OICR-9429

WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones. For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3. WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones. 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 = Structural Genomics Consortium (SGC). The negative control, OICR-0547, for OICR-9429 is also available exclusively through the SGC. You can submit a request to receive the negative control here.Formal Name: N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide. CAS Number: 1801787-56-3. Molecular Formula: C29H32F3N5O3. Formula Weight: 555.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: .5 mg/ml (with gentle warming), Methanol: .5 mg/ml (with gentle warming). lambdamax: 259 nm. SMILES: O=C(C1=CNC(C=C1C(F)(F)F)=O)NC2=CC(C3=CC(CN4CCOCC4)=CC=C3)=CC=C2N5CCN(C)CC5. InChi Code: InChI=1S/C29H32F3N5O3/c1-35-7-9-37(10-8-35)26-6-5-22(21-4-2-3-20(15-21)19-36-11-13-40-14-12-36)16-25(26)34-28(39)23-18-33-27(38)17-24(23)29(30,31)32/h2-6,15-18H,7-14,19H2,1H3,(H,33,38)(H,34,39). InChi Key: DJOVLOYCGXNVPI-UHFFFAOYSA-N.