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| Targets |
DPBQ targets the p53 tumor suppressor protein, a key regulator of the cell cycle and apoptosis. It induces the expression and phosphorylation of p53. This activation of p53 leads to the initiation of apoptosis, specifically in high-ploidy (tetraploid) cells. The compound does not appear to act by inhibiting topoisomerase or by binding directly to DNA. This unique mechanism of action, targeting polyploid cells, is of interest in cancer research, as polyploidy is a feature of many cancer cells.
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| ln Vitro |
DPBQ promotes apoptosis and cell death and has a selective effect on 4N cells. DPBQ stimulates the production and phosphorylation of p53, an effect unique to tetraploid cells. Knockdown of TP53 restored the proliferation of tetraploid cells in the presence of DPBQ [1].
In vitro, DPBQ induces apoptosis and death in a manner that specifically affects 4N (tetraploid) cells. It induces the expression and phosphorylation of p53, and this effect is specific to tetraploid cells. In the absence of TP53, tetraploid cells can proliferate even in the presence of DPBQ. This demonstrates that the compound's activity is dependent on p53. Its activity is assessed by measuring p53 levels, apoptosis markers, and cell viability in cell lines with different ploidy levels. |
| ln Vivo |
In vivo, DPBQ's potential as an anticancer agent is of interest. By selectively inducing apoptosis in polyploid cancer cells, it could be a valuable tool for targeting this specific cell population. However, in vivo studies are limited, and the compound is primarily used in research settings.
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| Enzyme Assay |
In vitro non-cell enzyme/receptor binding assays for DPBQ are not applicable, as it does not act on a specific enzyme in a cell-free system. Its activity is assessed in cell-based assays. The compound does not inhibit topoisomerase or bind DNA.
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| Cell Assay |
In vitro cell-based assays for DPBQ use cell lines with different ploidy levels (e.g., diploid vs. tetraploid). Cells are treated with the compound, and the levels of p53 and phosphorylated p53 are measured by Western blotting. Apoptosis is assessed by measuring caspase activity, Annexin V staining, or DNA fragmentation. Cell viability is measured using MTT or similar assays. The compound's specificity for high-ploidy cells is a key feature of these studies.
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| Animal Protocol |
In vivo animal studies for DPBQ are limited. Xenograft models using tetraploid cancer cells could be used to study its antitumor efficacy. The compound would be administered, and its effects on tumor growth and p53 activation would be assessed. However, specific in vivo data are not available in the provided search results.
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| ADME/Pharmacokinetics |
DPBQ has a molecular weight of 362.38 g/mol and a molecular formula of C₂₄H₁₄N₂O₂. It has a purity of ≥95%. It is a solid. It is soluble in DMSO. The compound should be stored under appropriate conditions, typically at -20°C. Its stability in solution is not well reported.
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| Toxicity/Toxicokinetics |
The toxicity profile of DPBQ is not extensively detailed. As a p53 activator and apoptosis inducer, it has the potential to cause significant biological effects. It is classified as a research compound and is not intended for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
DPBQ is a potent apoptosis inducer specific for high-ploidy cells and a p53 activator. It does not inhibit topoisomerase or bind DNA. It is used in cancer research to study the role of p53 and polyploidy. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C24H14N2O2
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|---|---|
| Molecular Weight |
362.38
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| Exact Mass |
362.105
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| CAS # |
7029-89-2
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| PubChem CID |
364074
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| Appearance |
Light yellow to green yellow solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
28
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=CC=C12)C3=C(N=C(C4=CC=CC=C4)C(C5=CC=CC=C5)=N3)C2=O
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| InChi Key |
BDDRJIAFKGWLMD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H14N2O2/c27-23-17-13-7-8-14-18(17)24(28)22-21(23)25-19(15-9-3-1-4-10-15)20(26-22)16-11-5-2-6-12-16/h1-14H
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| Chemical Name |
2,3-diphenylbenzo[g]quinoxaline-5,10-dione
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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 : ~2.94 mg/mL (~8.11 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7595 mL | 13.7977 mL | 27.5953 mL | |
| 5 mM | 0.5519 mL | 2.7595 mL | 5.5191 mL | |
| 10 mM | 0.2760 mL | 1.3798 mL | 2.7595 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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