PIK3CA (E545K)/PIK3R1 NanoBRET Target Engagement Intracellular Kinase Assay for screening of compounds binding to the target.
MGC142161, MGC142163, p110-alpha, PI3K, PI3K-alpha
HEK293 human epithelial cell line from ATCC
384-well plate format using Promega’s NanoBRET TE Intracellular Kinase Assay
HEK293 cells transiently co- expressing NanoLuc- PIK3CA(E545K) Fusion Vector and PIK3R1 Expression Vector were seeded into the wells of 384-well plates. The cells were pre-treated with the NanoBRET Tracer K-3 and then treated with reference compound PI-103 for 1 hour. The BRET signal was measured on an Envision 2104 Multilabel Reader. IC50 value was calculated and IC50 curve was plotted using the GraphPad Prism program based on a sigmoidal dose response equation.
Binding of compound to target kinase
Malvern, PA, USA
More information can be found on our website NanoBRET Target Engagement Intracellular Kinase Assay Services
Reference compound IC50 for PIK3CA (E545K)/PIK3R1