Home Ubiquitin E2 conjugating inhibitor NSC697923 For research use only.

NSC697923

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

NSC697923 Chemical Structure

NSC697923 Chemical Structure

CAS No. 343351-67-7

Purity & Quality Control

NSC697923 Related Products

Signaling Pathway

E2 conjugating Signaling Pathways

E2 conjugating Signaling Pathway

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
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]
Kinase Assay 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 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.
In Vivo
In vivo NSC697923 (5 mg/kg/day, i.p.) demonstrates potent antitumor efficacy in both NB SH-SY5Y and NGP xenografts. [2]
Animal Research Animal Models SH-SY5Y and NGP xenografts.
Dosages ~5 mg/kg/day
Administration i.p.

Chemical Information & Solubility

Molecular Weight 267.26 Formula

C11H9NO5S
CAS No. 343351-67-7 SDF Download NSC697923 SDF
Smiles CC1=CC=C(C=C1)S(=O)(=O)C2=CC=C(O2)[N+](=O)[O-]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 53 mg/mL ( (198.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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