PKM2-IN-6 (compound 7d) is a potent and orally active PKM2 inhibitor with an IC50 value of 23 nM. PKM2-IN-6 induces apoptosis and cell cycle arrest at G2 phase. PKM2-IN-6 reduces the level of PKM1 and PKM2 at the mRNA level. PKM2-IN-6 shows anticancer activity and has the potential for the research of triple-negative breast cancer.
PKM2-IN-6 (compound 7d) (0, 20, 40, 60, 80, 100 μM; 48 h) shows cytotoxicity with IC50s of 18.33, 47.00, 19.80 µM for COLO-205, A-549, MCF-7 cells, respectively[1].PKM2-IN-6 (14.38 μM; 48 h) induces apoptosis and cell cycle arrest at G2 phase[1].PKM2-IN-6 (14.38 μM; 24 h) reduces the PKM1 and PKM2 at the mRNA level[1].
PKM2-IN-6 (25, 50 mg/kg; p.o.; daily for 3 weeks) decreases the tumor volume and tumor weight in mice[1].
References:
[1]. Das R, et al. Mechanistic Investigation of Thiazole-Based Pyruvate Kinase M2 Inhibitor Causing Tumor Regression in Triple-Negative Breast Cancer. J Med Chem. 2024 Feb 26.