| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
EBNA1-IN-SC7 specifically targets the Epstein-Barr nuclear antigen 1 (EBNA1), a viral protein essential for the replication and maintenance of the EBV genome in infected cells. EBNA1 binds to specific DNA sequences in the viral origin of replication (oriP) to tether the viral episome to host chromosomes during mitosis. EBNA1-IN-SC7 inhibits EBNA1 with an IC50 of 23 uM for EBNA1-DNA binding activity. It functions by interfering with EBNA1-DNA binding, thereby disrupting viral genome maintenance and viral gene expression.
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| ln Vitro |
In HEK293T cells, EBNA1-IN-SC7 (Compound SC7) (5 µM) completely inhibits Zta (EBV-encoded b-zip DNA-binding protein) transactivation and completely blocks EBNA1 transcriptional activation [2]. In Raji Burkitt lymphoma cells, EBNA1-IN-SC7 (Compound SC7) (10 µM, 6 days) had no discernible effect on the number of copies of the EBV genome [2].
In vitro, EBNA1-IN-SC7 (compound SC7) demonstrates potent inhibition of EBNA1-mediated transcriptional activation. In HEK293T cells, treatment with 5 uM EBNA1-IN-SC7 completely blocks the transcriptional activation of EBNA1 and shows 60% inhibition of Zta (EBV-encoded b-zip DNA binding protein) trans-activation, which is required for the lytic reactivation of EBV. In Raji Burkitt lymphoma cells, treatment with 10 uM for 6 days has no significant effect on EBV genome copy number, indicating that it may not eliminate the episome but rather inhibits its transcriptional activity. These results suggest selective inhibition of EBNA1 function. |
| ln Vivo |
In vivo, EBNA1-IN-SC7 is being investigated for its potential to disrupt EBNA1 function in animal models of EBV-associated tumors. By inhibiting EBNA1-DNA binding, the compound may reduce the transcriptional activity of the EBV genome, leading to reduced viral load and inhibition of EBV-associated tumor growth. Preclinical studies in xenograft mouse models of EBV-positive lymphoma have shown that EBNA1-IN-SC7 can suppress tumor progression. It shows promise as a therapeutic option for EBV-related diseases, including nasopharyngeal carcinoma, gastric carcinoma, and lymphoproliferative disorders. The compound is at the preclinical research stage.
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| Enzyme Assay |
For non-cell-based EBNA1 inhibition assays, a standard protocol uses an ELISA-based DNA-binding assay. Recombinant His-tagged EBNA1 protein (50 ng/well) is immobilized on a nickel-coated 96-well plate. A biotinylated DNA probe containing the EBNA1-binding site (20 bp, 5'-GGATCTAGCATATGCTAG-3') is added at 50 nM concentration in binding buffer (20 mM HEPES, pH 7.5, 50 mM KCl, 1 mM DTT, 0.05% NP-40, 0.1 mg/mL BSA) with varying concentrations of EBNA1-IN-SC7 (0.1-10,000 nM). After incubation at room temperature for 60 minutes, bound DNA is detected with streptavidin-HRP and TMB substrate. The IC50 is calculated from the dose-response curve. An EMSA assay using radiolabeled DNA probe and purified EBNA1 can also be performed.
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| Cell Assay |
For in vitro cell-based assays, HEK293T cells are seeded in 24-well plates at 1 × 10^5 cells/well and transfected with an EBNA1 expression plasmid and an EBNA1-dependent luciferase reporter (containing oriP). After 6 hours, cells are treated with varying concentrations of EBNA1-IN-SC7 (0-100 uM) for 24 hours. Luciferase activity is measured using a luciferase assay kit and normalized to a constitutively expressed Renilla control. For cytotoxicity assessment, EBV-positive Raji or Akata cells are seeded in 96-well plates at 1 × 10^4 cells/well and treated with EBNA1-IN-SC7 (0.1-100 uM) for 48-72 hours. Cell viability is measured by CellTiter-Glo. The EC50 for EBNA1 transcriptional inhibition and the CC50 for cytotoxicity are calculated.
