| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The primary target of PARP14 inhibitor H10 is PARP14, a member of the poly(ADP-ribose) polymerase family of enzymes that catalyze the transfer of ADP-ribose units from NAD+ to target proteins. PARP14 is involved in various cellular processes including DNA repair, transcription regulation, and immune signaling. The compound selectively inhibits PARP14 with an IC₅0 of 490 nM while showing significantly lower potency against other PARP family members such as PARP1 (≈24-fold selectivity) and TNKS1 (≈18-fold selectivity). This selectivity makes H10 a valuable tool for studying the specific biological functions of PARP14.
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| ln Vitro |
In vitro studies have demonstrated that PARP14 inhibitor H10 is a potent and selective inhibitor of PARP14 with an IC₅0 of 490 nM. It exhibits approximately 24-fold selectivity over PARP1 and 18-fold selectivity over TNKS1. The compound induces caspase-3/7-mediated apoptosis in cells, indicating that PARP14 inhibition leads to cell death. This pro-apoptotic effect is likely mediated through disruption of PARP14's role in DNA repair and cell survival pathways. H10 has been shown to be effective in various cancer cell lines, making it a useful tool for studying PARP14 biology and validating it as a therapeutic target.
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| ln Vivo |
In vivo studies of PARP14 inhibitor H10 are limited, as the compound is primarily used as a research tool in cellular assays. However, given its potent and selective inhibition of PARP14 and its ability to induce apoptosis in cancer cells, H10 may have potential for in vivo efficacy studies in animal models of cancer. The compound's selectivity for PARP14 over other PARP family members suggests that it could provide a more targeted approach compared to pan-PARP inhibitors. Further studies are needed to evaluate its pharmacokinetic properties, bioavailability, and antitumor activity in vivo. H10 may also be useful for studying the role of PARP14 in immune function and other physiological processes.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, PARP14 inhibitor H10 is typically evaluated using enzymatic activity assays that measure PARP14-mediated ADP-ribosylation of target proteins or auto-modification. The compound is incubated with recombinant PARP14 enzyme, NAD+, and a suitable substrate (such as histones or automodification) at various concentrations. PARP activity is quantified using methods such as radioactive incorporation of [32P]-NAD+, chemiluminescent detection of ADP-ribosylated products, or fluorescence-based assays. IC₅0 values are determined from dose-response curves. Selectivity profiling against other PARP family members (PARP1, TNKS1, etc.) is performed using similar enzymatic assays to confirm specificity.
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| Cell Assay |
For in vitro cellular experiments, PARP14 inhibitor H10 is typically tested in cancer cell lines to evaluate its effects on cell viability, proliferation, and apoptosis. Cells are cultured in appropriate media and treated with various concentrations of the compound (typically ranging from nanomolar to micromolar) for defined periods. Cell viability and proliferation are assessed using MTT, CellTiter-Glo, or colony formation assays. Apoptosis is evaluated using Annexin V staining, caspase-3/7 activity assays, or TUNEL staining. PARP14 inhibition can be confirmed by measuring ADP-ribosylation levels in cell lysates using Western blotting with anti-PAR antibodies. Gene expression changes and signaling pathway alterations can be analyzed by qPCR, Western blotting, or proteomic approaches.
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| Animal Protocol |
For in vivo animal experiments, PARP14 inhibitor H10 can be administered to tumor-bearing mice via various routes including oral gavage, intravenous injection, or intraperitoneal injection, depending on its solubility and pharmacokinetic properties. Xenograft models using human cancer cell lines in immunodeficient mice are commonly used to evaluate antitumor efficacy. Typical dosing regimens may range from 1 to 50 mg/kg administered daily or intermittently. Tumor volume is measured regularly, and tumor growth inhibition is calculated. Body weight and overall health are monitored. At study termination, tumors and tissues are collected for analysis of PARP14 inhibition markers, apoptosis, and pharmacokinetic parameters.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of PARP14 inhibitor H10 have not been extensively characterized in the public literature. As a small molecule with a molecular weight of 557.58 g/mol, its pharmacokinetic profile would depend on its solubility, lipophilicity, and protein binding. The compound's molecular properties suggest it may have moderate bioavailability and tissue distribution. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies in relevant animal models. The compound's metabolism, potential for drug-drug interactions, and excretion pathways remain to be fully elucidated. Formulation development may be necessary for optimal in vivo administration.
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| Toxicity/Toxicokinetics |
Toxicological data for PARP14 inhibitor H10 are limited, as the compound is primarily a research tool. Preliminary studies suggest that H10 is effective at inducing apoptosis in cancer cells at concentrations that inhibit PARP14. However, comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. As a PARP inhibitor, potential toxicities related to DNA repair inhibition in normal tissues should be considered. Appropriate safety precautions should be taken when handling this compound, including the use of personal protective equipment and adherence to institutional safety guidelines.
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| References | |
| Additional Infomation |
PARP14 inhibitor H10 is a research compound used to study the role of PARP14 in DNA repair, apoptosis, and cancer biology. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. H10's selectivity for PARP14 over other PARP family members makes it a valuable tool for dissecting the specific functions of PARP14. The compound induces caspase-3/7-mediated apoptosis, providing a mechanism for studying PARP14's role in cell survival. Further research may elucidate its potential therapeutic applications.
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| Molecular Formula |
C24H27N7O7S
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|---|---|
| Molecular Weight |
557.5788834095
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| Exact Mass |
557.169
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| CAS # |
2084811-68-5
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| PubChem CID |
122707115
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| Appearance |
Light yellow to khaki solid powder
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| LogP |
-1
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
39
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| Complexity |
974
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C=CC=C(C(=O)O)C=1)(NCCN1C=C(CCNC(CCC(NC2C=CC=C(C(N)=O)C=2)=O)=O)N=N1)(=O)=O
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| InChi Key |
MUOMSHSMJCWQFH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H27N7O7S/c25-23(34)16-3-1-5-18(13-16)28-22(33)8-7-21(32)26-10-9-19-15-31(30-29-19)12-11-27-39(37,38)20-6-2-4-17(14-20)24(35)36/h1-6,13-15,27H,7-12H2,(H2,25,34)(H,26,32)(H,28,33)(H,35,36)
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| Chemical Name |
3-[2-[4-[2-[[4-(3-carbamoylanilino)-4-oxobutanoyl]amino]ethyl]triazol-1-yl]ethylsulfamoyl]benzoic acid
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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 : ~62.5 mg/mL (~112.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.73 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7935 mL | 8.9673 mL | 17.9346 mL | |
| 5 mM | 0.3587 mL | 1.7935 mL | 3.5869 mL | |
| 10 mM | 0.1793 mL | 0.8967 mL | 1.7935 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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