PKMYT1-IN-10 is a selective PKMYT1 inhibitor with an IC50 of 3 nM. It suppresses colony formation, induces apoptosis, and causes cancer cell cycle arrest in the S phase. This compound exhibits excellent hepatic microsomal and plasma stability with minimal inhibition of CYPs. PKMYT1-IN-10 is applicable for research in ovarian and breast cancer.

PKMYT1:3 nM

PKMYT1-IN-10 (Compound A30) demonstrates potent cellular inhibitory activity, with IC50 values of 0.32 μM, 0.33 μM, and > 8 μM in OVCAR3, HCC1569, and A549 cell lines, respectively. At concentrations of 0.125-2 μM over 14 days, it inhibits colony formation in OVCAR3 and HCC1569 cells, with EC50 values of 0.37 and 0.35 μM, respectively. Additionally, PKMYT1-IN-10 at 0.3-2.4 μM over 5 days can induce apoptosis in HCC1569 cells and cause S phase-specific cell cycle arrest in both HCC1569 and OVCAR3 cells. In combination with Gemcitabine, PKMYT1-IN-10 (37.5-600 nM) shows a highly synergistic effect, with combination index (CI) values of < 0.5 and 0.5-0.8 in HCC1569 and OVCAR3 cells, respectively.