NSC697923

For research use only. Not for use in humans.

Catalog No.S7142

5 publications

NSC697923 Chemical Structure

Molecular Weight(MW): 267.26

NSC697923 is a cell-permeable and selective inhibitor of the Ub-conjugating enzyme (E2) complex Ubc13-Uev1A.

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Selleck's NSC697923 has been cited by 5 publications

2 Customer Reviews

  • Immunofluorescence analysis of b-actin distribution and Lys63 ubiquitination in HK2 cells. Cells were preincubated with the specific inhibitor of the Ubc13–Uev1A complex NSC697923, in the indicated conditions before D-glucose was added. The results represent 4 independent experiments.

    FASEB J, 2017, 31(1):308-319. NSC697923 purchased from Selleck.

    Effect of lys63 ubiquitination inhibition on HG-induced LC3 and p62 protein expression in HK2 cells. Cells were pre-incubated with the inhibitor NSC697923, in the specific conditions before adding Dglucose. a, d Immunofluorescence analysis of LC3 and p62 puncta and lysine63 ubiquitinated proteins after 48 h of HG stimulation.

    J Mol Med (Berl), 2018, 96(7):645-659. NSC697923 purchased from Selleck.

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Choose Selective E2 conjugating Inhibitors

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

Kinase Assay:[1]
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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 Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[2]
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  • Animal Models: SH-SY5Y and NGP xenografts.
  • Formulation: DMSO
  • Dosages: ~5 mg/kg/day
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 53 mg/mL (198.3 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
15mg/mL

* 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.

Chemical Information

Molecular Weight 267.26
Formula

C11H9NO5S

CAS No. 343351-67-7
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)[S](=O)(=O)C2=CC=C(O2)[N+]([O-])=O

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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E2 conjugating Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID