NSC697923

Catalog No.S7142 Batch:S714202

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Technical Data

Formula

C11H9NO5S
Molecular Weight 267.26 CAS No. 343351-67-7
Solubility (25°C)* In vitro DMSO 53 mg/mL (198.3 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.
Targets
E2 complex Ubc13-Uev1A [1]
In vitro 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. [1] In neuroblastoma (NB) cell lines, NSC697923 shows cytotoxic effect, and inhibits both anchorage-dependent and -independent colony formation. [2]
In vivo NSC697923 (5 mg/kg/day, i.p.) demonstrates potent antitumor efficacy in both NB SH-SY5Y and NGP xenografts. [2]

Protocol (from reference)

Kinase Assay:[1]
  • In vitro ubiquitination 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:[1]
  • Cell lines

    BC-DLBCL, GCB-DLBCL and primary DLBCL cells.

  • Concentrations

    ~1 μM

  • Incubation Time

    24 hours

  • Method

    Cell viability is measured by trypan blue exclusion assay following the manufacturer's instructions.
Animal Study:[2]
  • Animal Models

    SH-SY5Y and NGP xenografts.

  • Dosages

    ~5 mg/kg/day

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , FASEB J, 2017, 31(1):308-319]

Data from [Data independently produced by , , J Mol Med (Berl), 2018, 96(7):645-659]

Selleck's NSC697923 has been cited by 14 publications

Polyubiquitinated PCNA triggers SLX4-mediated break-induced replication in alternative lengthening of telomeres (ALT) cancer cells [ Nucleic Acids Res, 2024, gkae785] PubMed: 39291733
CRISPR-Cas9 knockout screen identifies novel treatment targets in childhood high-grade glioma [ Clin Epigenetics, 2023, 15(1):80] PubMed: 37161535
Enzymatic Redox Properties and Cytotoxicity of Irreversible Nitroaromatic Thioredoxin Reductase Inhibitors in Mammalian Cells [ Int J Mol Sci, 2023, 24(15)12460] PubMed: 37569833
Darapladib, an inhibitor of Lp-PLA2, sensitizes cancer cells to ferroptosis by remodeling lipid metabolism [ bioRxiv, 2023, 10.1101/2023.04.08.536136] PubMed: None
A small molecule inhibitor of caspase-1 inhibits NLRP3 inflammasome activation and pyroptosis to alleviate gouty inflammation [ Immunol Lett, 2022, 244:28-39] PubMed: 35288207
RNF8-mediated regulation of Akt promotes lung cancer cell survival and resistance to DNA damage [ Cell Rep, 2021, 37(3):109854] PubMed: 34686341
Ubiquitination status does not affect Vps34 degradation [ Genes Dis, 2020, 7(3):401-407] PubMed: 32884994
Prolonged unfolded protein reaction is involved in the induction of chronic myeloid leukemia cell death upon oprozomib treatment [ Cancer Sci, 2020, 112(1):133-143] PubMed: 33067904
Chilling stress reduced protein translation by the ubiquitination of ribosomal proteins in Volvariella volvacea. [ J Proteomics, 2020, 215:103668] PubMed: 31982547
Ube2v1-mediated ubiquitination and degradation of Sirt1 promotes metastasis of colorectal cancer by epigenetically suppressing autophagy [Shen T J Hematol Oncol, 2018, 11(1):95] PubMed: 30016968

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.