PX-478 | HIF-1α抑制剂 | MCE - MCE-生物活性分子大师
pc3 和 du 145 细胞表达 hif-1α 蛋白，在常氧条件下用 px-478 处理 20 小时。与 du 145 细胞相比，pc3 细胞对 px-478 更敏感。光密度分析表明，在常氧条件下，pc3 细胞抑制 hif-1α 的 ic 50 为 20-25 μm，而 du 抑制 hif-1α 的 ic 50 145 个细胞为 40-50 μm。pc3 和 du 145 细胞在常氧或 ...
Molecular mechanisms for the activity of PX-478, an antitumor
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 …
PX-478 (PX-478) - 药物靶点：HIF-1α_在研适应症：弥漫性大B细 …
PX-478, targeting HIF-1α, was administered intravaginally. The analysis of fibroblasts, macrophage and inflammation was performed through Masson staining, immunofluorescence, and ELISA. Collagen distribution was assessed using Sirius Red staining.
PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances ...
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. The drug was less effective in inhibiting HIF-1alpha and enhancing radiosensitivity of DU 145 cells compared to PC3 cells with EF 1.13 (normoxia) and 1.25 (hypoxia) at 50 mumol/L ...
HIF-1α inhibitor PX-478 preserves pancreatic β cell function in ...
2022年3月30日 · In response to PX-478 treatment, human islet organoids chronically exposed to high glucose presented improved stimulation index of glucose-induced insulin secretion. These results suggest that the HIF-1α inhibitor PX-478 has the potential to act as an antidiabetic therapeutic agent that preserves β cell function under metabolic overload.
PX-478: Uses, Interactions, Mechanism of Action - DrugBank Online
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.
Hypoxia inducible factor 1α inhibitor PX-478 reduces
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.
PX-478, a Novel Small Molecule Inhibitor of Hypoxia
2009年11月20日 · PX-478 is a novel small molecule inhibitor of HIF-1α being developed for the treatment of cancer. We treated several DLBCL cell lines (SUDHL4, SUDHL6, and SUDHL10) with increasing concentrations (2–25μM) of PX-478 for 4 hours followed by 20-hour incubation under normoxic (5% oxygen) or hypoxic (1.5% oxygen) conditions.
Px-478 | C13H20Cl4N2O3 | CID 11234794 - PubChem
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.
PX-478 2HCl | HIF-1α inhibitor | CAS NO.:685898-44-6 - GlpBio
PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels. PX-478 inhibits HIF-1α at multiple levels including inhibition of HIF-1α translation and reduction in HIF-1α mRNA levels. [1] PX-478 also has been shown antitumor activity against several aggressive human tumor xenografts. [2]
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