A cell-permeable thienopyrimidine compound that competes against MLL (Mixed Lineage Leukemia) for menin binding (IC50 = 46 and 520nM, respectively, against MBM1 sequence MLL4-15 and MLL4-43 containing both MBM1 & MBM2) by targeting menin MLL-binding pocket with high affinity (KD = 22nM), effectively disrupting cellular menin and MLL-AF9 fusion interaction (by >90% at 12uM in MLL-AF9-expressing HEK293 cells). Shown to inhibit the oncogenic proliferation of four MLL translocation-harboring human leukemia cell lines (by >95% in 12 d at 6uM), but not non-MLL leukemia Kasumi-1 and HAL-01 lines (16% inhibition at 12uM), by downregulating MLL target genes expression via simultaneous hematopoietic differentiation induction and killing of non-differentiated population. Formula: C17H20F3N5S2 HCl Solubility: DMSO Primary Target: Menin Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
Purity:
99% (HPLC)
Form:
Supplied as an off-white powder.
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