KDM5c70

KDM5c70 is a small molecule inhibitor specifically targeting the KDM5 family of histone lysine demethylases, including KDM5A, KDM5C, and KDM5D. It is primarily utilized as a research tool to investigate the epigenetic dysregulation associated with IDH-mutant cancers, such as acute myeloid leukemia (AML) and glioma. By inhibiting KDM5 enzymes, KDM5c70 leads to an enrichment of H3K4 trimethylation (H3K4me3) at specific genomic sites, effectively mimicking the biochemical effects of the oncometabolite R-2-hydroxyglutarate (R-2HG). In experimental models, treatment with KDM5c70 has been shown to induce cytokine independence in TF-1 leukemia cells and promote colony formation in normal human astrocytes, suggesting that KDM5 inhibition plays a critical role in cellular transformation and tumorigenesis driven by IDH mutations.