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C301-3161

Development stage: Preclinical
Lead developer: University of Miami
Modality: Small Molecules

Overview

C301-3161 is a small molecule inhibitor of Lysine Acetyltransferase 2A (KAT2A), also known as GCN5, identified as a synergistic hit in combination with menin inhibitors for the treatment of acute myeloid leukemia (AML). Discovered through an epigenetic drug library screen by researchers at the University of Miami, C301-3161 enhances the anti-leukemic effects of agents like DSP-5336 in KMT2A-rearranged and NPM1-mutant AML cell lines. While the compound exhibits minimal single-agent potency, its epigenetic modulation of KAT2A-dependent pathways sensitizes leukemia cells to menin-MLL complex disruption, offering a potential strategy to overcome resistance in high-risk AML populations.

Other names: KAT2A inhibitor C301-3161KAT-2A inhibitor C301-3161KAT 2A inhibitor C301-3161

Targets

KAT2A (Lysine acetyltransferase 2A)

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