The PI3-K Alpha Inhibitor Screening Service is a competitive assay for the product of the PI3-Kinase reaction, PI(3,4,5)P3. The enzyme used in the service is purified recombinant human p110α/p85α active enzyme and the substrate is diC8 PI(4,5)P2. Duplicate PI3K reactions are performed in the presence of each sample compound provided by the customer. After the PI3K reactions are complete, reaction products are detected using Luminescent Assay for PI3-Kinase Activity ( AlphaScreen® Assay, cat# K-1300).
The full PI3-K Alpha Inhibitor Screening Service is divided into two parts – (Stage 1) screening for potential inhibitors targeting human PI3K p110α/p85α, and (Stage 2) determination of IC50 value for hit compound from stage 1. When testing for inhibition potential in stage 1, a single selected compound concentration (determined by customer, usually a high dose) for all compound samples will be tested. Assay controls include “Positive Reaction control” without compound or inhibitor; “Positive Inhibition controls” with a well known PI3K inhibitor; “Substrate control” without enzyme and inhibitor; and “Compound Interference control” without enzyme. A PI(3,4,5)P3 Standard curve can be included upon request with extra charge. When a sample compound shows inhibition potential (a hit) and further characterization is required, IC50 value of the compound can be determined through compound titration as test service stage 2.
Please refer to the technical data sheet for sample considerations and shipping information. To place an order please call Echelon at 801.588.0455