MM-102

MM-102 is a potent small molecule inhibitor designed to disrupt the protein-protein interaction between Myeloid/Lymphoid or Mixed-Lineage Leukemia 1 (MLL1) and WD Repeat Domain 5 (WDR5). By binding to the WDR5 protein at the MLL1-binding pocket, MM-102 prevents the assembly of the MLL1 core complex, which is essential for its histone H3 lysine 4 (H3K4) methyltransferase activity. This inhibition leads to a reduction in H3K4 trimethylation (H3K4me3) at the promoters of target genes, effectively modulating epigenetic signaling. Originally developed as a chemical probe for MLL-rearranged leukemias, MM-102 has also demonstrated potential in inflammatory conditions such as rheumatoid arthritis by suppressing the expression of pro-inflammatory chemokines (e.g., CCL5, CXCL9, CXCL10, CXCL11) in synovial fibroblasts.