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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
PARP10 1.8 or 2.7 μM (IC50) |
In Vitro
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. Further protocols information, click here.
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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