LY364947 (LY-364947, HTS 466284, HTS466284)是一种二杂芳基取代的吡唑类化合物,是有效的、ATP竞争性转化生长因子β I型受体激酶(TGFβR-I)抑制剂(IC50: 59 nM),高于对TGFβR-II的选择性。
参考文献
1.Li HY, et al. Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7. J Med Chem. 2006;49(6):2138-2142.
2.Peng SB, et al. Kinetic characterization of novel pyrazole TGF-beta receptor I kinase inhibitors and their blockade of the epithelial-mesenchymal transition. Biochemistry, 2005;44(7):2293-2304.
3.Oka M, et al. Inhibition of endogenous TGF-beta signaling enhances lymphangiogenesis. Blood, 2008;111(9):4571-4579.
4.Naka K, et al. TGF-beta-FOXO signalling maintains leukaemia-initiating cells in chronic myeloid leukaemia. Nature, 2010;463(7281):676-680.
冰袋运输。粉末直接保存于-20℃,有效期2年。建议分装后-20℃避光保存,避免反复冻融。