Cat. No.: HY-10231

PX-478

102 Cited Publications

Customer Review

Based on 102 publication(s) in Google Scholar

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

For research use only. We do not sell to patients.

Purity: 99.58%
CAS No.: 685898-44-6
Formula: C₁₃H₂₀Cl₄N₂O₃
Molecular Weight:394.12

Storage:

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

PX-478 Chemical Structure

CAS No.: 685898-44-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (102)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

HIF-1α

All HIF/HIF Prolyl-Hydroxylase Isoforms :

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	19.7 μM Compound: PX-478	Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]
MDA-MB-231	IC₅₀	62.8 μM Compound: PX-478	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs under hypoxic condition by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]
MDA-MB-468	IC₅₀	45.1 μM Compound: PX-478	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay Antiproliferative activity against human MDA-MB-468 cells after 72 hrs under hypoxic condition by MTT assay	[PMID: 28209257]

In Vitro

PX-478 (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 (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 (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 (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 (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 (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 (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 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 (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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 685898-44-6
Appearance Solid
Molecular Weight 394.12
Formula C₁₃H₂₀Cl₄N₂O₃
Color Off-white to yellow
SMILES

[O-][N+](CCCl)(CCCl)C(C=C1)=CC=C1C[C@H](N)C(O)=O.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Publications (102)

All WBIHCCell Migration/Invasion AssayIF

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Journal Impact Factor

Cancer Cell

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

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

PX-478 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 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 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
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
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 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.
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
Chem Eng J

2025 Aug 28;522:167831.
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
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
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
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
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
Cancer Lett

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

2024 May 8:593:216940. PMID: 38729554
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 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
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
J Pharm Anal

2025 Nov 11.
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
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
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 Transl Med

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

2023 Mar 27;21(1):224. PMID: 36973679
Arterioscler Thromb Vasc Biol

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

2025 Nov;45(11):1983-1996. PMID: 41036559
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
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
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
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
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
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
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
JCI Insight

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

2023 Aug 22;8(16):e166076. PMID: 37526979
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 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).
Neurobiol Dis

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

2026 May 25:226:107459. PMID: 42190991
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
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
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
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 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

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
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
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 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
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

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
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
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
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
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
FASEB J

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

2023 Sep;37(9):e23140. PMID: 37584647
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
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
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
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
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
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
J Biol Chem

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

2017 Jun 30;292(26):11009-11020. PMID: 28487365
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
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
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
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
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
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
Mol Reprod Dev

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

2025 May;92(5):e70025. PMID: 40342239
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
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
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
Gene

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

2024 Mar 10:898:148077. PMID: 38097093
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
Cardiovasc Innov Appl

2023 May 23.
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

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

2024 Jul 16:2024.07.10.602985. PMID: 39071307
bioRxiv

2024 July 06.
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.

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (253.73 mM; Need ultrasonic)

DMSO : 100 mg/mL (253.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5373 mL

12.6865 mL

25.3730 mL

5 mM

0.5075 mL

2.5373 mL

5.0746 mL

10 mM

0.2537 mL

1.2686 mL

2.5373 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator

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

Mass

Concentration

Volume

Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (12.69 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.34 mM); Clear solution

Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: ≥ 0.5 mg/mL (1.27 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: Saline

Solubility: 16.67 mg/mL (42.30 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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.

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	2.5373 mL	12.6865 mL	25.3730 mL	63.4325 mL
	5 mM	0.5075 mL	2.5373 mL	5.0746 mL	12.6865 mL
	10 mM	0.2537 mL	1.2686 mL	2.5373 mL	6.3432 mL
	15 mM	0.1692 mL	0.8458 mL	1.6915 mL	4.2288 mL
	20 mM	0.1269 mL	0.6343 mL	1.2686 mL	3.1716 mL
	25 mM	0.1015 mL	0.5075 mL	1.0149 mL	2.5373 mL
	30 mM	0.0846 mL	0.4229 mL	0.8458 mL	2.1144 mL
	40 mM	0.0634 mL	0.3172 mL	0.6343 mL	1.5858 mL
	50 mM	0.0507 mL	0.2537 mL	0.5075 mL	1.2686 mL
	60 mM	0.0423 mL	0.2114 mL	0.4229 mL	1.0572 mL
	80 mM	0.0317 mL	0.1586 mL	0.3172 mL	0.7929 mL
	100 mM	0.0254 mL	0.1269 mL	0.2537 mL	0.6343 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

PX-478

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) PX-478

All HIF/HIF Prolyl-Hydroxylase Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (102)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PX-478

MCE Bioactive Compound Library

Clinical Compound Library Plus

Publications Citing Use of MedChemExpress (MCE) PX-478

All HIF/HIF Prolyl-Hydroxylase Isoforms

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (102)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PX-478 Related Classifications

Cat. No.: HY-10231