BAY 87-2243
Based on 30 publication(s) in Google Scholar
BAY 87-2243 is a highly potent and selective hypoxia-inducible factor-1 (HIF-1) inhibitor.
For research use only. We do not sell to patients.
- Purity: 99.40%
- CAS No.: 1227158-85-1
- Formula: C26H26F3N7O2
- Molecular Weight:525.53
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Epigenetics Compound Library
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HY-L204
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HY-L205
Publications Citing Use of MedChemExpress (MCE) BAY 87-2243
More- Immunity. 2025 Aug 9:S1074-7613(25)00326-7. [Abstract]
- Cell Res. 2018 Dec;28(12):1171-1185. [Abstract]
- Theranostics. 2020 Jun 12;10(16):7409-7421. [Abstract]
- Redox Biol. 2024 Aug 16:76:103316. [Abstract]
- J Control Release. 2024 Jun 14:372:69-84. [Abstract]
- Brain Behav Immun. 2023 Mar:109:308-320. [Abstract]
- J Med Chem. 2025 Oct 29. [Abstract]
- Mol Ther Oncolytics. 2022 Aug 5:26:372-386. [Abstract]
- Cancer Metab. 2019 Mar 6:7:2. [Abstract]
- Cancer Metab. 2019 Jul 16;7:7. [Abstract]
- Radiother Oncol. 2015 Sep;116(3):431-7. [Abstract]
- Inflammation. 2025 Jan 13. [Abstract]
- Int Immunopharmacol. 2025 Jul 15:163:115198. [Abstract]
- Molecules. 2022 Jan 26;27(3):804. [Abstract]
- J Biol Chem. 2023 Jun;299(6):104829. [Abstract]
- Environ Toxicol. 2021 Aug;36(8):1654-1663. [Abstract]
- Med Gas Res. 2025 Sep 1;15(3):398-403. [Abstract]
- BMC Mol Cell Biol. 2024 Apr 23;25(1):13. [Abstract]
- Drug Test Anal. 2022 Oct;14(10):1703-1723. [Abstract]
- Exp Biol Med. 2021 Jan;246(1):84-96. [Abstract]
- Drug Test Anal. 2021 Feb;13(2):283-298. [Abstract]
- PLoS One. 2022 May 16;17(5):e0268445. [Abstract]
- Theriogenology. 2020 Nov;157:418-430. [Abstract]
- Eur J Integr Med. 2025 Aug 28;78:102545.
- Res Sq. 2026 Apr 24:rs.3.rs-9504540. [Abstract]
- bioRxiv. 2025 May 31.
- Research Square Preprint. 2022 May.
- Research Square Preprint. 2021 Feb.
- Patent. US20180263995A1.
- Hypoxia. 2016 Nov 8:4:147-159. [Abstract]
Customer Validation & Images
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RT-PCR
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WB
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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2D/3D Cell Culture and Differentiation
Biological Activity
HIF-1α[1]
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Cell Line
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Type | Value | Description | References |
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| G-361 | IC50 |
4.8 μM
Compound: 38; BAY 87-2243
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Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
Antiproliferative activity against human G-361 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
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[PMID: 36332549] |
| Melanoma cell | IC50 |
2 nM
Compound: 28; BAY 57-2243
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Antiproliferative activity against human melanoma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor reagent based fluorescence analysis
Antiproliferative activity against human melanoma cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Fluor reagent based fluorescence analysis
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[PMID: 36893622] |
| NCI-H460 | EC50 |
3 nM
Compound: 28; BAY 57-2243
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Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by cell titer glow assay
Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 48 hrs by cell titer glow assay
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[PMID: 36893622] |
| NSCLC | IC50 |
10 mM
Compound: 28; BAY 57-2243
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Inhibition of mitochondrial respiration in human NSCLC cells assessed as oxygen consumption rate incubated for 1 hr by oxygen sensitive fluorescence dye based analysis
Inhibition of mitochondrial respiration in human NSCLC cells assessed as oxygen consumption rate incubated for 1 hr by oxygen sensitive fluorescence dye based analysis
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[PMID: 36893622] |
| PC-3 | IC50 |
10 nM
Compound: BAY 87-2243
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Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method
Inhibition of complex-I-dependent oxygen consumption in mitochondria of human PC-3 cells by luxcel-dye staining based MitoXpress method
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[PMID: 34982568] |
| SK-MEL-28 | IC50 |
2.4 μM
Compound: 38; BAY 87-2243
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Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
Antiproliferative activity against human SK-MEL-28 cells harboring BRAF V600E mutant assessed as cell viability incubated for 72 hrs by crystal violet staining based assay
