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Apexbio Technology LLC EPZ004777 1338466-77-5 10mM (in 1mL DMSO)
Supplier: Apexbio Technology LLC A41705.1
EPZ004777 (CAS 1338466-77-5) is a selective small-molecule inhibitor targeting DOT1L a histone H3K79 methyltransferase involved in leukemogenesis It inhibits DOT1L enzymatic activity with an IC50 of approximately 400 pM in radiometric assays EPZ004777 selectively reduces viability in leukemia cell lines harboring MLL rearrangements such as MV4-11 (MLL-AF4) and MOLM13 (MLL-AF9) Additionally treatment with EPZ004777 attenuates Hoxa9 and Meis1 mRNA expression and exhibits inhibitory activity (IC50 range 0 1 1 M) against cells transformed by MLL-AF10 and CALM-AF10 oncogenes Overall EPZ004777 serves as a valuable tool for studying DOT1L-mediated epigenetic regulation and leukemic pathogenesis
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