| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
TNKS-1 and TNKS-2 (tankyrase 1 and 2). TNKS-2-IN-1 inhibits TNKS-1 and TNKS-2 with IC50 values of 259 nM and 1100 nM, respectively. By blocking TNKS2 activity, this compound stabilizes AXIN proteins, leading to the suppression of beta-catenin signaling. It also has antibacterial activity.
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| ln Vitro |
TNKS-2-IN-1 demonstrates inhibition of TNKS-1 and TNKS-2 in enzymatic assays with IC50 values of 259 nM and 1100 nM, respectively. It has antibacterial activity against Escherichia coli and Staphylococcus aureus. The compound's activity in Wnt/beta-catenin signaling makes it valuable for oncology research.
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| ln Vivo |
In vivo activity of TNKS-2-IN-1 has not been extensively characterized in published literature. The compound is primarily used as an in vitro research tool. In vivo studies would be needed to evaluate its therapeutic potential in Wnt-dependent tumor growth and other applications. Currently, no in vivo efficacy data have been reported.
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| Enzyme Assay |
In vitro enzyme assays for TNKS inhibition are performed using recombinant TNKS-1 or TNKS-2 enzymes and appropriate substrates in the presence of NAD+. TNKS-2-IN-1 is incubated at varying concentrations with the enzyme and substrate. Auto-ADP-ribosylation or substrate PARsylation is detected by radioactivity or immunoassay. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cells (e.g., cancer cell lines with Wnt/beta-catenin signaling) are cultured and treated with TNKS-2-IN-1 at concentrations typically ranging from 0.1–10 μM for 24–72 hours. TNKS inhibition is assessed by measuring AXIN protein levels (stabilization) and beta-catenin levels by Western blot. Cell proliferation and viability are assessed by standard assays. Antibacterial activity is assessed by MIC determination.
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| Animal Protocol |
In vivo animal studies for TNKS-2-IN-1 have not been reported in publicly available literature. The compound is primarily used for in vitro research. Future studies in xenograft models of Wnt-dependent tumors would be needed to evaluate in vivo efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for TNKS-2-IN-1 have not been published. The compound has a molecular weight of 267.24 and formula C14H9N3O3. Solubility information is limited. In vivo PK parameters such as half-life, bioavailability, and tissue distribution have not been characterized.
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| Toxicity/Toxicokinetics |
Toxicology data for TNKS-2-IN-1 have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling chemical inhibitors should be observed.
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| References | |
| Additional Infomation |
TNKS-2-IN-1 (CAS: 4765-59-7, molecular formula C14H9N3O3, molecular weight 267.24) is a TNKS-2 inhibitor. It inhibits TNKS-1 and TNKS-2 with IC50s of 259 nM and 1100 nM. It has antibacterial activity. It is not in clinical trials and has no regulatory approval. The compound is supplied as a research-grade inhibitor for laboratory use only.
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| Molecular Formula |
C14H9N3O3
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|---|---|
| Molecular Weight |
267.24
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| Exact Mass |
267.064
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| CAS # |
4765-59-7
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| PubChem CID |
135402338
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.021
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PDSXUXCWTDUVSZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H9N3O3/c18-14-11-3-1-2-4-12(11)15-13(16-14)9-5-7-10(8-6-9)17(19)20/h1-8H,(H,15,16,18)
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| Chemical Name |
2-(4-nitrophenyl)-3H-quinazolin-4-one
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| Synonyms |
TNKS-2-IN-1
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 3.7420 mL | 18.7098 mL | 37.4195 mL | |
| 5 mM | 0.7484 mL | 3.7420 mL | 7.4839 mL | |
| 10 mM | 0.3742 mL | 1.8710 mL | 3.7420 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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