XX-650-23 is a small molecule inhibitor of CREB, blocks CREB/CBP interaction (IC50=3.2 uM) and disrupts CREB-driven gene expression; suppresses AML cell lines growth with IC50 of 0.87-2.3 uM, specifically disrupts CREB-driven transcription, induces apoptosis and cell-cycle arrest; significantly increases survival of cell line- and patient-derived xenograft mice with no toxicity to normal hematopoietic cells or animals.
A small-molecule antagonist of CREB-CBP interaction, inhibits the cAMP-dependent activation of cellular genes via CREB; disruptes phospho (Ser-133) CREB binding to CBP KIX domain with Ki of 90 uM, similar Ki for binding of phospho (Ser-133) CREB protein to p300; also interferes with the Myb-KIX interaction in vitro and inhibits Myb activity in vivo.
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