SGC0946 is a potent and selective inhibitor of Histone H3-lysine79 (H3K79) methyltransferase DOT1L with an IC50 of 0.3 nM in a radioactive enzyme assay, and over 100-fold selectivity for DOT1L over other histone methyltransferases. In cell studies, SGC0946 reduces H3K79 dimethylation with an IC
50 of 2.6 nM in A431 cells and 8.8 nM in MCF10A cells. SGC0946 was found to selectively kills cells transformed with the MLL-AF9 fusion oncogene in an
in vitro model of leukemia. For full characterization details, please visit the
SGC0946 probe summary on the Structural Genomics Consortium (SGC) website.
SGC0649 is the negative control for the active probe, SGC0946. To request a sample of the negative control from the SGC,
click here.
To learn about other SGC chemical probes for epigenetic targets, visit
sigma.com/sgc