GN44028
Based on 6 publication(s) in Google Scholar
GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.
For research use only. We do not sell to patients.
- Purity: 99.60%
- CAS No.: 1421448-26-1
- Formula: C18H15N3O2
- Molecular Weight:305.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GN44028
More- ACS Nano. 2023 Nov 28;17(22):22240-22258. [Abstract]
- Antioxidants (Basel). 2026 Mar 25;15(4):413. [Abstract]
- Oncogenesis. 2021 Oct 27;10(10):72. [Abstract]
- Cancer Sci. 2024 Aug;115(8):2673-2685. [Abstract]
- J Pers Med. 2023 Jan 11;13(1):146. [Abstract]
- Environ Toxicol. 2021 Aug;36(8):1654-1663. [Abstract]
Biological Activity
IC50: 14 nM (HIF-1α)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
2.1 μM
Compound: 2l
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Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| HeLa | IC50 |
0.014 μM
Compound: 2l
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Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
Inhibition of hypoxia-induced HIF1alpha transcriptional activity in human HeLa cells expressing HRE-Luc after 12 hrs by luciferase reporter gene assay
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[PMID: 24900662] |
| HeLa | IC50 |
1.8 μM
Compound: 2l
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Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| HepG2 | IC50 |
3.7 μM
Compound: 2l
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Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
| PC-3 | IC50 |
25.4 μM
Compound: 2l
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Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
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[PMID: 24900662] |
GN44028 (compound 2I, 0-30 μM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells[1].
GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells[1].
GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:0.001, 0.01, 0.1, 1µM
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Incubation Time:4 h
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Result:Inhibited the hypoxia-induced HIF-1 transcriptional activity without affecting HIF-1α/HIF-1β heterodimerization.
GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells[3]
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Dosage:10 mg/kg
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Administration:Oral gavage
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Result:Reduced both proneural and mesenchymal markers.
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Animal Model:Subcutaneous colorectal cancer model (HCT116)[2]
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Dosage:5 mg/kg
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Administration:Tail vein injection, twice a week
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Result:Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.
Chemical Information
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CAS No. 1421448-26-1
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Appearance Solid
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Molecular Weight 305.33
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Formula C18H15N3O2
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Color White to off-white
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SMILES
C1(NC2=CC=C(OCCO3)C3=C2)=NNC4=C1CC5=CC=CC=C45
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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 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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ACS Nano
Long Noncoding RNA URB1-Antisense RNA 1 (AS1) Suppresses Sorafenib-Induced Ferroptosis in Hepatocellular Carcinoma by Driving Ferritin Phase Separation. [Abstract]2023 Nov 28;17(22):22240-22258. PMID: 37966480 -
Antioxidants (Basel)
Alpha-Lipoic Acid Inhibits IFN-γ-Induced PD-L1 Expression in Prostate Cancer Cells and Enhances T-Cell-Mediated Anti-Tumor Cytotoxicity. [Abstract]2026 Mar 25;15(4):413. PMID: 42072056 -
Oncogenesis
2021 Oct 27;10(10):72. PMID: 34707087 -
Cancer Sci
Hexokinase 2 nonmetabolic function-mediated phosphorylation of IκBα enhances pancreatic ductal adenocarcinoma progression. [Abstract]2024 Aug;115(8):2673-2685. PMID: 38801832 -
J Pers Med
Microglia-Derived Spp1 Promotes Pathological Retinal Neovascularization via Activating Endothelial Kit/Akt/mTOR Signaling. [Abstract]2023 Jan 11;13(1):146. PMID: 36675807 -
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
Solvent & Solubility
DMSO : 50 mg/mL (163.76 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Minegishi H, et al. Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors. ACS Med Chem Lett. 2013 Jan 27;4(2):297-301. [Content Brief]
[2]. Changfu Liu, et al. Tumor-associated macrophage-derived transforming growth factor-β promotes colorectal cancer progression through HIF1-TRIB3 signaling. Cancer Sci. 2021 Oct;112(10):4198-4207. [Content Brief]
[3]. Xiaoqing Fan, et al. Heterogeneity of subsets in glioblastoma mediated by Smad3 palmitoylation. Oncogenesis. 2021 Oct 27;10(10):72. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2751 mL | 16.3757 mL | 32.7515 mL | 81.8786 mL |
| 5 mM | 0.6550 mL | 3.2751 mL | 6.5503 mL | 16.3757 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2751 mL | 8.1879 mL | |
| 15 mM | 0.2183 mL | 1.0917 mL | 2.1834 mL | 5.4586 mL | |
| 20 mM | 0.1638 mL | 0.8188 mL | 1.6376 mL | 4.0939 mL | |
| 25 mM | 0.1310 mL | 0.6550 mL | 1.3101 mL | 3.2751 mL | |
| 30 mM | 0.1092 mL | 0.5459 mL | 1.0917 mL | 2.7293 mL | |
| 40 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0470 mL | |
| 50 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6376 mL | |
| 60 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3646 mL | |
| 80 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL |
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