Poly (ADP-ribose) Polymerase 3 (PARP3) Human Enzymatic LeadHunter Assay - TW
OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Poly (ADP-ribose) polymerase 3 (PARP3) catalyzes the covalent attachment of a single ADP-ribose derived from NAD+ to the target protein, a post-translational modification to regulate cellular events including programmed and stress-induced double-strand break repair, chromosomal rearrangements, transcriptional regulation, mitotic segregation, differentiation, cell metabolism, or cell death. The demonstrated protein targets of PARP3 include the mitotic components, the DNA repair proteins, and the histone H2B. PARP3 also MARylates 5ʹ and 3ʹ-terminal phosphate residues in DNA. Highly expressed PARP3 in aggressive tumors drives malignancy by promoting TGFβ-induced EMT and mTORC2 signaling that exemplifies PARP3 as a prominent beneficial target in precision medicine for highly aggressive breast cancers.
Family:
DNA Repair & Mitotic Regulation
Class:
Other
Protein Name:
PARP3
Uniprot Number:
Q9Y6F1
Protein Aliases:
ARTD3
Gene Name:
PARP3
Gene ID:
10039
Gene Aliases:
ADPRT3, IRT1, ARTD3
Accession Number:
NM_001003931
Organism:
Human
Construct Details:
Full length, Recombinant
Assay Information
Assay Type:
Biochemical
Assay Sub Type:
Enzymatic
Functional Mode:
Antagonist
Detection Method:
Spectrophotometry
Platform:
Plate reader
Measured Response:
Absorbance
Testing Information
Procedure Summary:
Human recombinant protein PARP3 expressed in Sf9 cells is used. 100 ng histone proteins are coated on a 96-well plate. Test compound and/or vehicle is preincubated with 0.1 µg/ml enzyme for 15 minutes at 25°C in Tris-HCl buffer pH 8.0. The reaction is initiated by addition of 50 µM spiked biotinylated NAD+ plus NAD+ for another 60 minutes reaction time. Streptavidin-HRP is added and followed by addition of the TMB substrate to produce color that can be measured at 450 nm on a spectrophotometer. Compounds are screened at 10 µM.
Substrate:
50 µM NAD+
Incubation:
60 min at 25°C
Control Inhibitor:
Talazoparib
Criteria For Significance:
≥ 50% of max stimulation or inhibition
Test Concentration / Dose:
Suggested concentration for initial testing is 10 uM
Test Sample Requirements:
Minimum for 1) Screen: 25 μl of 10 mM stock -OR- 1 mg (pre-weighed). 2) Dose Response: 60 μl of 10 mM stock -OR- 1 mg (pre-weighed).
Minimum Order Quantity:
2
Turnaround Time
Standard:
15 Business Days
Reference Compound Data
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
RELATED SOLUTIONS
PARP Screen LeadHunter Panel - TW
Item: PP317
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