| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
VK‑1727 directly targets EBNA1, reducing its DNA‑binding activity. EBNA1 binds to specific viral and cellular DNA sequences to enable episome replication and transcription of other viral genes. By inhibiting EBNA1, VK‑1727 disrupts viral genome maintenance and cell proliferation driven by EBV, without affecting EBV‑negative cells.
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| ln Vitro |
In EBV+ cells, VK-1727 (25 μM, 72 hours) dramatically decreased the overall number of G2 cells [1].
VK‑1727 selectively inhibits the proliferation of EBV‑positive gastric cancer cell lines (SNU‑719 and YCCEL1) and spontaneous lymphoblastoid cell lines derived from multiple sclerosis patients. In contrast, it has no discernible effect on EBV‑negative gastric cancer cells (AGS and MKN74) or EBV‑negative lymphoblastoid cell lines. |
| ln Vivo |
In mouse xenograft models using EBV‑positive gastric cancer cells (SNU‑719 and YCCEL1), intraperitoneal treatment with VK‑1727 produces a significant, dose‑dependent reduction in tumor growth. In contrast, the compound has no effect on xenografts established from EBV‑negative gastric cancer cell lines. These results confirm the on‑target, EBV‑dependent mechanism of action.
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| Enzyme Assay |
In vitro EBNA1 DNA‑binding assays are performed using electrophoretic mobility shift assays (EMSA) or FRET‑based assays. Recombinant EBNA1 protein is incubated with a fluorescently labeled oligonucleotide containing the EBNA1 binding site. VK‑1727 is added at concentrations ranging from 0.01 uM to 100 uM, and the reduction in protein-DNA complex formation is quantified.
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: EBV- B cell lines; EBV+ SLCLs Tested Concentrations: 25 μM Incubation Duration: 72 hrs (hours) Experimental Results: Dramatically diminished the total population of G2 cells in EBV+ cells(HC1-2, SMS1-3 and AMS1- 4) and not observed on EBV-(Ramos and BJAB) B cells. EBV‑positive and EBV‑negative cell lines are seeded in 96‑well plates and treated with increasing concentrations of VK‑1727 (0.01‑100 uM) for 72 hours. Cell viability is then measured using an ATP‑based luminescence assay (CellTiter‑Glo). Additionally, cell cycle progression can be analyzed by flow cytometry after propidium iodide staining, and EBNA1 binding at known sites can be assessed by chromatin immunoprecipitation (ChIP‑qPCR). |
| Animal Protocol |
Female NOD/SCID or nude mice are implanted subcutaneously with EBV‑positive gastric cancer cells (SNU‑719 or YCCEL1) or EBV‑negative controls (AGS or MKN74). Once tumors reach approximately 100 mm3, VK‑1727 is administered by intraperitoneal injection at 20‑50 mg/kg daily or twice daily. Tumor volumes are measured every 2‑3 days with calipers. At the end of the study, tumors are excised, weighed, and analyzed for EBV gene expression and cell proliferation markers.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for VK‑1727 are limited. As a small‑molecule inhibitor (MW ~400‑500 g/mol), it is expected to have reasonable oral bioavailability and tissue penetration. Maximum plasma concentrations likely occur within 1‑2 hours after oral administration, and the compound is expected to be metabolized primarily by CYP enzymes in the liver.
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| Toxicity/Toxicokinetics |
In the available preclinical studies, VK‑1727 appears well‑tolerated at the tested doses (≤50 mg/kg) without obvious weight loss or behavioral changes in mice. No specific LD50 or target organ toxicity data have been published, but the selectivity for EBV‑positive cells suggests a favorable safety margin.
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| References | |
| Additional Infomation |
VK‑1727 was initially identified as an EBNA1 inhibitor with potential applications in EBV‑associated gastric cancer (EBVaGC). More recent studies have extended its use to multiple sclerosis, where EBV‑infected B‑cells are thought to drive pathology. VK‑1727 is currently in the preclinical research stage and has not yet entered clinical trials. It is a valuable chemical probe for dissecting the role of EBNA1 in viral persistence and EBV‑driven diseases.
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| Molecular Formula |
C29H25NO4
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| Molecular Weight |
451.51
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| Appearance |
Off-white to light brown solid powder
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| SMILES |
O=C(OC)C1=CC=CC(C#CC2=CC=C(OC3CCOCC3)C=C2)=C1C4=CC5=C(C=C4)C=CN5
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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 (~221.5 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.54 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (5.54 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2148 mL | 11.0740 mL | 22.1479 mL | |
| 5 mM | 0.4430 mL | 2.2148 mL | 4.4296 mL | |
| 10 mM | 0.2215 mL | 1.1074 mL | 2.2148 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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