Biological Information

Background Information:

Poly (ADP-ribose) polymerase 7 (PARP7, also known as TiPARP) is a mono (ADP-ribosyl) transferase, containing a C-terminal HYI catalytic domain, a WWE motif thought to bind PAR and a single CCCH-type zinc-finger. PARP7 catalyzes the transfer of single unit of ADP-ribose onto substrate to regulate their function. Only a few targets of PARP-7 have been identified, including PARP-7 itself through automodification, as well as histones, AHR, and LXR. PARP7 is involved in a variety of cellular processes including innate immune regulation, cellular stress response, and transcription factor regulation. A selective inhibitor of PARP7 is assessed its efficacy against lung cancer in clinical trials, highlighting the potential of PARP7 as a cancer therapy target.

Family:

DNA Repair & Mitotic Regulation

Class:

Other

Protein Name:

PARP7

Uniprot Number:

Q7Z3E1

Protein Aliases:

Poly [ADP-ribose] polymerase 7, ADP-ribosyltransferase diphtheria toxin-like 14, TCDD-inducible poly [ADP-ribose] polymerase

Gene Name:

TIPARP

Gene ID:

25976

Gene Aliases:

DKFZP434J214, DKFZp686N0351, DDF1, PARP7, PARP-7, PARP-1, pART14, RM1, ARTD14

Accession Number:

NM_015508

Organism:

Human

Construct Details:

Fragment, 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 PARP7 expressed in Sf9 cells are used. 100 ng histone proteins are coated on a 96-well plate. Test compound and/or vehicle is preincubated with 2 µg/ml enzyme for 15 minutes at 25°C in Tris-HCl buffer pH 8.0. The reaction is initiated by addition of 20 µM biotinylated 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:

20 µM NAD+

Incubation:

60 min at 25°C

Control Inhibitor:

RBN-2397

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

146047148

Name

RBN-2397

Measurement

0.0071µM - IC50

Clinical Relevance

Therapeutic Area:

Oncology/Immuno-Oncology

Additional Information

Brand:

LeadHunter

Testing Location:

Taiwan - Taipei

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