PARP10-IN-1
PARP10-IN-1 is a PARP10 inhibitor with an IC50 of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 2286261-72-9
- Formula: C16H13F3N2O
- Molecular Weight:306.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PARP10 1.8 or 2.7 μM (IC50) |
PARP10-IN-1 potently inhibits the catalytic domain of PARP10 with an IC50 of 1.8 μM and exhibits 29-fold selectivity over full-length PARP11 in a cell-free MARylation assay[1].
PARP10-IN-1 inhibits the catalytic domain of PARP10 with an IC50 of 2.7 μM, exhibits >37-fold selectivity over all tested H-Y-E PARPs, >10-fold selectivity over most tested H-Y-Φ PARPs (PARP6, PARP8, PARP12, PARP11, PARP14, PARP15), 7-fold selectivity over PARP7, and 2.5-fold selectivity over PARP16_ΔTM in cell-free MARylation assays[1].
PARP10-IN-1 (1-100 μM; 3 h) is membrane-permeable and inhibits PARP10 auto-MARylation (EC50 = 11 μM) and PARP10-mediated MARylation of endogenous high molecular weight targets (EC50 = 2.3 μM) in GFP-PARP10-transfected HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells transfected with GFP-PARP10
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Concentration:1-100 μM
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Incubation Time:3 h
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Result:Inhibited PARP10 auto-MARylation with an EC50 of 11 μM.
Inhibited PARP10-mediated MARylation of high molecular weight (HMW) endogenous targets with an EC50 of 2.3 μM.
Inhibited total PARP10-dependent MARylation with an EC50 of 6.8 μM.
Chemical Information
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CAS No. 2286261-72-9
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Molecular Weight 306.28
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Formula C16H13F3N2O
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SMILES
O=C1NCCC2=C1C=CC(C3=CC(C(F)(F)F)=NC=C3)=C2C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PARP10-IN-1 Related Classifications
HY-125217 Related Classifications
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