| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PARP10 160 nM (IC50) PARP15 370 nM (IC50)
The primary molecular targets of PARP10/15-IN-1 are PARP10 and PARP15, two mono-ADP-ribosyltransferases. It acts as a potent dual inhibitor, with reported IC50 values of 160 nM (0.16 uM) against PARP10 and 370 nM (0.37 uM) against PARP15. By binding to these enzymes, it inhibits their transfer of ADP-ribose onto target proteins, disrupting their roles in DNA repair and cellular stress responses. |
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| ln Vitro |
In vitro, PARP10/15-IN-1 demonstrates potent biochemical inhibition of PARP10 and PARP15. While the provided texts do not detail specific cellular EC50 values, its mechanism of action is established for cancer research. By inhibiting these enzymes, it blocks the cellular processes they regulate, leading to the suppression of cancer cell survival mechanisms. This makes it a useful tool for studying the role of mono-ADP-ribosylation in cancer.
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| ln Vivo |
Specific in vivo efficacy data for PARP10/15-IN-1 is not presented in the provided literature. Given its role as an inhibitor, it is expected to be evaluated in xenograft mouse models to assess its potential anti-cancer activity. By inhibiting PARP10 and PARP15, which are involved in DNA repair and cell survival, it could potentially sensitize tumors to chemotherapy or other DNA-damaging agents, a common strategy for PARP inhibitors.
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| Enzyme Assay |
A cell-free biochemical assay is used to determine the inhibitory activity of PARP10/15-IN-1. The assay is performed by incubating purified recombinant PARP10 or PARP15 enzyme with a biotinylated substrate protein and a radiolabeled co-substrate, 3H-NAD+. The incorporation of the 3H-ADP-ribose unit onto the substrate is measured by scintillation counting. The compound is added to the reaction to calculate its IC50.
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| Cell Assay |
In cellular assays, cancer cell lines are treated with PARP10/15-IN-1 to assess its anti-proliferative effects. After treatment for 48-72 hours, cell viability is measured using a luminescence-based CellTiter-Glo or colorimetric MTT assay. The induction of apoptosis can be quantified by flow cytometry after staining cells with Annexin V and propidium iodide. Changes in PARP10/15 downstream signaling pathways can be assessed by Western blotting.
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| Animal Protocol |
As a research tool, detailed in vivo animal protocols for this specific compound are not provided. However, a typical study for a PARP inhibitor involves using immunocompromised mice bearing human cancer xenografts. The compound, formulated in a suitable vehicle (e.g., DMSO:PEG300:Tween80:saline), would be administered via intraperitoneal (IP) injection. Tumor volume would be measured by calipers to assess growth inhibition.
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| ADME/Pharmacokinetics |
Specific ADME data for PARP10/15-IN-1 is not provided in the literature. The compound has a molecular weight of 274.30 and is soluble in DMSO at 25 mg/mL. Its solubility and predicted LogP (1.6) suggest it has suitable drug-like properties for use in biological assays. It is typically stored as a powder at -20degC, and solutions can be stored for up to 6 months at -80degC.
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| Toxicity/Toxicokinetics |
No specific toxicology data for PARP10/15-IN-1 is presented. As with many PARP inhibitors, on-target toxicities can include hematological effects such as thrombocytopenia, anemia, or neutropenia. However, as a research tool, detailed toxicology evaluations are typically performed as part of later-stage drug discovery efforts. Standard laboratory safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
PARP10 and PARP15 are unique mono-ADP-ribosyltransferases whose biological roles are less well-understood than classical PARP1/2. Research suggests they are involved in the DNA damage response and cellular stress signaling. PARP10/15-IN-1 is a valuable tool for dissecting these specific biological functions and validating them as potential drug targets for cancer therapy. The compound is in the preclinical stage.
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| Molecular Formula |
C13H10N2O3S
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|---|---|
| Molecular Weight |
274.295101642609
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| Exact Mass |
274.041
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| CAS # |
2892065-01-7
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| PubChem CID |
166597669
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
377
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=C1OCC3=CSC=C3)C(=O)NNC2=O
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| InChi Key |
RFKWWUGSOVDNFF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H10N2O3S/c16-12-10-2-1-9(5-11(10)13(17)15-14-12)18-6-8-3-4-19-7-8/h1-5,7H,6H2,(H,14,16)(H,15,17)
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| Chemical Name |
6-(thiophen-3-ylmethoxy)-2,3-dihydrophthalazine-1,4-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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 25 mg/mL (91.14 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 | 3.6456 mL | 18.2282 mL | 36.4564 mL | |
| 5 mM | 0.7291 mL | 3.6456 mL | 7.2913 mL | |
| 10 mM | 0.3646 mL | 1.8228 mL | 3.6456 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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