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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
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1. 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 cells. J. Med. Chem. 57(19), 7916-7932 (2014).
2. Radiosensitization of head and neck squamous cell carcinoma (HNSCC) by a podophyllotoxin. ACS Med. Chem. Lett. 10(9), 1314-1321 (2019).