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 -20C. Stable for 12 months at -20C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20C. 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.
Molecular Weight:
618.57
Purity:
~99% (HPLC)
Form:
Supplied as a white solid.
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