2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK Autophagy
  3. HIF/HIF Prolyl-Hydroxylase VEGFR Autophagy
  4. PX-478 free base

PX-478 free base is a multifunctional HIF-1α inhibitor with properties including radiosensitization, autophagy activation, and lipid accumulation inhibition. PX-478 free base also blocks hypoxia-induced VEGF production and regulates β-cell phenotypes under hypoxic conditions. PX-478 free base induces cell cycle arrest and DNA damage, restores autophagic function, reduces foam cell formation, and maintains glucose homeostasis. PX-478 free base is widely used in research on related diseases such as human tumors (e.g., prostate cancer), type 2 diabetes, and atherosclerosis.

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CAS No. : 685847-78-3

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PX-478 free base Related Antibodies

Top Publications Citing Use of Products

96 Publications Citing Use of MCE PX-478 free base

WB
IHC
Cell Migration/Invasion Assay
IF

    PX-478 free base purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 May 12;43(5):937-954.e9.  [Abstract]

    IHC of MT2A in HCT116-bearing mice treated with ES + Cu (0.25 mg/kg, per day, i.p.) and PX-478 (20 mg/kg per day, i.p.).

    PX-478 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681.  [Abstract]

    Control and ASH1L-F3-overexpressing LNCaP cells were treated with Vehicle (Veh) or HIF-1α inhibitors LW6 (15 μM), 2-MeOE2 (2-ME, 25 μM), or PX-478 (20 μM) for 48 h in the presence of CoCl2 (200uM), followed by migration assays. n = 3 biological replicates per group. Scale bar = 1000 μm.

    PX-478 free base purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 20;16(1):4681.  [Abstract]

    PX-478 (40 mg/kg; i.p.; thrice weekly for three weeks) abrogates the significant inhibition of intraosseous tumor growth induced by ASH1L knockdown in C57BL/6J mice.

    PX-478 free base purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2020 Apr 8;12(538):eaay1620.  [Abstract]

    Representative pimonidazole staining of kidney sections from 16-week-old MRL/lpr mice treated with PBS or PX-478, and quantification of pimonidazole-positive cortical tubular cells.

    PX-478 free base purchased from MedChemExpress. Usage Cited in: Front Immunol. 2018 Jul 23:9:1667.  [Abstract]

    Manipulation of the protein level of hypoxia-inducible factor 1 alpha (HIF-1α) in NR8383. 50 µM PX478 treatment for 20 h is used to downregulate the HIF-1α protein level in NR8383 cells (A). 1 mM DMOG treatment for 8 h is used to upregulate the HIF-1α protein level in NR8383 cells (B).

    View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

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    HIF-1α HIF PHD1

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    Description

    PX-478 free base is a multifunctional HIF-1α inhibitor with properties including radiosensitization, autophagy activation, and lipid accumulation inhibition. PX-478 free base also blocks hypoxia-induced VEGF production and regulates β-cell phenotypes under hypoxic conditions. PX-478 free base induces cell cycle arrest and DNA damage, restores autophagic function, reduces foam cell formation, and maintains glucose homeostasis. PX-478 free base is widely used in research on related diseases such as human tumors (e.g., prostate cancer), type 2 diabetes, and atherosclerosis[1][2][3][4].

    IC50 & Target[1]

    HIF-1α

     