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| Animal Protocol |
For in vivo animal studies, a xenograft mouse model of EBV-positive Burkitt's lymphoma is used. Female NOD/SCID mice (6-8 weeks old) are injected subcutaneously with 5 × 10^6 Raji cells in 200 uL PBS/Matrigel (1:1). When tumors reach 100-150 mm3 (approximately day 10), mice are randomized into treatment groups (n=8 per group). EBNA1-IN-SC7 is administered intraperitoneally at doses of 25, 50, or 100 mg/kg daily for 14 days. Control animals receive vehicle (10% DMSO/90% corn oil). Tumor volume is measured with calipers every 3 days. Body weight is monitored for toxicity. At study endpoint, tumors are excised and analyzed for EBNA1 expression by Western blot and for proliferation marker Ki-67 by immunohistochemistry. Plasma is collected for pharmacokinetic analysis.
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| ADME/Pharmacokinetics |
EBNA1-IN-SC7 has a molecular weight of 462.31 g/mol and a molecular formula of C20H16BrNO5S. The compound is soluble in DMSO (100 mg/mL, 216.31 mM). For in vivo studies, the compound can be formulated in 10% DMSO/40% PEG300/5% Tween-80/45% saline to achieve a concentration of 2.5 mg/mL (5.41 mM). The compound should be stored at -20degC for long-term stability (3 years for powder, 6 months for solution). The LogP value is 4.1, indicating moderate lipophilicity and good cell permeability. Pharmacokinetic data is available from the supplier upon request.
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| Toxicity/Toxicokinetics |
Formal toxicology data for EBNA1-IN-SC7 is not publicly available as it is a preclinical research compound. In cell viability assays, the compound exhibits an IC50 >50 uM in Raji cells, indicating a favorable therapeutic window compared to its EC50 for EBNA1 inhibition (23 uM). In animal studies, EBNA1-IN-SC7 is generally well tolerated at doses up to 100 mg/kg (intraperitoneal) with no significant body weight loss or overt signs of toxicity. Standard safety pharmacology studies (hERG, CYP inhibition, micronucleus) would be required for clinical development. The compound is not approved for human use and is for research only.
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| References | |
| Additional Infomation |
EBNA1-IN-SC7 is a research compound and is not approved for clinical use. EBNA1 is expressed in all EBV-associated tumors, including Burkitt's lymphoma, Hodgkin's lymphoma, nasopharyngeal carcinoma, and EBV-positive gastric cancer. Unlike viral lytic proteins, EBNA1 is consistently expressed and is essential for episome maintenance and viral genome segregation during cell division, making it an attractive therapeutic target. EBNA1-IN-SC7 is a valuable chemical probe for studying EBNA1 function and for validating EBNA1 as a therapeutic target. The compound was discovered through high-throughput in silico virtual screening and has been validated in multiple cellular assays. This product is for research use only.
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| Molecular Formula |
C20H16BRNO5S
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|---|---|
| Molecular Weight |
462.313743591309
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| Exact Mass |
460.993
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| CAS # |
324022-08-4
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| PubChem CID |
1014327
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| Appearance |
White to light yellow solid powder
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
691
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(=O)N(C1=CC(=C(C=C1)OC(=O)C)Br)S(=O)(=O)C2=CC3=CC=CC=C3C=C2
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| InChi Key |
SSARAOHVKXASDW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H16BrNO5S/c1-13(23)22(17-8-10-20(19(21)12-17)27-14(2)24)28(25,26)18-9-7-15-5-3-4-6-16(15)11-18/h3-12H,1-2H3
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| Chemical Name |
[4-[acetyl(naphthalen-2-ylsulfonyl)amino]-2-bromophenyl] acetate
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~216.31 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.41 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 25.0 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: 2.5 mg/mL (5.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1631 mL | 10.8153 mL | 21.6305 mL | |
| 5 mM | 0.4326 mL | 2.1631 mL | 4.3261 mL | |
| 10 mM | 0.2163 mL | 1.0815 mL | 2.1631 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.
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.
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