OICR-9429

1801787-56-3

C29H32F3N5O3

DMSO : >= 32 mg/mL (57.60 mM)

Epigenetics

OICR-9429 is a novel small-molecule antagonist of the Wdr5-MLL interaction with IC50 of 5 uM. inhibit proliferation and induce differentiation . target: Wdr5 IC 50: 5 uM In vitro: OICR-9429 inhibit proliferation and induce differentiation in p30-expressing human AML cells. OICR-9429 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. [1] reduce the viability of primary human AML cells with N-terminal C/EBPalpha mutations by about 50% (mean value, n = 8) at 5 uM [2] In vivo:The reference for OICR-9429 to mice (female NOD-SCID) is 3 mg/kg.