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[PMID: 36332549] |
BAY 87-2243 inhibits luciferase activity with a calculated IC50 value of ~0.7 nM. Hypoxic induction of the HIF target gene CA9 on protein level in HCT116luc cells is inhibited by BAY 87-2243 with an IC50 value of ~2 nM. BAY 87-2243 inhibits mitochondrial oxygen consumption measured by using the oxygen sensitive fluorescence dye LUX-MitoXpress with an IC50 value of ~10 nM[1]. BAY-87-2243 inhibits nuclear HIF-1α protein expression. Administration of BAY-87-2243 for about 18 days significantly reduces HIF-1α protein expression as well as pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p<0.0001), and necrotic fraction (NF) (mean 9% vs. 35.6%, p=0.0002), whereas relative vascular area (RVA) and perfused vessels (PF) remained unchanged[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1227158-85-1
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Appearance Solid
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Molecular Weight 525.53
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Formula C26H26F3N7O2
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Color White to off-white
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SMILES
FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCN(C6CC6)CC5)=NC=C4)C(C)=C3)=N2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (30)
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Journal Impact Factor
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Most Recent
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Immunity
2025 Aug 9:S1074-7613(25)00326-7. PMID: 40816269 -
Cell Res
2018 Dec;28(12):1171-1185. PMID: 30287942 -
Theranostics
2020 Jun 12;10(16):7409-7421. PMID: 32642002
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Theranostics. 2020 Jun 12;10(16):7409-7421. [Abstract]
BAY 87-2243 (5 μM/mL for 7 days) were applied to perform gain- and loss-of-function assays. The sphere-formation rate and the diameter of spheroids were severely inhibited by HIF-1 inhibitor and enhanced by HIF-1 activator, indicating that the HIF-1 pathway is important for the formation and expansion of HERS spheroids. In addition, the expansion of 2D monolayer HERS cells was also inhibited by BAY.
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Redox Biol
2024 Aug 16:76:103316. PMID: 39260060
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 16:76:103316. [Abstract]
VEGFA gene expression in ARPE-19 cells exposed to heme (25 μM) and BAY 87–2243 (20–80 nM).
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 16:76:103316. [Abstract]
Protein levels in ARPE-19 cells exposed to heme (25 μM) and BAY 87–2243 (20–80 nM).
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 16:76:103316. [Abstract]
Mito Stress Profile of ARPE-19 cells exposed to heme and heme + BAY 87–2243 (80 nM) or LY294002 or Rapamycin. NC: non-treated cells.
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 16:76:103316. [Abstract]
Glycolysis Stress Profile of ARPE-19 cells exposed to heme and heme + BAY 87–2243 (80 nM) or LY294002 or Rapamycin. NC: non-treated cells. Data are represented as mean value ± SEM (n = 3).
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J Control Release
Fine-tuning of liposome integrity for differentiated transcytosis and enhanced antitumor efficacy. [Abstract]2024 Jun 14:372:69-84. PMID: 38866244 -
Brain Behav Immun
Schwann cell-derived CXCL2 contributes to cancer pain by modulating macrophage infiltration in a mouse breast cancer model. [Abstract]2023 Mar:109:308-320. PMID: 36754246 -
J Med Chem
Discovery of Oral Natural Benzofuranoid p-Terphenyl Derivative CHNQD-03301 as a Potent Hypoxia-Inducible Factor-1α Signaling Inhibitor for Cancer Therapy. [Abstract]2025 Oct 29. PMID: 41159374 -
Mol Ther Oncolytics
Berberine inhibits carcinogenesis through antagonizing the ATX-LPA-LPAR2-p38-leptin axis in a mouse hepatoma model. [Abstract]2022 Aug 5:26:372-386. PMID: 36090480 -
Cancer Metab
CHCHD4 confers metabolic vulnerabilities to tumour cells through its control of the mitochondrial respiratory chain. [Abstract]2019 Mar 6:7:2. PMID: 30886710 -
Cancer Metab
CHCHD4 regulates tumour proliferation and EMT-related phenotypes, through respiratory chain-mediated metabolism. [Abstract]2019 Jul 16;7:7. PMID: 31346464 -
Radiother Oncol
Nuclear EGFR renders cells radio-resistant by binding mRNA species and triggering a metabolic switch to increase lactate production. [Abstract]2015 Sep;116(3):431-7. PMID: 26320552
BAY 87-2243 purchased from MedChemExpress. Usage Cited in: Radiother Oncol. 2015 Sep;116(3):431-7. [Abstract]
Radiation-induced Hif1α expression and blockage by BAY87-2243 or EGFR siRNA. A549 and FaDu cells are pretreated with BAY87-2243 or hypoxia and irradiated with 2 Gy. Six hours after irradiation, cells are lysed, and Western blotting is performed.
