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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Angiogenesis>HIF inhibitor>PX-478
PX-478
  • PX-478

PX-478 NEW

Price $48 $81 $139
Package 2mg 5mg 10mg
Min. Order:
Supply Ability: 10g
Update Time: 2025-07-15

Product Details

Product Name: PX-478 CAS No.: 685898-44-6
Supply Ability: 10g Release date: 2025/07/15

Product Introduction

Bioactivity

NamePX-478
DescriptionPX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
Cell ResearchPX-478 is prepared as a 10 mM stock in distilled water and used immediately[1]. To determine the effect of PX-478 in combination with radiation, cells are treated with PX-478 for 24 hr under normoxic condition, irradiated and plated after 1 hr. Colonies are stained with crystal violet after 12 days and the colonies of >50 cells are counted. For combination treatments, net survival is calculated by correcting the toxicity of PX-478 alone. Enhancement factor (EF) is calculated by dividing the dose of radiation required to reduce plating efficiency to 10% when cells are treated with radiation alone by the dose of radiation required to reduce plating efficiency to 10% when cells are treated with PX-478 and radiation[1].
In vitroMETHODS: Tumor cells MCF-7, HT-29 and PC-3 were treated with PX-478 under normoxic or hypoxic conditions for 16 h, and then grown under normoxic conditions for another 56 h. Cell viability was detected by MTT assay. RESULTS: PX-478 produced a smaller but significantly greater inhibition of cell growth under hypoxic conditions compared to normoxic conditions. the hypoxic/normoxic IC50 of MCF-7 cells was 25.1/20.0 μM, with a ratio of 1.25. the hypoxic/normoxic IC50 of HT-29 cells was 29.5/23.9 μM, with a ratio of 1.20, and that of PC-3 cells was 16.2/11.9 μM, with a ratio of 16.2/11.0 μM. IC50 for PC-3 cells was 16.2/11.1 μM with a ratio of 1.45. [1] METHODS: Human prostate cancer cells PC3 and DU 145 were treated with PX-478 (10-40 μM) under normoxic conditions for 20 h. The expression levels of target proteins were detected by Western Blot. RESULTS: Under normoxic conditions, the IC50 of PX-478 for HIF-1α inhibition in PC3 cells was 20-25 μM (ΔHIF:0.56±0.08), while the IC50 of HIF1α inhibition in DU 145 cells was 40-50 μM (ΔHIF:0.47±0.08). [2]
In vivoMETHODS: To study the activity on metabolism in vivo, PX-478 (5 mg/kg) was administered by gavage to C57BL/6 mice on a high-fat diet (HFD) every two days for seven weeks. RESULTS: PX-478 treatment effectively inhibited HFD-induced HIF1α activation in adipose tissue. Inhibition of HIF1α in adipocytes significantly improved metabolism. [3] METHODS: In order to detect the anti-tumor activity in vivo, PX-478 (75-100 mg/kg) was intraperitoneally injected into scid mice carrying tumors OvCar-3, SHP-77, MCF-7, or PC-3 once a day for five days. RESULTS: PX-478 showed antitumor activity against established human tumor xenografts. [4]
Storagestore under nitrogen,keep away from moisture,store at low temperature | -20°C for 1 year | Shipping with blue ice.
Solubility InformationDMSO : 50 mg/mL (126.86 mM), Sonication is recommended.
H2O : 88.81 mM, Sonication is recommended.
KeywordsPX-478 | PX478 | PX 478 | HIFProlylHydroxylase | HIF-1α | HIF/HIFProlylHydroxylase | HIF/HIF Prolyl-Hydroxylase | HIF/HIF ProlylHydroxylase | HIF Prolyl-Hydroxylase | HIF ProlylHydroxylase | HIF | Autophagy
Inhibitors RelatedStavudine | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Valproic Acid | Curcumin | Hydroxycitric acid tripotassium hydrate | Paeonol | Naringin | Alginic acid | Gefitinib
Related Compound LibrariesBioactive Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Metabolism Compound Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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