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Art. -Nr.: HY-125217

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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.

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CAS. Nr.: 2286261-72-9
Formel: C₁₆H₁₃F₃N₂O
Molecular Weight:306.28

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PARP10-IN-1 Chemical Structure

CAS. Nr.: 2286261-72-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

PARP10

1.8 or 2.7 μM (IC₅₀)

Alle PARP Isoform-spezifische Produkte anzeigen :

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.

Western Blot Analysis^[1]

Cell Line:

HEK293T cells transfected with GFP-PARP10
Concentration:

1-100 μM
Incubation Time:

3 h
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

CAS. Nr. 2286261-72-9
Molecular Weight 306.28
Formel C₁₆H₁₃F₃N₂O
SMILES

O=C1NCCC2=C1C=CC(C3=CC(C(F)(F)F)=NC=C3)=C2C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Morgan RK, et al. Rational Design of Cell-Active Inhibitors of PARP10. ACS Med Chem Lett. 2018;10(1):74-79. Published 2018 Nov 29. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
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PARP10-IN-1

Alle PARP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PARP10-IN-1 Related Classifications

HY-125217 Related Classifications