PKM2/PDK1-IN-1 

PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway^[1].

PKM2, PDK-1^[1]

PKM2/PDK1-IN-1 (compound E5) (0.5-4 μM; 24 h) shows a synergistic anticancer effects with Gefitinib (HY-50895)^[1].
PKM2/PDK1-IN-1 (0.5 μM; 24 h) regulates the apoptotic proteins of both mitochondrial and death receptor pathway^[1].
PKM2/PDK1-IN-1 (0.5 μM, 1 μM; 24 h) causes the mitochondria transmembrane potential (ΔΨm) dissipation and intracellular ROS accumulation in lung cancer cells^[1].
PKM2/PDK1-IN-1 (1 μM, 2 μM; 24 h) inhibits PDK1 and enhances the downstream PDH activity in H1975 cells^[1].
PKM2/PDK1-IN-1 inhibits intracellular NADPH concentration and increases ATP production of H1975 cells^[1].

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

PKM2/PDK1-IN-1 (compound E5) (2.4 mg/kg, 4.8 mg/kg; 6 times in 2 days) suppress the growth of H1975 xenograft tumor in nude mice in vivo with low toxic side effects^[1].

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

697.92

C₃₆H₄₃NO₇S₃

3041957-90-5

COC([C@@H](NC(CCCC[C@@H]1CCSC(S1)C2=C(C=CC=C2)C)=O)CS[C@@H](C3=CC(C4=C(C=CC(O)=C4C3=O)O)=O)C/C=C(C)\C)=O

Room temperature in continental US; may vary elsewhere.

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

• [1]. Lin H, et al. PKM2/PDK1 dual-targeted shikonin derivatives restore the sensitivity of EGFR-mutated NSCLC cells to gefitinib by remodeling glucose metabolism. Eur J Med Chem. 2023 Mar 5;249:115166.  [Content Brief]