9-ING-41是一种ATP竞争性的GSK-3β选择性抑制剂,IC50为0.71 μM,具有广泛的抗肿瘤活性,在啮齿动物中有良好耐受性。9-ING-41在细胞分裂前期靶向中心体和结合微管的GSK3β诱导细胞周期停滞和凋亡。FDA已授予9-ING-41孤儿药身份,用于治疗神经母细胞瘤,批准了9-ING-41用于人体I期/II期临床试验。
参考文献
1Irina N Gaisina, et al. From a natural product lead to the identification of potent and selective benzofuran-3-yl-(indol-3-yl)maleimides as glycogen synthase kinase 3beta inhibitors that suppress proliferation and survival of pancreatic cancer cells. J Med Chem. 2009 Apr 9;52(7):1853-63.
2.Wu X, et al. Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma. Blood. 2019 Jul 25;134(4):363-373.
3.Hiroo Kuroki, et al. 9-ING-41, a small molecule inhibitor of GSK-3beta, potentiates the effects of anticancer therapeutics in bladder cancer. Sci Rep. 2019 Dec 27;9(1):19977.
4.Ugolkov AV, et al. 9-ING-41, a small-molecule glycogen synthase kinase-3 inhibitor, is active in neuroblastoma. Anticancer Drugs. 2018 Sep;29(8):717-724.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。