HIF-IN-3
HIF-IN-3 is a HIF inhibitor. HIF-IN-3 blocks the dimerization of HIF-α with HIF-1β by binding to the PAS domain of HIF-α, and induces the degradation of HIF-1α and HIF-2α via the ubiquitin-proteasome pathway. HIF-IN-3 inhibits the expression of the endogenous HIF-1 target gene CA9 and the HIF-2 target gene EPO in cancer cells. HIF-IN-3 inhibits tumor growth in the BT-474 breast cancer model. HIF-IN-3 can be used for research on HIF-related tumors such as breast cancer, colorectal cancer, and head and neck squamous cell carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 1783134-96-2
- Formula: C20H26N4O2
- Molecular Weight:354.45
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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HIF-1α |
HIF-2α |
In Vitro
HIF-IN-3 (5-10 μM; 6-24 h) triggers the degradation of HIF-1α and HIF-2α in Hep3B cells and inhibits HIF target gene expression[1].
HIF-IN-3 (0-10 μM; 24 h) does not significantly alter RPL13A or HIF mRNA levels in Hep3B cells[1].
HIF-IN-3 (5 μM; 24 h) inhibited HIF target gene expression by 84% in Hep3B human hepatocellular carcinoma cells, with an IC50 of 1.6 μM, and an IC50 of 6.1 μM in MDA-MB-231 breast cancer cells[1].
HIF-IN-3 (5 μM) has a Luc assay IC50 of 3[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hep3B cells
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Concentration:5 or 10 μM
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Incubation Time:6 or 24 h
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Result:Triggered degradation of HIF-1α and HIF-2α and inhibited HIF target gene expression, as assessed by immunoblot and immunoprecipitation assays.
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Cell Line:Hep3B cells
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Concentration:0, 1, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:No significant difference vs vehicle control for RPL13A and HIF mRNAs.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice were injected with BT-474 human breast cancer cells into the mammary fat pad (MFP), and the experiment began when the tumor volume reached 150 mm3[1]
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Dosage:10 mg/kg
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Administration:i.p.; twice daily (BID); 7 days
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Result:HIF-IN-3 inhibited tumor growth in BT-474 mammary fat pad xenografts.
Chemical Information
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CAS No. 1783134-96-2
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Molecular Weight 354.45
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Formula C20H26N4O2
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SMILES
O[C@@H]1C[C@H](C2=NC=NC(N3CCN(CC3)CCOC4=CC=CC=C4)=C2)C1
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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-IN-3 Related Classifications
HY-189519 Related Classifications
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