Biological Information

Background Information:

Poly (ADP-ribose) polymerase 2 (PARP2) is an ADP-ribosyltransferase and plays a critical role in the DNA damage response, DNA metabolism, and chromatin architecture. While PARP1 is activated by multiple forms of DNA damage-mimicking oligonucleotides, PARP2 is specifically activated by 5′-phosphorylated DNA breaks. At the BER process of DNA repair, PARP1 synthesizes poly ADP-ribose (PAR) and recruits repairing machinery at the initial stage, along with PARP2 which maintains the following repair process. Pharmacological inhibition of PARP2 provides a multipronged attack on tumor physiology in genomic, cellular, and microenvironmental aspects.

Family:

DNA Repair & Mitotic Regulation

Class:

Other

Protein Name:

PARP2

Uniprot Number:

Q9UGN5

Protein Aliases:

ARTD2

Gene Name:

PARP2

Gene ID:

10038

Gene Aliases:

ARTD2

Accession Number:

NM_005484

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 PARP2 protein 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 0.25 µg/ml enzyme for 15 minutes at 25°C in Tris-HCl buffer pH 8.0. The reaction is initiated by addition of 25 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:

25 µM NAD+

Incubation:

60 min at 25°C

Control Inhibitor:

Olaparib

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

PubChem ID

23725625

Name

Olaparib

Measurement

0.0012µM - IC50

PubChem ID

135565554

Name

Pamiparib

Measurement

0.00029µM - IC50

PubChem ID

135565981

Name

Stenoparib

Measurement

0.0007µM - IC50

PubChem ID

25015515

Name

UPF 1069

Measurement

4.4µM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

RELATED SOLUTIONS

Item: PP317