PKM2/PDK1-IN-1

PKM2/PDK1-IN-1

• CAS Number: 3041957-90-5
• UNSPSC Description: 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].
• Target Antigen: Akt; Apoptosis; EGFR; PDK-1; Pyruvate Kinase
• Type: Reference compound
• Related Pathways: Apoptosis;JAK/STAT Signaling;Metabolic Enzyme/Protease;PI3K/Akt/mTOR;Protein Tyrosine Kinase/RTK
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/pkm2-pdk1-in-1.html
• Solubility: 10 mM in DMSO
• Smiles: 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
• Molecular Weight: 697.92
• References & Citations: [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.
• Shipping Conditions: Room temperature
• Clinical Information: No Development Reported