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MLL-r

" in MedChemExpress (MCE) Product Catalog:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-114410

    Mitochondrial Metabolism Cancer
    CCI-006 is a selective inhibitor and chemosensitizer of MLL-rearranged leukemia cells, by inhibits mitochondrial respiration resulting in insurmountable mitochondrial depolarization and a pro-apoptotic unfolded protein response (UPR) in a subset of MLL-r leukemia cells .
    CCI-006
  • HY-136175
    Revumenib
    10+ Cited Publications

    SNDX-5613

    Epigenetic Reader Domain Cancer
    Revumenib (SNDX-5613) is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. Revumenib can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML) .
    Revumenib
  • HY-122698

    Apoptosis Cancer
    CCI-007 is a small molecule with cytotoxic activity against infant leukemia with MLL rearrangements, with IC50 values of 2.5-6.2 μM in sensitive cells .
    CCI-007
  • HY-173422

    PROTACs Histone Methyltransferase Cancer
    MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .
    MS2133
  • HY-114162B

    Epigenetic Reader Domain Apoptosis Cancer
    VTP50469 mesylate is a potent, and selective Menin-MLL1 inhibitor that effectively targets MLL-rearranged and NPM1c+ leukemia. VTP50469 mesylate selectively kills cell lines with MLL rearrangements and NPM1c+ mutations. VTP50469 mesylate displaces Menin from protein complexes and inhibits MLL's chromatin occupancy at specific genes, leading to significant changes in gene expression, differentiation, and apoptosis. VTP50469 demonstrates dramatic reductions in leukemia burden in patient-derived xenograft models of MLL-r acute myeloid leukemia and MLL-r acute lymphoblastic leukemia, with some mice remaining disease-free for over a year post-treatment.
    VTP50469 mesylate
  • HY-178172

    Histone Methyltransferase c-Myc Epigenetic Reader Domain HOXA Cancer
    AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia .
    AF9/ENL-DOT1L PPI-IN-1
  • HY-168082

    Histone Methyltransferase Cancer
    Dot1L-IN-8 (Compound 15) is a potent Dot1L inhibitor. Dot1L-IN-8 inhibits HL-60, K562, MV4-11, HH, and KG-1 cells vitality with IC50s of 0.45, 1.03, 0.68, 1.66, and 1.12 μM, respectively .
    Dot1L-IN-8

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