination, UbcH5c (E2-627) instead of Ubc13 and Uev1A is used in the reaction. Compound NSC697923 is added into the reaction mixtures at the indicated concentrations. The reactions are terminated with an equal volume of SDS-PAGE sample buffer and the products are analyzed by Western blotting with a Ub-specific antibody. For detecting the E2-Ub (Ubc13∼Ub or UbcH5c∼Ub) thioester conjugates, the reactions are carried out as described in “In vitro ubiquitination assay” without GST-TRAF6. The reactions are terminated by the addition of the SDS-PAGE sample buffer without a reducing agent unless specified. The products are analyzed by Western blotting with an anti-Ubc13 or anti-UbcH5c antibody.   


    Cell Assay: Cell viability is measured by trypan blue exclusion assay.

    In VivoNSC697923 (5 mg/kg/day, i.p.) demonstrates potent antitumor efficacy in both NB SH-SY5Y and NGP xenografts. 
    Animal modelSH-SY5Y and NGP xenografts
    Formulation & DosageDissolved in DMSO; 5 mg/kg; i.p. injection
    References

    Blood. 2012 Aug 23;120(8):1668-77; Cell Death Dis. 2014 Feb 20;5:e1079.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    NSC697923

    Compound NSC697923 inhibits NF-κB activation induced by PMA, but not by TNFα. Blood. 2012 Aug 23;120(8):1668-77.
     

    NSC697923

    In vivo efficacy of NSC697923 on human NB xenografts. Cell Death Dis. 2014 Feb 20;5:e1079.
     

    NSC697923

    NSC697923 specifically inhibits Ubc13-mediated polyubiquitin chain synthesis in vitro. Blood. 2012 Aug 23;120(8):1668-77.


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