| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
PARP10 0.14 μM (IC50) PARP15 0.40 μM (IC50)
PARP10/15-IN-3 targets PARP10 and PARP15, which are members of the poly(ADP-ribose) polymerase family. PARP10 and PARP15 catalyze the addition of ADP-ribose polymers to target proteins, a post-translational modification involved in various cellular processes including DNA damage repair, cellular stress responses, and protein function regulation. By inhibiting these enzymes, the compound modulates ADP-ribosylation signaling pathways. |
|---|---|
| ln Vitro |
In vitro, PARP10/15-IN-3 demonstrates potent dual inhibitory activity against PARP10 and PARP15 with IC₅₀ values of 0.14 µM and 0.40 µM, respectively. The compound is a selective small-molecule inhibitor that can be used for biochemical and cellular studies. Its inhibitory activity makes it a valuable tool for studying the specific functions of PARP10 and PARP15 in cellular processes.
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| ln Vivo |
In vivo activity data for PARP10/15-IN-3 are limited. As a potent dual inhibitor of PARP10 and PARP15, the compound is expected to demonstrate biological effects in animal models where these enzymes play pathogenic roles. Further studies would be needed to evaluate its in vivo efficacy and pharmacokinetic properties.
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| Enzyme Assay |
For non-cellular in vitro enzyme assays, PARP10/15-IN-3 is evaluated for its inhibitory activity against purified PARP10 and PARP15. The compound is incubated with each enzyme and its substrate (NAD⁺), and the incorporation of ADP-ribose polymers is measured using radioactive or antibody-based detection methods. IC₅₀ values are determined from dose-response curves, with values of 0.14 µM for PARP10 and 0.40 µM for PARP15.
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| Cell Assay |
For in vitro cellular assays, PARP10/15-IN-3 is tested in cell lines to assess its effects on PARP10 and PARP15-mediated ADP-ribosylation. Cells are treated with serial dilutions of the compound, and ADP-ribosylation levels of target proteins are measured using specific antibodies. Cell viability and proliferation may be assessed using standard assays. The compound's effects on DNA damage repair and cellular stress responses are evaluated.
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| Animal Protocol |
For in vivo animal studies, PARP10/15-IN-3 would typically be evaluated in mouse models of diseases where PARP10 and PARP15 play roles. Mice are treated with the compound via oral or intraperitoneal administration at various doses. Efficacy is assessed by measuring disease-related endpoints, and ADP-ribosylation levels are measured in target tissues to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PARP10/15-IN-3 are limited. As a small-molecule inhibitor with a molecular weight of 274.32, it is expected to have favorable oral bioavailability and tissue distribution. The compound is supplied as a solid with defined molecular properties and storage recommendations to preserve stability for experiments. Further pharmacokinetic studies would be needed to fully characterize its ADME profile.
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| Toxicity/Toxicokinetics |
Toxicological data for PARP10/15-IN-3 are limited. As a PARP10 and PARP15 inhibitor, the compound may have on-target effects on normal cellular functions regulated by ADP-ribosylation. Comprehensive toxicology studies would be required for therapeutic development. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
PARP10/15-IN-3 (Compound 8a) is a potent dual inhibitor of PARP10 and PARP15 with IC₅₀ values of 0.14 µM and 0.40 µM, respectively. The compound has a molecular formula of C₁₅H₁₈N₂O₃ and a molecular weight of 274.32. PARP10 and PARP15 are involved in DNA damage repair, cellular stress responses, and protein post-translational modifications. This inhibitor is a valuable tool for studying ADP-ribosylation signaling pathways.
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| Molecular Formula |
C15H18N2O3
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|---|---|
| Molecular Weight |
274.315023899078
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| Exact Mass |
274.131
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| CAS # |
2892064-88-7
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| PubChem CID |
166597670
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| Appearance |
White to off-white solid powder
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| LogP |
2.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
379
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1CCC(CC1)COC2=CC3=C(C=C2)C(=O)NNC3=O
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| InChi Key |
PCAWJIMDNGAMRA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H18N2O3/c18-14-12-7-6-11(8-13(12)15(19)17-16-14)20-9-10-4-2-1-3-5-10/h6-8,10H,1-5,9H2,(H,16,18)(H,17,19)
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| Chemical Name |
6-(cyclohexylmethoxy)-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: 16.67 mg/mL (60.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 16.7 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. Solubility in Formulation 2: ≥ 1.67 mg/mL (6.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6454 mL | 18.2269 mL | 36.4538 mL | |
| 5 mM | 0.7291 mL | 3.6454 mL | 7.2908 mL | |
| 10 mM | 0.3645 mL | 1.8227 mL | 3.6454 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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