Profiling EZH2 Inhibitors with the Transzyme HMT EZH2 Assay Kit
16 September 2015
Numerous studies have shown that histone methyltransferase (HMT) EZH2 is overexpressed in prostate, breast, bladder, brain, and other tumor types and inhibitors of the enzyme recently began clinical testing as anti-cancer drugs. In this Application Note, we describe how compounds can be rapidly profiled for potency as HMT EZH2 inhibitors using the Transzyme HMT EZH2 Assay kit. The Transzyme HM T EZH2 Assay kit combines Transcreener® EPIGEN Methyltransferase Assay detection reagents with purified EZH2 and the optimal substrates and includes batch-specific reaction conditions that yield a Z’ of at least 0.6.