HIF-1α stabilizer-1
HIF-1α stabilizer-1 is a HIF-1α stabilizer and iron chelator. HIF-1α stabilizer-1 induces HIF-dependent transcription and upregulates VEGFA and GLUT1 expression without directly binding to PHD1-3. HIF-1α stabilizer-1 inhibits hyperglycemia-induced ROS accumulation. HIF-1α stabilizer-1 promotes cell migration. HIF-1α stabilizer-1 accelerates wound closure and improves tissue remodeling by enhancing neovascularization and collagen deposition. HIF-1α stabilizer-1 lacks antibacterial activity against P. aeruginosa. HIF-1α stabilizer-1 can be used for research on diabetic wounds.
For research use only. We do not sell to patients.
- CAS No.: 3128930-57-1
- Formula: C15H16N2O3
- Molecular Weight:272.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
GLUT1 |
HIF-1α |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L929 | IC50 |
>20 μM
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Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42623917 |
| HaCaT | IC50 |
>20 μM
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Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42623917 |
In Vitro
HIF-1α stabilizer-1 (Compound 17b) (3 h) exhibits good iron-chelating activity in the cell-free CAS assay, with an EC50 value of 20.65 μM[1].
HIF-1α stabilizer-1 (48 h) exhibits a favorable safety profile in L929 and HaCaT cells, with low cytotoxicity and an IC50 value greater than 20 μM[1].
HIF-1α stabilizer-1 (20 μM; 1-12 h) stabilizes HIF-1α and upregulates GLUT-1 in L929 cells under normoglycemic conditions[1].
HIF-1α stabilizer-1 (20 μM; 1-12 h) rapidly restores the expression of HIF-1α and GLUT-1 in L929 cells under high glucose conditions[1].
HIF-1α stabilizer-1 (5-10 μM; 48 h) effectively enhances fibroblast migration in L929 cells[1].
HIF-1α stabilizer-1 (five days) effectively inhibits hyperglycemia-induced ROS accumulation in L929 cells, with a ROS inhibition rate of 76.4%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:L929
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Concentration:20 μM
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Incubation Time:1-12 h
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Result:Induced HIF-1α stabilization beginning at 6 h and sustained up to 12 h.
Increased GLUT-1 expression in a time-dependent manner.\nRapidly restored HIF-1α and GLUT-1 expression as early as 1 h after treatment.
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Cell Line:L929
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Concentration:5-10 μM
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Incubation Time:48 h
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Result:Promoted wound closure with relative wound-closure fold changes of 2.1- and 2.2-fold at 5 and 10 μM, respectively.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (male, ~200 g)[1]
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Dosage:5 mM, 50 μL
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Administration:topical application to wounds
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Result:Accelerated wound repair, characterized by reduced purulent exudate with crust formation observed as early as day 2.
The wound area progressively decreased after treatment and the wound-healing rate in the 17b group was significantly higher than that in the model group.
Histological analysis on day 12 revealed more complete epidermal coverage, reduced inflammatory infiltration and exudate, enhanced neovascularization within the granulation tissue, and markedly increased collagen fiber deposition compared to the model group.
The dermal tissue was also more regularly organized in the 17b group.
Chemical Information
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CAS No. 3128930-57-1
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Molecular Weight 272.30
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Formula C15H16N2O3
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SMILES
O=C1C=CC=C(C(NC2=C(C)C=C(C)C=C2C)=O)N1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HIF-1α stabilizer-1 Related Classifications
HY-189274 Related Classifications
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