Profiling MT Inhibitors with Transzyme™ Methyltransferase Assay Kits

Methyltransferases are challenging targets from an assay development standpoint because they have low activity, high SAM affinities, and complex acceptor substrate requirements. Profiling inhibitor selectivity across several isoforms is especially challenging as it requires a combination of high sensitivity and the ability to accommodate diverse substrates and widely variable reaction conditions. TheTranscreener® EPIGEN Methyltransferase Assay was developed to meet these needs. It is a universal, mix-and-read assay method with a far red fluorescence polarization readout that is capable of detecting SAH at low nanomolar concentrations. This poster presents results on development of Transzyme MT Assay kits for several protein and DNA methyltransferases including Dot1L, NSD2 and PRMT1 and 3 and their use in selective profiling of MT-focused inhibitor library.