Art. -Nr.: HY-Z16784

PX-478 free base

109 Cited Publications

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Based on 109 publication(s) in Google Scholar

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. Nr.: 685847-78-3
Formel: C₁₃H₁₈Cl₂N₂O₃
Molecular Weight:321.20

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

PX-478 free base Chemical Structure

CAS. Nr.: 685847-78-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (109)
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Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HIF-1α

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

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.

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.

Chemical Information

CAS. Nr. 685847-78-3
Molecular Weight 321.20
Formel C₁₃H₁₈Cl₂N₂O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (109)

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Cancer Cell

Hypoxia inducible factor-1α drives cancer resistance to cuproptosis. [Abstract]

2025 May 12;43(5):937-954.e9. PMID: 40054467

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.).
Cell

Cuproptosis-immunity crosstalk informs strategy to overcome immunotherapy resistance. [Abstract]

2026 Jun 22:S0092-8674(26)00636-7. PMID: 42330950
Circulation

Single-Cell RNA Sequencing to Dissect the Immunological Network of Autoimmune Myocarditis. [Abstract]

2020 Jul 28;142(4):384-400. PMID: 32431172
Bioact Mater

Bidirectional modulation of glycolysis using a multifunctional nanocomposite hydrogel promotes bone fracture healing in type 2 diabetes mellitus. [Abstract]

2025 Apr 8:50:152-170. PMID: 40256330
Cancer Res

Hypoxic Memory Mediates Prolonged Tumor Intrinsic Type I Interferon Suppression to Promote Breast Cancer Progression. [Abstract]

2024 Oct 1;84(19):3141-3157. PMID: 38990731
Nat Commun

Histone methyltransferase ASH1L primes metastases and metabolic reprogramming of macrophages in the bone niche. [Abstract]

2025 May 20;16(1):4681. PMID: 40394007

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.
Nat Commun

FNDC4 alleviates cardiac ischemia/reperfusion injury through facilitating HIF1α-dependent cardiomyocyte survival and angiogenesis in male mice. [Abstract]

2024 Nov 8;15(1):9667. PMID: 39516487
Sci Transl Med

Kidney tissue hypoxia dictates T cell-mediated injury in murine lupus nephritis. [Abstract]

2020 Apr 8;12(538):eaay1620. PMID: 32269165

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.
J Nanobiotechnology

Small extracellular vesicles of hypoxic endothelial cells regulate the therapeutic potential of adipose-derived mesenchymal stem cells via miR-486-5p/PTEN in a limb ischemia model. [Abstract]

2022 Sep 24;20(1):422. PMID: 36153544
Acta Pharm Sin B

Adiponectin restores the obesity-induced impaired immunomodulatory function of mesenchymal stromal cells via glycolytic reprogramming. [Abstract]

2024 Jan;14(1):273-291. PMID: 38261813
Acta Pharm Sin B

Disruption of adipocyte HIF-1 α improves atherosclerosis through the inhibition of ceramide generation. [Abstract]

2022 Apr;12(4):1899-1912. PMID: 35847503
Adv Sci (Weinh)

Single-Nucleus Multi-Omics Reveals Hypoxia-Driven Angiogenic Programs and Their Epigenetic Control in Sinonasal Squamous Cell Carcinoma. [Abstract]

2026 Feb;13(12):e10302. PMID: 41498635
Sci Adv

MAGE-A4 induces non-small cell lung cancer and tumor-promoting plasma cell accumulation. [Abstract]

2025 Feb 14;11(7):eads4227. PMID: 39937892
Research (Wash D C)

UBE2V1 Promotes Hepatocellular Carcinoma Progression by Forming a Positive Feedback Loop with HIF-1α. [Abstract]

2025 Dec 23:8:1041. PMID: 41446875
Chem Eng J

2025 Aug 28;522:167831.
J Control Release

In situ formed chemo-immunotherapeutic hydrogel for suppression of postoperative glioma recurrence and intraoperative hemostasis. [Abstract]

