Potent DOT1L methyltransferase inhibitor (KD = 0.06nm, IC50 = 0.3nm in a radioactive assay); blocks H3K79 methylation in A431 cells and MCF10A cells (IC50 values are 2.65 and 8.8nm respectively). 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 and Meis1.
Sequence:C28H40BrN7O4
Solubility:DMSO (~100mM), Ethanol (~100mM)
Molecular Weight:~618.57
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.