Discover EZH2 Inhibitors with BellBrook's EZH2 Assay Kits
Numerous studies have shown that histone methyltransferase enhancer of zeste homolog 2 (EZH2) is overexpressed in prostate, breast, bladder, brain, and other tumor types and inhibitors of the enzyme show promise as anti-cancer drugs. EZH2 methyltransferase inhibitors also have shown promise for combating neuropathic pain.
EZH2 is the catalytic component of the polycomb group repressive Complex (PRC2), that selectively methylates histone H3 lysine 27 (H3K27). Reconstituting EZH2 enzyme reactions in vitro is complex, as it requires an optimal combination of five different protein subunits and a specific acceptor substrate. Please see the materials required section below for more on suggested enzyme and substrate combinations.
Universal Detection of SAH to Measure EZH2 Enzymatic Activity
BellBrook Labs has two assays available to measure EZH2 enzyme activity. Both platforms measure SAH produced by EZH2. The EPIGEN SAH FP Assay uses the coupling enzymes to turn SAH into AMP which is then detected by the Transcreener AMP FP Assay. The AptaFluor SAH TR-FRET Assay uses a split aptamer approach, which upon binding to SAH produces a positive TR-FRET readout. To learn more about the differences in assay technology please go to the methyltransferase assays page to determine what assay might be the best fit for your research.