OICR-9429

Description: OICR-9429 is a novel, potent and selective antagonist of the interaction of WDR5 with peptide regions of MLL and Histone 3. It inhibits proliferation and induces differentiation in p30-expressing human AML cells. It can cause a significant decrease in viability in the majority of patient cells with mutations in the N-terminal part of the CEBPA gene. OICR-9429 displays exquisite cellular selectivity and specificity in disrupting critical protein-protein interactions between WDR5. It reduces the viability of primary human AML cells with N-terminal C/EBPalpha mutations by about 50% (mean value, n = 8) at 5 uM.

References: Nat Chem Biol. 2015 Aug; 11(8):571-8; J Med Chem. 2016 Mar 24; 59(6):2478-96.