    In Vitro

    PX-478 free base (25 μM; 16 h) inhibits HIF-1α translation in human breast cancer MCF-7 cells under both normoxic and hypoxic conditions, with a more pronounced effect under hypoxic conditions; it also reduces global protein synthesis (especially under hypoxic conditions), yet does not alter the phosphorylation levels of hypoxia-induced translation pathway components eIF2α and 4E-BP, and suppresses the reporter gene activity driven by the 5'-UTR of HIF-1α and c-Myc[1].
    PX-478 free base (20-50 μM; 20 h) inhibits HIF-1α protein in human prostate cancer cell lines PC3 and DU 145. Its activity in PC3 cells (with an IC50 of 20-25 μM under normoxic conditions) is stronger than that in DU 145 cells (with an IC50 of approximately 40-50 μM under normoxic conditions), and it also attenuates hypoxia-induced HIF-1α accumulation in both cell lines[2].
    PX-478 free base (16-35 μM; 18-20 hr) reduces the clonogenic survival rate of PC3 and DU 145 human prostate cancer cells; PC3 cells show higher sensitivity under normoxic conditions (IC50 17 μM), while the sensitivity of DU 145 cells increases under hypoxic conditions (IC50 22 μM)[2].
    PX-478 free base (15-20 μM; 24 hr) enhances the radiosensitivity of human PC3 prostate cancer cells under normoxic irradiation conditions, with an enhancement factor (EF) of 1.44 at 20 μM (24 hr incubation) and 1.19 at 15 μM (24 hr incubation)[2].
    PX-478 free base (20-30 μM; 20 hr) enhances the radiosensitivity of hypoxic-irradiated human prostate cancer PC3 cells, with an enhancement factor (EF) of 1.56 at 20 μM (pretreated under normoxic conditions for 20 hours) and 1.78 at 30 μM (pretreated under normoxic conditions for 20 hours)[2].
    Treatment with PX-478 free base (10-50 μM; 24 hr) induces S/G2M phase arrest in the human prostate cancer cell line PC3, but exerts no significant effect on the cell cycle distribution of the human prostate cancer cell line DU 145[2].
    PX-478 free base (20 μM; 30 min-18 hr) induces sustained phosphorylation of γH2AX (a marker of DNA double-strand breaks) in human prostate cancer cell lines PC3 and DU 145, and prolongs radiation-induced γH2AX expression in PC3 cells even after only a short (30 min) treatment[2].
    PX-478 free base improves pancreatic β-cell function in islets of mice with glucose metabolism disorders by inhibiting abnormal low-glucose intracellular Ca2+ oscillations and excessive basal insulin release[3].
    PX-478 free base (100 μM; 48 h) restores autophagic function, inhibits ferroptosis and reduces lipid accumulation in ox-LDL-induced THP-1 macrophage foam cells by downregulating HIF-1α, and these effects depend on intact autophagy[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PX-478 free base Related Antibodies

    Western Blot Analysis[2]

    Cell Line: PC3 and DU 145 human prostate carcinoma cells
    Concentration: 20 μM (20 hr normoxia pretreatment followed by 1 hr hypoxia, PC3 cells); 50 μM (20 hr normoxia pretreatment followed by 1 hr hypoxia, DU 145 cells)
    Incubation Time: 20 hr (normoxia); 20 hr normoxia pretreatment followed by 1 hr hypoxia
    Result: Inhibited HIF-1α protein with an IC50 of 20-25 μmol/L in PC3 cells under normoxia.
    Inhibited HIF-1α protein with an IC50 of ~40-50 μmol/L in DU 145 cells under normoxia.
    Reduced hypoxia-induced HIF-1α accumulation by 40% in PC3 cells treated with 20 μM.
    Reduced hypoxia-induced HIF-1α accumulation by 35% in DU 145 cells treated with 50 μM.

    Cell Viability Assay[2]

    Cell Line: PC3 and DU 145 human prostate carcinoma cells
    Concentration: 17 μM (20 hr normoxia, PC3 cells); 35 μM (20 hr normoxia, DU 145 cells); 16 μM (18 hr hypoxia, PC3 cells); 22 μM (18 hr hypoxia, DU 145 cells)
    Incubation Time: 18-20 hr (normoxia or hypoxia)
    Result: Achieved an IC50 of 17 μmol/L for clonogenic survival in PC3 cells under normoxia.
    Achieved an IC50 of 35 μmol/L for clonogenic survival in DU 145 cells under normoxia.
    Achieved an IC50 of 16 μmol/L for clonogenic survival in PC3 cells under hypoxia.
    Achieved an IC50 of 22 μmol/L for clonogenic survival in DU 145 cells under hypoxia.
    Increased sensitivity of DU 145 cells to PX-478 under hypoxia compared to normoxia.

