A selective inhibitor of the interaction of WDR5 with peptide regions of MLL and Histone 3; binds to WDR5 with a Kd = 24-52 nM and disrupts the interaction of WDR5 with MLL1 and RbBP5 in cells at IC50 values below 1 µM

OICR-9429 – 5 mg

Brand:
Cayman
CAS:
1801787-56-3
Storage:
-20
UN-No:
Non-Hazardous - /

WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.{22296} For example, WDR5 is a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3.{20287} WDR5 can also be a component of histone acetyltransferase complexes and can directly bind methylated as well as unmodified histones.{22296,24221} 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.  

 

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Description

A selective inhibitor of the interaction of WDR5 with peptide regions of MLL and Histone 3; binds to WDR5 with a Kd = 24-52 nM and disrupts the interaction of WDR5 with MLL1 and RbBP5 in cells at IC50 values below 1 µM

Formal name: N-(4-(4-methylpiperazin-1-yl)-3′-(morpholinomethyl)-[1,1′-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide

Synonyms: 

Molecular weight: 555.6

CAS: 1801787-56-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Writers|Histone Methylation

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