2025 Aug 25:387:114168. PMID: 40865879
Cell Death Dis

De-ubiquitinase USP35 promotes peritoneal dissemination of gastric cancer by regulating metabolic reprogramming. [Abstract]

2025 Dec 10;16(1):889. PMID: 41372134
Cell Death Dis

Oncometabolite fumarate facilitates PD-L1 expression and immune evasion in clear cell renal cell carcinoma. [Abstract]

2025 Jun 3;16(1):432. PMID: 40461489
Cell Mol Biol Lett

Immunodynamic axis of fibroblast-driven neutrophil infiltration in acute pancreatitis: NF-κB-HIF-1α-CXCL1. [Abstract]

2025 May 7;30(1):57. PMID: 40335899
Cell Death Dis

METTL8 links mt-tRNA m3C modification to the HIF1α/RTK/Akt axis to sustain GBM stemness and tumorigenicity. [Abstract]

2024 May 14;15(5):338. PMID: 38744809
Cell Death Dis

Sirtuin4 alleviates severe acute pancreatitis by regulating HIF-1α/HO-1 mediated ferroptosis. [Abstract]

2023 Oct 21;14(10):694. PMID: 37865653
Cancer Lett

β-hydroxybutyrate restrains colitis-associated tumorigenesis by inhibiting HIF-1α-mediated angiogenesis. [Abstract]

2024 May 8:593:216940. PMID: 38729554
Phytomedicine

Astragaloside IV alleviates radiation-induced heart disease by regulating energy metabolism. [Abstract]

2025 Oct:146:157135. PMID: 40774010
Phytomedicine

Baicalin attenuates neuronal damage associated with SDH activation and PDK2-PDH axis dysfunction in early reperfusion. [Abstract]

2024 Jul:129:155570. PMID: 38579645
Phytomedicine

Dan-Deng-Tong-Nao softgel capsule promotes angiogenesis of cerebral microvasculature to protect cerebral ischemia reperfusion injury via activating HIF-1α-VEGFA-Notch1 signaling pathway. [Abstract]

2023 Sep:118:154966. PMID: 37487254
J Pharm Anal

2025 Nov 11.
Cell Death Discov

Mitochondrial retrograde signaling initiates HIF-1α/BNIP3/NIX-mediated mitophagy in Tibetan high-altitude adaptation. [Abstract]

2026 Jan 6;12(1):81. PMID: 41490888
Acta Pharmacol Sin

GDF11 promotes wound healing in diabetic mice via stimulating HIF-1ɑ-VEGF/SDF-1ɑ-mediated endothelial progenitor cell mobilization and neovascularization. [Abstract]

2023 May;44(5):999-1013. PMID: 36347996
Cell Death Discov

Estrogens revert neutrophil hyperplasia by inhibiting Hif1α-cMyb pathway in zebrafish myelodysplastic syndromes models. [Abstract]

2022 Jul 16;8(1):323. PMID: 35842445
J Transl Med

Cholesterol suppresses human iTreg differentiation and nTreg function through mitochondria-related mechanisms. [Abstract]

2023 Mar 27;21(1):224. PMID: 36973679
Proc Natl Acad Sci U S A

Dynamic investigation of hypoxia-induced L-lactylation. [Abstract]

2025 Mar 11;122(10):e2404899122. PMID: 40030031
Proc Natl Acad Sci U S A

Gp130-HIF1α axis-induced vascular damage is prevented by the short-term inhibition of IL-6 receptor signaling. [Abstract]

2024 Jan 9;121(2):e2315898120. PMID: 38165930
Arterioscler Thromb Vasc Biol

Low Wall Shear Stress Promotes Atheroma via Arterial Iron Accumulation. [Abstract]

2025 Nov;45(11):1983-1996. PMID: 41036559
Neural Regen Res

Hypoxia-inducible factor 1α inhibitor reduces hippocampal neuronal ferroptosis. [Abstract]

2025 Feb 24. PMID: 39995090
Antioxidants (Basel)

Hydroxysafflor Yellow A Blocks HIF-1 α Induction of NOX2 and Protects ZO-1 Protein in Cerebral Microvascular Endothelium. [Abstract]

