中文同义词:
HIF-1抑制剂(SYP-5);化合物SYP-5
英文同义词:
SYP-5;SYP5; SYP 5;2-Propen-1-one, 1-(5-hydroxy-2,2-dimethyl-2H-1-benzopyran-6-yl)-3-(2-thienyl)-, (2E)-;SYP-5 >=98% (HPLC)
沸点
502.0±50.0 °C(Predicted)
密度
1.263±0.06 g/cm3(Predicted)
酸度系数(pKa)
7.12±0.40(Predicted)
生物活性
SYP-5 是一种 Hypoxia-inducible factor-1 (HIF-1) 的抑制剂,可抑制肿瘤细胞迁移和侵袭以及肿瘤血管生成。
体外研究
SYP-5 inhibits hypoxia-induced upregulation of HIF-1. SYP-5 inhibits HIF-1 and downstream gene expression in Hep3B and Bcap37 cells. SYP-5 inhibits tumor cell migration and invasion, as well as tumor angiogenesis, which are mediated by suppressing PI3K/AKT- and MAPK/ERK-dependent HIF-1 pathway. The proteins of vascular endothelial growth factor (VEGF) and matrix metalloproteinases (MMP)-2 that are targets of HIF-1, are down-regulated by SYP-5. SYP-5 displays significant inhibition on hypoxia-induced overexpression of VEGF and MMP2 in both cell lines. In the tube formation assay, SYP-5 suppresses angiogenesis induced by hypoxia and VEGF in vitro. SYP-5 also retards the Hep3B and Bcap37 cells migration and invasion induced by hypoxia and FBS. SYP-5 specifically inhibits hypoxic induction of luciferase expression in U251-HRE but not in U251-pGL3.