85-2074-42　Menin-MLL Interaction Inhibitor, MI-2-2 (MI22, 4-(4-(5,5-Dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidine, HCl) 10mg　217541

特徴

• 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 4°C. For long-term storage, aliquot and store at 4°C. 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.