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Inflammation
Inhibition of Mitochondrial Succinate Dehydrogenase with Dimethyl Malonate Promotes M2 Macrophage Polarization by Enhancing STAT6 Activation. [Abstract]2025 Jan 13. PMID: 39806091 -
Int Immunopharmacol
GDF15 attenuates sepsis-induced acute lung injury by suppressing the HIF-1α/LDHA pathway. [Abstract]2025 Jul 15:163:115198. PMID: 40669249 -
Molecules
2-Hydroxyestradiol Overcomes Mesenchymal Stem Cells-Mediated Platinum Chemoresistance in Ovarian Cancer Cells in an ERK-Independent Fashion. [Abstract]2022 Jan 26;27(3):804. PMID: 35164068 -
J Biol Chem
VBP1 negatively regulates CHIP and selectively inhibits the activity of hypoxia-inducible factor (HIF)-1α but not HIF-2α. [Abstract]2023 Jun;299(6):104829. PMID: 37201586 -
Environ Toxicol
Lysosome Fe2+ release is responsible for etoposide- and cisplatin-induced stemness of small cell lung cancer cells. [Abstract]2021 Aug;36(8):1654-1663. PMID: 33969609 -
Med Gas Res
2025 Sep 1;15(3):398-403. PMID: 39923136 -
BMC Mol Cell Biol
mTOR signaling pathway regulation HIF-1 α effects on LPS induced intestinal mucosal epithelial model damage. [Abstract]2024 Apr 23;25(1):13. PMID: 38654163 -
Drug Test Anal
Metabolic study of hypoxia-inducible factor stabilizers BAY 87-2243, MK-8617, and PT-2385 in equine liver microsomes for doping control. [Abstract]2022 Oct;14(10):1703-1723. PMID: 35853151 -
Exp Biol Med
2021 Jan;246(1):84-96. PMID: 33167688 -
Drug Test Anal
High-throughput liquid chromatography tandem mass spectrometry assay as initial testing procedure for analysis of total urinary fraction. [Abstract]2021 Feb;13(2):283-298. PMID: 32852861 -
PLoS One
The protective effects of HIF-1α activation on sepsis induced intestinal mucosal barrier injury in rats model of sepsis. [Abstract]2022 May 16;17(5):e0268445. PMID: 35576220 -
Theriogenology
Enhancing effect of FSH on follicular development through yolk formation and deposition in the low-yield laying chickens. [Abstract]2020 Nov;157:418-430. PMID: 32871446 -
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Res Sq
A sodium-HIF1α axis coordinates immune metabolic reprogramming and mitochondrial remodeling in salt-sensitive hypertension. [Abstract]2026 Apr 24:rs.3.rs-9504540. PMID: 42078875 -
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Hypoxia
2016 Nov 8:4:147-159. PMID: 27878135
Solvent & Solubility
DMSO : 20 mg/mL (38.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Luciferase activity is given in % of DMSO-treated cells. To evaluate the cytotoxicity of BAY 87-2243, 2.000 cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth medium containing 10% FCS. BAY 87-2243 at various concentrations is added at 24 h after seeding for additional 48 h and cell viability is determined using Cell Titer Glow Assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Tumor xenograft experiment is carried out on female immune-deficient, athymic NMRI nude mice, aged 7-9 weeks, weighing 20-25 g. The lung carcinoma xenograft mouse model is established by subcutaneous injection into the right flank with 0.1 mL H460 tumor cells (1.5×106) mixed 1:1 with Matrigel. Mice are randomized into control and BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) groups when tumors reach a size of more than 40 mm2. Body weight is monitored as a measure for treatment-related, acute toxicity. Tumor area (measured by caliper) or tumor weight (measured when mice are sacrificed 21 days after cell injection) is calculated by the formula 100-100×(tumor weight/area of treatment group)/(tumor weight/area of vehicle group). Tumor Statistical analysis is performed using the one-way analysis of variance.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Ellinghaus P, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer Med. 2013 Oct;2(5):611-24. [Content Brief]
[2]. Helbig L, et al. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep 19;9:207. [Content Brief]
Complete Stock Solution Preparation Table
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9028 mL | 9.5142 mL | 19.0284 mL | 47.5710 mL |
| 5 mM | 0.3806 mL | 1.9028 mL | 3.8057 mL | 9.5142 mL | |
| 10 mM | 0.1903 mL | 0.9514 mL | 1.9028 mL | 4.7571 mL | |
| 15 mM | 0.1269 mL | 0.6343 mL | 1.2686 mL | 3.1714 mL | |
| 20 mM | 0.0951 mL | 0.4757 mL | 0.9514 mL | 2.3786 mL | |
| 25 mM | 0.0761 mL | 0.3806 mL | 0.7611 mL | 1.9028 mL | |
| 30 mM | 0.0634 mL | 0.3171 mL | 0.6343 mL | 1.5857 mL |
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