NSC697923

Alias: NSC697923; NSC 697923; NSC-697923
Cat No.:V1317 Purity: ≥98%
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 Chemical Structure CAS No.: 343351-67-7
Product category: E2 conjugating
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
ln 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. In neuroblastoma (NB) cell lines, NSC697923 shows cytotoxic effect, and inhibits both anchorage-dependent and -independent colony formation
ln Vivo
NSC697923 (5 mg/kg/day, i.p.) demonstrates potent antitumor efficacy in both NB SH-SY5Y and NGP xenografts.
Enzyme 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.
Animal Protocol
Dissolved in DMSO; 5 mg/kg; i.p. injection
SH-SY5Y and NGP xenografts
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.
Physicochemical Properties
Molecular Formula
C11H9NO5S
Molecular Weight
267.255
Exact Mass
267.02
Elemental Analysis
C, 49.44; H, 3.39; N, 5.24; O, 29.93; S, 12.00
CAS #
343351-67-7
Related CAS #
343351-67-7
Appearance
Solid powder
SMILES
O=[N+](C1=CC=C(S(=O)(C2=CC=C(C)C=C2)=O)O1)[O-]
InChi Key
GAUHIPWCDXOLCZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H9NO5S/c1-8-2-4-9(5-3-8)18(15,16)11-7-6-10(17-11)12(13)14/h2-7H,1H3
Chemical Name
2-[(4-Methylphenyl)sulfonyl]-5-nitrofuran
Synonyms
NSC697923; NSC 697923; NSC-697923
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 200~53 mg/mL (748.33 ~198.3 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 5 mg/mL (18.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 5 mg/mL (18.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.7417 mL 18.7084 mL 37.4167 mL
5 mM 0.7483 mL 3.7417 mL 7.4833 mL
10 mM 0.3742 mL 1.8708 mL 3.7417 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • 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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