BKT300

BKT300 is a first-in-class, potent, and highly selective small molecule inhibitor of Protein Regulator of Cytokinesis 1 (PRC1). Developed by AlonBio (originally by Biokine Therapeutics), it targets PRC1, a scaffold protein essential for cytokinesis and often overexpressed in aggressive tumors. BKT300 binds directly to PRC1 with a dissociation constant (Kd) of 28.3 nM, locking it in a phosphorylated, inactive conformation. This action disrupts actin and microtubule formation, leading to G2/M cell cycle arrest, mitotic catastrophe, and apoptosis via the caspase-3 pathway. Additionally, it downregulates CDC25C, upregulates p21, and inhibits PLK-1 activation. The compound has a molecular weight of 399.33 and a chemical formula of C₂₂H₂₅NO₆. BKT300 is being investigated for various solid and hematological malignancies, including triple-negative breast cancer (TNBC), lung cancer, and leukemia.