GN44028 |
Catalog No.GC34595
One-Click Copy Product Info
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GN44028 is a hypoxia-inducible factor (HIF)-1α inhibitor with an IC₅₀ value of 14nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1421448-26-1
Sample solution is provided at 25 µL, 10mM.
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GN44028 is a hypoxia-inducible factor (HIF)-1α inhibitor with an IC₅₀ value of 14nM[1-2]. GN44028 can be used in cancer research and has demonstrated the ability to enhance anticancer effects in the treatment of colorectal cancer[3-4].
In vitro, BV2 microglial cells were pretreated with GN44028 (10μM) for 1 hour, followed by culture under hypoxic conditions (1% O₂). GN44028 significantly inhibited hypoxia-induced HIF-1α protein expression and downregulated the secretion of its downstream target gene Spp1[5]. In human myoblasts adapted to chronic hypoxia (2% O₂, 3 weeks), pretreatment with GN44028 (1μM) for 48 or 96 hours significantly suppressed hypoxia-induced HIF-1α protein activity, reduced cell proliferation and glycolytic capacity, and impaired mitochondrial respiratory function (decreased OCR)[6].
In vivo, BALB/c mice infected with Leishmania donovaniwere intraperitoneally administered GN44028 (10mg/kg body weight/day) starting from day 10 post-infection, with injections every 5 days until day 45. GN44028 significantly reduced parasitic loads in the spleen and liver and alleviated infection-associated immunopathology[7]. In tumor-bearing mice (HCT116 or CT26 cells), GN44028 (5mg/kg) was administered via tail vein injection twice weekly from day 14 to day 60 post-cell inoculation. GN44028 significantly suppressed tumor growth, enhanced the chemotherapeutic effects of 5-fluorouracil (25mg/kg) and oxaliplatin (10mg/kg), and reduced the number of lung metastatic nodules[8].
References:
[1] Shahruzaman SH, Fakurazi S, Maniam S. Targeting energy metabolism to eliminate cancer cells. Cancer Manag Res. 2018 Jul 31;10:2325-2335.
[2] Farina AR, Cappabianca L, Sebastiano M, et al. Hypoxia-induced alternative splicing: the 11th Hallmark of Cancer. J Exp Clin Cancer Res. 2020 Jun 15;39(1):110.
[3] Qannita RA, Alalami AI, Harb AA, et al. Targeting Hypoxia-Inducible Factor-1 (HIF-1) in Cancer: Emerging Therapeutic Strategies and Pathway Regulation. Pharmaceuticals (Basel). 2024 Feb 1;17(2):195.
[4] Yu T, Tang B, Sun X. Development of Inhibitors Targeting Hypoxia-Inducible Factor 1 and 2 for Cancer Therapy. Yonsei Med J. 2017 May;58(3):489-496.
[5] Bai Q, Wang X, Yan H, et al. Microglia-Derived Spp1 Promotes Pathological Retinal Neovascularization via Activating Endothelial Kit/Akt/mTOR Signaling. J Pers Med. 2023 Jan 11;13(1):146.
[6] Yin A, Fu W, Elengickal A, et al. Chronic hypoxia impairs skeletal muscle repair via HIF-2α stabilization. J Cachexia Sarcopenia Muscle. 2024 Apr;15(2):631-645.
[7] Roy S, Roy S, Halder S, et al. Leishmania exploits host cAMP/EPAC/calcineurin signaling to induce an IL-33-mediated anti-inflammatory environment for the establishment of infection. J Biol Chem. 2024 Jun;300(6):107366.
[8] Liu C, Zhang W, Wang J, 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.
| Cell experiment [1]: | |
Cell lines | BV2 murine microglial cells |
Preparation Method | BV2 cells were cultured in Dulbecco's modified eagle medium (DMEM) supplemented with 10% fetal bovine serum (FBS), 100units/mL penicillin G, and 100μg/mL streptomycin at 37°C with 5% CO₂. For hypoxic treatment, cells were exposed to 1% O₂. GN44028 (10μM) was added to BV2 cells 1 hour before hypoxia induction. |
Reaction Conditions | 10μM; pretreatment 1 hour before hypoxia. |
Applications | GN44028 effectively inhibited hypoxia-induced stabilization of HIF-1α in BV2 microglial cells. This suppression of HIF-1α led to reduced expression of Spp1 (osteopontin). |
| Animal experiment [2]: | |
Animal models | Balb/C mice and NOD-SCID mice bearing subcutaneous colorectal tumors (HCT116 or CT26 cells) |
Preparation Method | Mice with established subcutaneous tumors were treated GN44028 (5mg/kg) via tail vein injection. |
Dosage form | 5mg/kg; i.v.; Twice a week for 60 days. |
Applications | GN44028 significantly suppressed tumor growth and lung metastasis. GN44028 enhanced the anticancer effects of chemotherapy drugs 5-Fluorouracil (5-FU) and Oxaliplatin (OXA), leading to reduced tumor volumes and improved survival rates in tumor-bearing mice. |
References: | |
| Cas No. | 1421448-26-1 | SDF | |
| Canonical SMILES | C1(NC2=CC=C(OCCO3)C3=C2)=NNC4=C1CC5=CC=CC=C45 | ||
| Formula | C18H15N3O2 | M.Wt | 305.33 |
| Solubility | DMSO : 50 mg/mL (163.76 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2751 mL | 16.3757 mL | 32.7514 mL |
| 5 mM | 655 μL | 3.2751 mL | 6.5503 mL |
| 10 mM | 327.5 μL | 1.6376 mL | 3.2751 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)