NSC 756093 是一种有效的 GBP1:PIM1 相互作用抑制剂。 NSC 756093 可以潜在地恢复对紫杉醇的耐药性。 NSC 756093 可用于卵巢癌研究。
Cas No. | 1629908-92-4 |
Canonical SMILES | O=C1OCC2=C1C(C3=CC=C(C=C3N2CCO)OC)C4=CC=CC=C4 |
分子式 | C20H19NO4 |
分子量 | 337.4 |
溶解度 | DMSO: soluble |
储存条件 | -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | NSC 756093 is an inhibitor of the protein-protein interaction between guanylate binding protein 1 (GBP1) and the serine/threonine kinase Pim-1.1It 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) |