Product Name: OICR-9429
OICR-9429 Chemical Structure
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OICR-9429 is a cell penetrant, potent and selective antagonist of the interaction of WDR5 (WD repeat domain 5) with peptide regions of MLL and Histone 3 that potently binds to WDR5. OICR-9429 inhibits the interaction of WDR5 with MLL1 and RbBP5 in cells. WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.1 For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.2 WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.1,3 OICR-9429 is a chemical probe that inhibits the interaction of WDR5 with peptide regions of MLL and Histone 3, demonstrating >100-fold selectivity over other chromatin reader domains, methyltransferases, and other non-epigenetic targets. It selectively binds to WDR5 (Kd = 24-52 nM) and disrupts its interaction with MLL1 and RbBP5 in cells (IC50 = <1 µM).
Mol. Formula: C29H32F3N5O3
Storage Conditions: 2ºC to 8 ºC, or -20ºC for 2 years.
IUPAC/Chemical name: N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide
SMILES code: O=C(C1=CNC(C=C1C(F)(F)F)=O)NC2=CC(C3=CC(CN4CCOCC4)=CC=C3)=CC=C2N5CCN(C)CC5
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