NSC 756093 is an inhibitor of the protein-protein interaction between guanylate binding protein 1 (GBP1) and the serine/threonine kinase Pim-1.1 It binds to GBP1-Pim-1 (Kd = 38 nM) and inhibits the interaction by 65% when used at a concentration of 100 nM. NSC 756093 enhances radiation-induced cytotoxicity in FaDu hypopharyngeal carcinoma cells (IC50 = 496 nM), as well as induces apoptosis and cell cycle arrest at the G2/M phase in the same cells.2
1.Andreoli, M., Persico, M., Kumar, A., et al.Identification of the first inhibitor of the GBP1:PIM1 interaction. Implications for the development of a new class of anticancer agents against paclitaxel resistant cancer cellsJ. Med. Chem.57(19)7916-7932(2014) 2.Resendez, A., Tailor, D., Graves, E., et al.Radiosensitization of head and neck squamous cell carcinoma (HNSCC) by a podophyllotoxinACS Med. Chem. Lett.10(9)1314-1321(2019)