HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC 50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC 50 of 17 µM.
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