| 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 0.15 μM (IC50) PARP15 0.37 μM (IC50)
The primary molecular targets of PARP10/15-IN-2 are PARP10 and PARP15, which belong to the mono-ADP-ribosyltransferase (mono-ART) subfamily of PARP enzymes. It acts as a potent dual inhibitor, with reported IC50 values of 0.15 uM (150 nM) against PARP10 and 0.37 uM (370 nM) against PARP15. By binding to these enzymes, it blocks their ability to transfer a single ADP-ribose unit onto target proteins. |
|---|---|
| ln Vitro |
In vitro, PARP10/15-IN-2 effectively penetrates cellular membranes, demonstrating excellent cell permeability. Its primary observed in vitro activity is its ability to rescue cells from apoptosis, meaning it prevents programmed cell death. This is a direct consequence of its potent dual inhibition of PARP10 and PARP15, which are known to play roles in cell survival signaling pathways. Its IC50s are 0.15 uM for PARP10 and 0.37 uM for PARP15.
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| ln Vivo |
Specific in vivo efficacy data for PARP10/15-IN-2 is not presented in the provided literature. As a tool compound for studying cell survival mechanisms, its primary application is likely focused on in vitro assays to dissect the cellular functions of PARP10 and PARP15. However, its cell permeability suggests it could potentially be used in animal models to probe the biology of these targets in vivo.
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| Enzyme Assay |
A cell-free biochemical assay is used to determine the IC50 of PARP10/15-IN-2. The assay involves incubating purified, recombinant PARP10 or PARP15 enzyme with a biotinylated target protein substrate and a radio-labeled NAD+ (the co-substrate for ADP-ribosylation). The incorporation of the label onto the substrate is measured by scintillation counting. The compound is added to the reaction mixture to assess its inhibitory activity.
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| Cell Assay |
For cellular studies, cell lines (e.g., those relevant to stress responses) are treated with PARP10/15-IN-2. The key endpoint is the assessment of apoptosis. Cells are treated with an apoptotic inducer (e.g., a chemotherapeutic agent) in the presence or absence of the compound. Apoptosis is then quantified by flow cytometry using Annexin V and propidium iodide (PI) staining, or by measuring caspase activity. A reduction in these signals indicates the compound is rescuing cells from apoptosis.
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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 PK/PD study would involve administering the compound to mice via intraperitoneal (IP) injection. The solubility data (e.g., DMSO: Tween 80: Saline = 10:5:85) provides a formulation for such studies. Blood and tissues would be collected at time points to measure the concentration of the compound (PK) and to assess PARP10/15 inhibition in target tissues (PD).
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| ADME/Pharmacokinetics |
Specific ADME data for PARP10/15-IN-2 is not provided in the literature. It is described as cell-permeable, indicating it can cross biological membranes. The compound has a molecular weight of 286.26 and is soluble in DMSO at 50 mg/mL. This high solubility facilitates its use in in vitro assays and allows for the preparation of stock solutions for potential in vivo studies. It is typically stored as a powder at -20degC.
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| Toxicity/Toxicokinetics |
No specific toxicology data for PARP10/15-IN-2 is presented. Given its role in rescuing cells from apoptosis, its toxicity profile may be linked to its on-target effect. By promoting cell survival, it could potentially have undesirable effects. However, it is a research tool, and its toxicological evaluation is likely the subject of ongoing or future studies. Standard safety precautions should be taken when handling.
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| References | |
| Additional Infomation |
PARP10 and PARP15 are unique among PARP family members as they are primarily mono-ADP-ribosyltransferases (mono-ARTs), not poly-ARTs like PARP1. Their biological functions include regulation of cell proliferation, apoptosis, and the DNA damage response. PARP10/15-IN-2 is a valuable tool for investigating the specific roles of these mono-ARTs, which are less studied than their poly-ART counterparts. The compound is in the preclinical research stage.
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| Molecular Formula |
C15H11FN2O3
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|---|---|
| Molecular Weight |
286.257847070694
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| Exact Mass |
286.075
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| CAS # |
2892064-99-0
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| PubChem CID |
163409145
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| Appearance |
White to off-white solid powder
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| LogP |
2
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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 |
21
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| Complexity |
418
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C(=C1)COC2=CC3=C(C=C2)C(=O)NNC3=O)F
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| InChi Key |
GJJIICZAOJXOEJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H11FN2O3/c16-13-4-2-1-3-9(13)8-21-10-5-6-11-12(7-10)15(20)18-17-14(11)19/h1-7H,8H2,(H,17,19)(H,18,20)
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| Chemical Name |
6-[(2-fluorophenyl)methoxy]-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: 50 mg/mL (174.67 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 | 3.4933 mL | 17.4666 mL | 34.9333 mL | |
| 5 mM | 0.6987 mL | 3.4933 mL | 6.9867 mL | |
| 10 mM | 0.3493 mL | 1.7467 mL | 3.4933 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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