LY2109761 (LY-2109761; LY 2109761) 是一种TGF-β受体I/II型激酶的小分子抑制剂(IC50 = 69 nM)。已用于研究TGF-β信号通路在胰腺癌细胞系肿瘤细胞迁移和转移过程中的作用,其中5 μM的化合物能完全破坏Smad-2磷酸化,其是激酶的一种直接作用的下游靶点。它还可以抑制人原代纤维细胞中辐射诱导的炎性细胞因子信号传导和促血管生成基因,包括ID1。
参考文献
[1]. Wan X, et al. Effect of transforming growth factor beta (TGF-β) receptor I kinase inhibitor on prostate cancer bone growth[J]. Bone, 2012, 50(3): 695-703.
[2] Melisi, et al. LY2109761, a novel transforming growth factorβreceptor type I and type II dual inhibitor, as a therapeutic approach to suppressing pancreatic cancer metastasis. Molecular CancerTherapeutics 7(4), 829-840 (2008).
[3] Flechsig, P., et al. LY2109761 attenuates radiation-induced pulmonary murine fibrosis via reversal of TGF-β and BMP-associated proinflammatory and proangiogenic signals. Clinical Cancer Research 18(13), 3616-3627 (2012).
冰袋运输。粉末直接保存于-20℃,有效期2年。溶于DMSO。建议分装后-20℃避光保存,避免反复冻融。