2022 Apr 7;11(4):728. PMID: 35453413
Free Radic Biol Med

HIF-1α translation mediated by PKCδ facilitates RSV-induced production of innate inflammatory cytokines in vitro and in vivo. [Abstract]

2026 Mar 16:246:614-626. PMID: 41611036
Free Radic Biol Med

Influenza A virus-induced glycolysis facilitates virus replication by activating ROS/HIF-1α pathway. [Abstract]

2024 Nov 20:225:910-924. PMID: 39491735
J Anim Sci Biotechnol

HIF1A regulates follicular atresia through O-GlcNAcylation-mediated VEZF1/ET-1/FOXO1/BAX signaling in porcine granulosa cells. [Abstract]

2025 Sep 20;16(1):127. PMID: 40973947
Clin Transl Med

Mitochondrial dysfunction induced by HIF-1α under hypoxia contributes to the development of gastric mucosal lesions. [Abstract]

2024 Apr;14(4):e1653. PMID: 38616702
Cell Rep

Hexokinase 2-mediated metabolic stress and inflammation burden of liver macrophages via histone lactylation in MASLD. [Abstract]

2025 Feb 25;44(3):115350. PMID: 40014451
Environ Pollut

Oxygen sensors mediated HIF-1α accumulation and translocation: A pivotal mechanism of fine particles-exacerbated myocardial hypoxia injury. [Abstract]

2022 May 1:300:118937. PMID: 35114305
Front Immunol

Hypoxia Exacerbates Inflammatory Acute Lung Injury via the Toll-Like Receptor 4 Signaling Pathway. [Abstract]

2018 Jul 23:9:1667. PMID: 30083155

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).
Redox Rep

Rhaponticin alleviates pancreatic acinar cell necrosis by attenuating oxidative stress via modulation of the HIF-1α signaling pathway. [Abstract]

2026 Dec 31;31(1):2663628. PMID: 42261783
Mol Cancer Ther

Heterogeneous Responses to High-Dose Testosterone in Castration-Resistant Prostate Cancer Tumors with Mixed Rb-Proficient and Rb-Deficient Cells. [Abstract]

2025 May 2;24(5):772-783. PMID: 40116305
JCI Insight

HIF-1 regulates pathogenic cytotoxic T cells in lupus skin disease. [Abstract]

2023 Aug 22;8(16):e166076. PMID: 37526979
Biochem Pharmacol

PX-478 induces apoptosis in acute myeloid leukemia under hypoxia by inhibiting the PI3K/AKT/mTOR pathway through downregulation of GBE1. [Abstract]

2024 Nov 9:116620. PMID: 39528073
Neurobiol Dis

ROS-HIF1α-driven glycolytic reprogramming sustains ATP production in Huntington's disease. [Abstract]

2026 May 25:226:107459. PMID: 42190991
Oncogenesis

GPX3 suppresses gallbladder cancer progression by modulating redox balance, glycolysis, and anti-tumor immunity. [Abstract]

2026 Apr 2;15(1):20. PMID: 41927557
Eur J Pharmacol

Nobiletin ameliorates intervertebral disc degeneration by upregulating HIF-1α to inhibit endoplasmic reticulum stress-induced apoptosis. [Abstract]

2026 Jan 12:1011:178480. PMID: 41397628
Eur J Pharmacol

Arctiin attenuated NASH by inhibiting glycolysis and inflammation via FGFR2/CSF1R signaling. [Abstract]

2025 Jun 5:996:177424. PMID: 40010483
Int Immunopharmacol

Rheumatoid arthritis synovial fibroblasts promote the glycolysis of myeloid-derived suppressor cells via TREM1/mTOR axis. [Abstract]

2026 Sep 1:184:116961. PMID: 42242136
Int Immunopharmacol

Albiflorin contributes to Xuebijing-mediated protection against sepsis-associated acute kidney injury by modulating the succinate-PFKFB3 immunometabolic axis. [Abstract]

