Highly potent DOT1L methyltransferase inhibitor (Kd
= 0.06 nM, IC50
= 0.3 nM in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells. Inactive at 12 histone methyltransferases and DNMT1. Selectively kills cells transformed with the MLL-AF9 fusion oncogene in an in vitro
model of leukemia; lowers levels of MLL target genes HOXA9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the SGC 0946 probe summary
on the SGC website.
Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Yu et al.