OICR-9429

OICR-9429 is a potent antagonist of the interaction that WDR5 effect with peptide regions of MLL and Histone 3. It reduces the viability of acute myeloid leukemia cells in vitro.

OICR-9429-N-C2-NH2, a ligand for WDR5, intermediate 2, serves as a crucial compound in the synthesis of PROTACs.

Dimethyl-F-OICR-9429-COOH, a ligand for WD40 repeat domain protein 5 (WDR5). This compound is utilized as a key component in the synthesis of PROTACs.

WDR5-IN-6 is a WDR5 inhibitor targeting the WBM locus and is highly synergistic with OICR-9429, a WDR5 inhibitor that targets the WIN locus. It exhibits potent antitumor activity and inhibits cell proliferation in neuroblastoma cell lines, making WDR5-IN-6 suitable for neuroblastoma research.

OICR-0547 is a closely related derivative of OICR-9429. OICR-9429 is a novel small-molecule Wdr5-MLL interaction antagonist.

OICR41114 (PROTAC4) is a PROTAC degrader targeting WDR5. It effectively degrades endogenous WDR5 with an EC50 of 40 nM and a Dmax of 49%. The degradation of HiBiT-tagged WDR5 by OICR41114 occurs in a proteasome-dependent manner. This compound is composed of a target protein ligand, Dimethyl-F-OICR-9429-COOH, an E3 ligase ligand, OICR-8268-acrylic acid, and a PROTAC linker, Amino-PEG9-amine. Notably, the conjugate of the E3 ligase ligand and the linker is OICR-8268-acrylic acid-amino-PEG9-amine.