2026 May 14:182:116841. PMID: 42134292
Int Immunopharmacol

Icariin sensitizes glucocorticoid therapy in doxorubicin-induced fibrotic nephrotic syndrome via the HIF-1α/NF-κB/HDAC2 Axis. [Abstract]

2026 Feb 15:171:116164. PMID: 41500175
Int Immunopharmacol

N-formyl methionine mediates NETosis of neutrophil to promote sepsis-induced cardiomyopathy via the FPR1 pathway. [Abstract]

2025 Sep 26:166:115602. PMID: 41014772
Int J Mol Sci

Role of Hypoxia-Inducible Factors in Respiratory Syncytial Virus Infection-Associated Lung Disease. [Abstract]

2025 Mar 29;26(7):3182. PMID: 40244000
Int Immunopharmacol

Unraveling the crucial role of SDF-1 in osteoarthritis progression: IL6/HIF-1α positive feedback and chondrocyte ferroptosis. [Abstract]

2025 Apr 16:152:114400. PMID: 40058106
Int J Mol Sci

Nicotinamide Mononucleotide (NMN) Ameliorates Free Fatty Acid-Induced Pancreatic β-Cell Dysfunction via the NAD+/AMPK/SIRT1/HIF-1α Pathway. [Abstract]

2024 Sep 30;25(19):10534. PMID: 39408861
Int Immunopharmacol

Isocitrate dehydrogenases 2-mediated dysfunctional metabolic reprogramming promotes intestinal cancer progression via regulating HIF-1A signaling pathway. [Abstract]

2024 Aug 1:140:112828. PMID: 39094359
Int Immunopharmacol

Hypoxia induces the production of epithelial-derived cytokines in eosinophilic chronic rhinosinusitis with nasal polyps. [Abstract]

2023 Aug:121:110559. PMID: 37364325
Int Immunopharmacol

Hypoxia disrupts the nasal epithelial barrier by inhibiting PTPN2 in chronic rhinosinusitis with nasal polyps. [Abstract]

2023 May:118:110054. PMID: 36963262
Mol Neurobiol

Advanced Glycation End-Products (AGEs) Promote Endothelial Cell Pyroptosis Under Cerebral Ischemia and Hypoxia via HIF-1α-RAGE-NLRP3. [Abstract]

2023 May;60(5):2355-2366. PMID: 36652049
Inflammation

Aquaporin-1 Facilitates Macrophage M1 Polarization by Enhancing Glycolysis Through the Activation of HIF1α in Lipopolysaccharide-Induced Acute Kidney Injury. [Abstract]

2024 Oct 4. PMID: 39365391
mBio

Respiratory syncytial virus co-opts hypoxia-inducible factor-1α-mediated glycolysis to favor the production of infectious virus. [Abstract]

2023 Oct 31;14(5):e0211023. PMID: 37796013
Mol Med Rep

Uremic toxin p‑cresyl sulfate enhances the calcification of aortic valvular interstitial cells via klotho/sirtuin‑1 signaling. [Abstract]

2026 Jun;33(6):162. PMID: 41930468
Mol Med Rep

LDHA protects vascular endothelial cells from oxidative stress‑induced mitochondrial damage via HIF‑1α activation and glycolytic reprogramming. [Abstract]

2026 May;33(5):141. PMID: 41891951
Biochim Biophys Acta Mol Basis Dis

Pulmonary succinate receptor 1 elevation in high-fat diet mice exacerbates lipopolysaccharides-induced acute lung injury via sensing succinate. [Abstract]

2024 Jun;1870(5):167119. PMID: 38479484
Sci Rep

Circadian gene BMAL1 ameliorates renal ischaemia-reperfusion injury in diabetic mice by enhancing mitophagy via the HIF-1/BNIP3 pathway. [Abstract]

2025 Jul 2;15(1):23001. PMID: 40594206
Oncol Rep

Hypoxia‑induced miR‑135b‑5p promotes neuroendocrine differentiation of prostate cancer cells through HIF1AN‑HIF1α axis. [Abstract]

