We now report that PX-478 inhibits HIF-1alpha protein levels and transactivation in a variety of cancer cell lines. Hypoxia-induced vascular endothelial growth factor formation was inhibited by PX-478, whereas baseline levels of vascular endothelial growth factor in …

2008年11月15日 · PX-478 (20 mumol/L) enhanced the radiosensitivity of PC3 cells irradiated under normoxic and hypoxic condition with enhancement factor (EF) 1.4 and 1.56, respectively.

PX-478 is a novel small molecule compound that inhibits the activity of hypoxia inducible factor (HIF)-1 alpha, a transcription factor that controls the expression of a number of genes important for growth and survival of cancer cells.

2022年3月30日 · Because we demonstrated that, under metabolic overload, the HIF-1α inhibitor PX-478 improves β cell function, we investigated the impact of PX-478 treatment in two diabetic mouse models, db/db and STZ-induced diabetic mice.

We show that PX-478 prevents postradiation HIF-1 signaling and abrogates downstream stromal adaptation in C6 and HN5 reporter xenografts as measured by serial ultrasound, vascular magnetic resonance imaging, and hypoxia response element–specific micro–positron emission tomography imaging.

2024年2月15日 · PX-478 effectively reduced HIF-1α levels in T and HeLa cells. While PX-478 exhibited dose-dependent inhibition of antigen-nonspecific T and mesoCAR T cell proliferation, it had minimal impact on antigen-specific mesoCAR T cell proliferation.

2022年3月1日 · PX-478 is a selective inhibitor of HIF1α, which was used to reduce cancer and obesity in animal models. Here, we tested whether PX-478 can be used to inhibit atherosclerosis. We first tested PX-478 in human aortic endothelial cells (HAEC) and found that it significantly inhibited expression of HIF1α and its targets, including Collagen I.

2008年1月17日 · PX-478 was initially identified through a screen for compounds that lowered cellular HIF-1α levels. PX-478 causes marked tumor regression, prolonged delays in tumor growth, and cure of some animals. PX-478 has recently entered phase I clinical trial in patients with advanced cancer.

PX-478 is a small molecule inhibitor of hypoxia inducible factor (HIF)-1 alpha currently in a clinical trial in patients with advanced metastatic cancer and lymphoma. PX-478 was effective in models of both non-small cell lung cancer and small cell lung cancer that express HIF-1 alpha.

2009年11月20日 · Our observations suggest that the novel small molecule HIF-1α inhibitor, PX-478, effectively downregulates HIF-1α protein at low concentrations and induces cell death in DLBCL cells.