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Apexbio Technology LLC EPZ5676 1380288-87-8 10mM (in 1mL DMSO)
Supplier: Apexbio Technology LLC A41665.1
EPZ5676 (CAS 1380288-87-8) is a selective inhibitor targeting DOT1L a histone methyltransferase responsible for H3K79 methylation Structural studies indicate EPZ5676 occupies the enzyme s S-adenosylmethionine (SAM) binding pocket inducing conformational changes and partial opening beyond the SAM hydrophobic pocket EPZ5676 displays potent inhibitory activity against DOT1L (IC50 0 8 nM) with markedly lower affinity for other methyltransferases In MLL-rearranged leukemia models EPZ5676 reduces H3K79 methylation inhibits MLL fusion target gene expression and induces cytotoxicity in leukemia cell lines harboring MLL translocations
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