InvivoChem Cat #:V28182CAS #:890190-22-4Purity >=98%Description: WDR5-0103 is a small molecule that binds a peptide-binding pocket on WDR5 (Kd = 450 nM), inhibiting the catalytic activity of the MLL core complex in vitro (IC50 = 39 uM). WD repeat domain 5 (WDR5) plays an important role in various biological functions through the epigenetic regulation of gene transcription. WDR5 may have oncogenic effect and WDR5-mediated H3K4 methylation plays an important role in leukemogenesis.
References: Li DD, Wang ZH, Chen WL, Xie YY, You QD, Guo XK. Structure-based design of ester compounds to inhibit MLL complex catalytic activity by targeting mixed lineage leukemia 1 (MLL1)-WDR5 interaction. Bioorg Med Chem. 2016 Nov 15; 24(22):6109-6118. doi: 10.1016/j.bmc.2016.09.073. Epub 2016 Oct 1. PubMed PMID: 27720555.