PKM2-IN-12 

PKM2-IN-12 is an orally active PKM2 inhibitor with an IC₅₀ of 10 nM. PKM2-IN-12 inhibits COLO-205 cell proliferation and migration, arrests the cell cycle, and induces apoptosis. PKM2-IN-12 significantly reduces cellular levels of lactate, pyruvate, and ROS. PKM2-IN-12 directly kills cancer cells and restores disrupted gut microbiota balance in mice model. PKM2-IN-12 can be used to study colorectal cancer^[1].

PKM2-IN-12 (Compound 10j) (24 h) shows significant differences in sensitivity in COLO-205, CAL-27 and MCF-7 cells with IC₅₀s of 4.21, 13.3 and 22.34 μM^[1].
PKM2-IN-12 (4.21 μM, 48 h) mainly kills COLO-205 cells by inducing late apoptosis and blocks the cells at the G2 phase^[1].
PKM2-IN-12 (4.21 μM) significantly inhibits the migration ability of COLO-205 cells^[1].
PKM2-IN-12 (4.21 μM, 0-48 h) significantly reduces the levels of lactate, pyruvate and ROS within the COLO-205 cells^[1].
PKM2-IN-12 (4.21 μM, 48 h) increases the expression of PKM2 monomers and tetramers, but did not affect PKM1 in COLO-205 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PKM2-IN-12 (Compound 10j) (50-100 mg/kg, p.o., once every three days for 72 days) effectively inhibits tumor growth in the colitis-associated colorectal cancer (CAC) model and reverses the intestinal flora imbalance in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

465.35

C₂₃H₁₄Cl₂N₄OS

O=C(C1=C(C2=CC=C(Cl)C=C2)N=C(NC3=CC=C(Cl)C=C3)S1)C4=CN=C5C=CC=CN54

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ghosh Chowdhury M, et al. Thiazole-Based Tumor Pyruvate Kinase M2 Inhibitors: A Paradigm-Shifting Therapeutic Strategy Targeting Metabolic and Microbial Synergy in Colorectal Cancer. J Med Chem. 2025 Oct 23;68(20):21786-21806.  [Content Brief]