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Integrase inhibitor screening drug discovery

Catalog# TS-INTEG   -   For pricing, please inquire

Integrase Inhibitors Testing Service 

 

Send your Integrase Inhibitor Candidates to our laboratory for dependable, rapid turn-around, economical, and professional evaluation of the effect that your drugs and compounds have on integrase activity.  

 

The assay protocol has the unique ability to isolate the two activities of integrase, the 3’ processing reaction of viral DNA from the homologous recombination event that occurs during strand transfer to insert viral DNA into host DNA. 

The separation of 3’processing from strand transfer allows for a direct and specific determination of drug inhibition with each of these unique integrase activities.

 

 

  • To submit samples for evaluation send 1-3 mg (3 mg of peptide samples with molecular weights around 10 kd) of dry power with solubility information.  

  • We make a stock solution, usually hydrated in DMSO, at 10 to 30 mM.

  • Dilution series of 7 concentrations from 500 mM to 2 nM for integrase activity determination in the integrase assay.  

  • Each assay run is controlled with negative, positive, and reference compounds (Elvitegravir or Raltegravir) controls.  

  • Determinations are made in triplicate wells and each drug is tested 2 times over several days.  

  • A final report include data from the experiments with tabulated giving mean, standard deviation, percent CV, percent inhibition of the controls and the drug concentrations tested.  In addition, the data is graphed and the IC50 and IC90 concentrations for each drug or compound are reported.

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