lunresertib (RP-6306)

RP-6306 is a selective inhibitor of PKMYT1 (Protein Kinase Membrane-Associated Tyrosine/Threonine 1), a key regulator of cell cycle progression. It was identified from patent WO2021195781A1 as compound 182. PKMYT1 is part of the DNA damage response pathway and plays a role in controlling the G2/M checkpoint, particularly in cells with disrupted cell cycle regulation, such as cancer cells. By inhibiting PKMYT1, RP-6306 can induce mitotic catastrophe and cell death in cancer cells, especially those with CCNE1 amplification or other dependencies on the G2/M checkpoint.