XX-650-23 is a potent CREB inhibitor. XX-650-23inhibits CREB function through disruption of CBP-CREB interaction.XX-650-23 can be used for AML research.
XX-650-23 (870 nM-2.3 μM; 48 hours) inhibits AML cell growth, the IC50 values are 870 nM, 910 nM, 2.0 μM and 2.3 μM for HL-60, KG-1, MOLM-13, and MV-4-11,respectively[1].XX-650-23(5 μM;6 or 24 hours) causes a specific decrease in H3K27 acetylation and is not a general inhibitor of acetyltransferase activity[1].XX-650-23 (2 μM; 72 hours) elicits apoptosis through the intrinsic apoptosis pathway, with activation of caspase-3and detectable caspase-9 cleavage. It also leads to the downregulation of Mcl-1 and bcl-2[1].
References:
[1]. B Mitton, et al. Small molecule inhibition of cAMP response element binding protein in human acute myeloid leukemia cells. Leukemia. 2016 Dec;30(12):2302-2311.