PKM2-IN-13 

PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC₅₀ value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research^[1].

PKM2-IN-13 (compound 7f) (48 h) induces e level of hemolysis around 5% and effectively induces cytotoxicity with an IC₅₀ = 12.29 μM in SCC-9 cell lines and selectively inhibits cancer cell lines (including cancer OSCC cells : SCC-9, SCC-4, SCC-25, primary gingival fibroblast and other cancer cell lines : 4T1, Hep-G2, HCT116, B16-F10 Primary Gingival Fibroblast with IC₅₀s values of 12.29, 7.93, 11.09, 22.77, 7.63, 15.98, 6.72, 4.93 and 22.77 μM^[1].
PKM2-IN-13 (24.58 μM, 0-48 h) exhibits a pronounced inhibition of proliferation, observes disruption of intercellular junctions, membrane blebbing, and subsequent proliferation arrest at 6 h becoming more evident after 12 h in SCC-9 cells ^[1].
PKM2-IN-13 (24.58 μM, 24 and 48 h) induces S-phase arrest at 24 h, subsequently triggers cancer cell death via the intrinsic caspase-dependent apoptotic pathway rather than necroptosis as observed over 12-24 h in SCC-9 cells ^[1].
PKM2-IN-13 (24.58 μM, 12-48 h) result a significant increase in ROS after 12 and 24 h^[1].
PKM2-IN-13 (24.58 μM, 48 h) induces cytotoxicity, which can be protected against by Antioxidant N-acetyl-L-cysteine (NAC) (10 mM) (HY-B0215) for 2 h, suggesting an oxidative mechanism of action^[1].

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

PKM2-IN-13 (100-400 mg/kg, i.p., 14 days) exerts good safety profile and low toxicity in C57BL/6 mice^[1].

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

457.43

C₂₅H₁₉N₃O₆

O=C1C=C(C2=CC=CC=C2O1)OCCCN3C=C(N=N3)COC4=CC(C5=C(C4=O)C=CC=C5)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Ouverney G, et al. Coumarin-1,2,3-Triazole Conjugates as Molecular Scaffolds for the Selective Induction of ROS-Driven Apoptosis in Cancer Cells in the Development of Pyruvate Kinase M2 Inhibitors. ACS Omega. 2025 Dec 9;10(50):61899-61914.  [Content Brief]