KDM5B-IN-4

KDM5B-IN-4 (compound 11ad) is a novel inhibitor of lysine demethylase 5B (KDM5B), with an IC50 of 0.025 μM for KDM5B. It increases the levels of the substrate H3K4me1/2/3 in PC-3 cells by inhibiting KDM5B. Furthermore, KDM5B-IN-4 induces G2/M phase arrest in PC-3 cells and downregulates proteins in the PI3K/AKT signaling pathway. Additionally, KDM5B-IN-4 reduces tumor volume in mice with minimal organ toxicity.