    Cell Viability Assay[2]

    Cell Line: PC3 and DU 145 human prostate carcinoma cells
    Concentration: 20 μM
    Incubation Time: 30 min; 18 hr
    Result: Increased γH2AX foci and protein levels in both cell lines when used alone, with the effect persisting at 24 hr after drug removal.
    Resulted in significantly higher γH2AX foci and protein levels at 24 hr post-irradiation in PC3 cells when combined with radiation compared to radiation alone.
    Increased γH2AX foci in irradiated PC3 cells at 24 hr post-irradiation even after 30-min exposure compared to radiation alone.
    Resulted in γH2AX levels comparable to PX-478 alone at 24 hr post-irradiation in DU 145 cells when combined with radiation.

    Cell Viability Assay[4]

    Cell Line: ox-LDL-induced THP-1 macrophage foam cells
    Concentration: 100 μM
    Incubation Time: 48 h
    Result: Counteracted the increase in MitoROS-positive cells induced by ox-LDL.
    Restored the reduced protein aggregation and expression levels of GPX4 and LC3II.
    Increased autophagosome numbers.
    Alleviated mitochondrial shrinkage.
    Attenuated the upregulation of HIF-1α protein.
    Reduced elevated iron content.
    Reversed decreased GSH concentration.
    Significantly reduced intracellular lipid accumulation.
    Had all its effects abrogated by co-treatment with autophagy inhibitor 3-MA.
    In Vivo

    PX-478 exhibits potent antitumor activity against HIF-1A-expressing human tumor xenografts in vivo in immunodeficient mice, inducing marked tumor regression, prolonged tumor growth delays, and cures in some animals[1].
    PX-478 (free base) exhibits in vivo antitumor activity against human tumor xenografts, with activity positively correlated with tumor HIF-1α levels and primary activity attributed to inhibition of glycolysis via prolonged Glut-1 reduction[2].
    PX-478 (free base) (daily; 5 days) causes neutropenia as the primary acute toxicity in nonimmunodeficient C57BL/6 mice[2].
    PX-478 (free base) prevents glycemia elevation and diabetes progression by sustaining elevated plasma insulin concentrations in db/db mice[3].
    PX-478 (free base) improves glucose homeostasis recovery and enhances multiple markers of pancreatic β cell function and maturity in streptozotocin-induced diabetic mice[3].
    PX-478 (5 mg/kg; i.p.; once every two days; two months) reduces atherosclerotic plaque, lipid lesion, and mucin areas by downregulating HIF-1α expression in HFD-fed ApoE-/- mice[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Apolipoprotein E knockout (ApoE-/-) (C57BL/6 background, 4-weeks-old, fed high-fat diet for five months)[4]
    Dosage: 5 mg/kg
    Administration: i.p.; once every two days; two months
    Result: Reduced relative plaque area, relative lipid lesion area, and relative mucin area in the aortic sinus compared to untreated high-fat diet-fed ApoE-/- mice.
    Reduced enhanced fluorescence intensity of HIF-1α in high-fat diet-fed mice.
    Significantly downregulated aortic HIF-1α protein expression compared to untreated high-fat diet-fed ApoE-/- mice.
    Molecular Weight

    321.20

    Formula

    C13H18Cl2N2O3
    CAS No.
    SMILES

    ClCC[N+](C1=CC=C(C=C1)C[C@H](N)C(O)=O)([O-])CCCl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
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    PX-478 free base Related Classifications

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    Keywords:

    PX-478685847-78-3PX478PX 478HIF/HIF Prolyl-HydroxylaseVEGFRAutophagyHypoxia-inducible factorsHIFsHIF-PHVascular endothelial growth factor receptorvascular endothelial growth factorMCF-7 human breast cancer cellsTHP-1 macrophage foam cellshypoxia-inducible factor-1αPC3 human prostate carcinoma cellsDU 145 human prostate carcinoma cellspancreatic β-cellVEGFApoE-/- miceHIF-1αInhibitorinhibitorinhibit

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