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
Clinical Relevance
Therapeutic Area:
Oncology/Immuno-Oncology
Additional Information
Brand:
LeadHunter
Testing Location:
Taiwan - Taipei
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