2026 Apr;55(4):74. PMID: 41716025
Hum Gene Ther

Matrix protein of vesicular stomatitis virus targets the mitochondria, reprograms glucose metabolism，and sensitizes to 2-deoxyglucose in glioblastoma. [Abstract]

2024 Oct;35(19-20):838-854. PMID: 39001830
iScience

Heat-killed Mycobacterium tuberculosis induces trained immunity in vitro and in vivo administered systemically or intranasally. [Abstract]

2024 Jan 11;27(2):108869. PMID: 38318361
Mol Nutr Food Res

Frataxin-Mediated PINK1-Parkin-Dependent Mitophagy in Hepatic Steatosis: The Protective Effects of Quercetin. [Abstract]

2018 Aug;62(16):e1800164. PMID: 29935106
FASEB J

Uric acid promotes aortic valve calcification via mediating valve interstitial cell osteogenic differentiation and endothelial dysfunction. [Abstract]

2025 Mar 31;39(6):e70437. PMID: 40100089
FASEB J

HIF-1α inhibition in macrophages preserves acute liver failure by reducing IL-1β production. [Abstract]

2023 Sep;37(9):e23140. PMID: 37584647
Front Biosci (Landmark Ed)

HIF-1α and VEGF Immunophenotypes as Potential Biomarkers in the Prognosis and Evaluation of Treatment Efficacy of Atherosclerosis: A Systematic Review of the Literature. [Abstract]

2025 Jan 8;30(1):27004. PMID: 39862086
J Biol Chem

The coccidian parasites Toxoplasma and Neospora dysregulate mammalian lipid droplet biogenesis. [Abstract]

2017 Jun 30;292(26):11009-11020. PMID: 28487365
Metab Brain Dis

Promotion of angiogenesis in cerebral infarction by Tongqiao Huoxue Decoction through activation of glycolysis. [Abstract]

2025 Oct 11;40(7):288. PMID: 41074933
J Biomed Mater Res A

Enhancing Bone Regeneration: The Role of Biomimetic Silicified Collagen Scaffold in Osteogenesis and Angiogenesis. [Abstract]

2025 Jul;113(7):e37954. PMID: 40635198
Biochim Biophys Acta Gene Regul Mech

Hypoxia inducible factor HIF1α elevates expression of mRNA capping enzyme during cobalt chloride-induced hypoxia. [Abstract]

2025 Apr 4:195087. PMID: 40189045
Arch Biochem Biophys

Exosomes derived from HISLA overexpressed-adipose stem cells accelerate wound healing in diabetic foot ulcers by regulating HIF-1α signal transduction. [Abstract]

2026 Apr:778:110747. PMID: 41581639
Arch Biochem Biophys

Chaetocin attenuates gout in mice through inhibiting HIF-1α and NLRP3 inflammasome-dependent IL-1β secretion in macrophages. [Abstract]

2019 Jul 30:670:94-103. PMID: 31255694
Chem Biol Drug Des

Tetrahydropalmatine Alleviates Osteoarthritis-Associated Pain and Inflammation by Suppressing KDM4A/MDM2/HIF-1α-Mediated M1 Macrophage Polarization. [Abstract]

2026 Mar;107(3):e70279. PMID: 41857767
Biol Reprod

Fetal hypoxia exposure induces Hif1a activation and autophagy in adult ovarian granulosa cells†. [Abstract]

024 Dec 12;111(6):1220-1234. PMID: 39361887
Iran J Basic Med Sci

Triiodothyronine potentiates angiogenesis-related factor expression through PI3K/AKT signaling pathway in human osteoarthritic osteoblasts. [Abstract]

2020 Jun;23(6):819-825. PMID: 32695299
J Neuroimmunol

Establishment of a passive-transfer mouse model of anti-NMDAR encephalitis and delineation of the PI3K-AKT-HIF-1α Axis in antibody-induced neuronal injury. [Abstract]

2026 Aug:417:578943. PMID: 42048740
J Pharmacol Sci

Dendrobine alleviates lung injury in septic mice by inhibiting mitochondrial-endoplasmic reticulum crosstalk-mediated NLRP3 inflammasome activation. [Abstract]

2026 Aug;161(4):119-129. PMID: 42303347
Gene

HIF signaling overactivation inhibits lateral line neuromast development through Wnt in zebrafish. [Abstract]

2024 Mar 10:898:148077. PMID: 38097093
Mol Reprod Dev

Decreased OGT Attenuates Endometrial Decidualization and Embryo Implantation by Affecting HIF-1α Stability. [Abstract]

2025 May;92(5):e70025. PMID: 40342239
Cardiovasc Innov Appl

2023 May 23.
Biochem Biophys Res Commun

Dietary fatty acids activate FATP4 and lipid transport via HIF1α and KDM4B in the small intestinal enterocytes. [Abstract]

2026 Aug 27:828:154141. PMID: 42284990
Biochem Biophys Res Commun

Isoquercitrin inhibits ferroptosis and ameliorates insulin resistance: Evidence from network pharmacology and in vitro studies. [Abstract]

2025 Aug 21:781:152500. PMID: 40858065
Biochem Biophys Res Commun

Inhibition of hypoxia-inducible factor-1α alleviates acinar cell necrosis in a mouse model of acute pancreatitis. [Abstract]

2021 Oct 1:572:72-79. PMID: 34358966
bioRxiv

Epigenetic de-repression of basal cell metaplasia in aging AT2 cells is a risk factor for idiopathic pulmonary fibrosis (IPF). [Abstract]

2026 Jun 10:2026.06.09.731212. PMID: 42327275
bioRxiv

2026 Apr 1.
bioRxiv

2026 Mar 10.
SSRN

2025 Dec 19.
Res Sq

2025 Oct 5.
Patent

US20250041255A1.
Res Sq

2024 Nov 11.
bioRxiv

2024 November 21.
bioRxiv

2024 July 06.
bioRxiv

MAGE-A4-Responsive Plasma Cells Promote Non-Small Cell Lung Cancer. [Abstract]

2024 Jul 16:2024.07.10.602985. PMID: 39071307
SSRN

2023 Jun 29.
SSRN

2023 Jun 22.
Oxid Med Cell Longev

Hypoxia Enhances Glioma Resistance to Sulfasalazine-Induced Ferroptosis by Upregulating SLC7A11 via PI3K/AKT/HIF-1 α Axis. [Abstract]

2022 Nov 18:2022:7862430. PMID: 36439690
Oxid Med Cell Longev

MicroRNA 101 Attenuated NSCLC Proliferation through IDH2/HIF α Axis Suppression in the Warburg Effect. [Abstract]

2022 Oct 18:2022:4938811. PMID: 36304962
Research Square Preprint

2022 Jul.
Research Square Print

2022 Jul.
Research Square Preprint

2021 Dec.
Research Square Preprint

2021 Dec.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Koh MY, et al. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Molecular cancer therapeutics. 2008 Jan;7(1):90-100. [Content Brief]

[2]. Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. International journal of cancer. 2008 Nov 15;123(10):2430-7. [Content Brief]

[3]. Ilegems E, et al. HIF-1α inhibitor PX-478 preserves pancreatic β cell function in diabetes[J]. Science translational medicine, 2022, 14(638): eaba9112.

[4]. Hu G, et al. Autophagy inhibition and ferroptosis activation during atherosclerosis: Hypoxia-inducible factor 1α inhibitor PX-478 alleviates atherosclerosis by inducing autophagy and suppressing ferroptosis in macrophages[J]. Biomedicine & Pharmacotherapy, 2023, 161: 114333.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

PX-478 free base

109 Cited Publications

100 mg Angebot einholen

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PX-478 free base

Publications Citing Use of MedChemExpress (MCE) PX-478 free base

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (109)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PX-478 free base Related Classifications

HY-Z16784 Related Classifications