HIF-IN-4
HIF-IN-4 is a HIF inhibitor. HIF-IN-4 induces degradation of HIF-1α and HIF-2α and inhibits HIF target gene expression. HIF-IN-4 inhibits colorectal cancer and head and neck squamous cell carcinoma xenograft tumor growth in vivo, and inhibits laser-induced choroidal neovascularization. HIF-IN-4 can be used in research on colorectal cancer, head and neck squamous cell carcinoma, and ocular neovascularization-related diseases.
For research use only. We do not sell to patients.
- CAS No.: 401642-27-1
- Formula: C27H36N4S2
- Molecular Weight:480.73
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HIF-1α |
HIF-2α |
In Vitro
HIF-IN-4 (0-10 μM; 24 h) did not significantly alter RPL13A or HIF mRNA expression in Hep3B cells[1].
HIF-IN-4 (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-4 (5 μM) inhibited HEP3B.C1 luciferase reporter gene activity by 50%, inhibited Hep3B gene expression by 84%, with an IC50 of 3 in the Luc assay[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:0, 1, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:No significant difference in RPL13A or HIF mRNA expression was observed versus vehicle control cells.
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Cell Line:Hep3B human hepatocellular carcinoma 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.
In Vivo
HIF-IN-4 (10-20 mg/kg; i.p.; twice daily; 5 days) inhibited the growth of SCCVII HNSCC tumors in syngeneic C3H mice[1].
HIF-IN-4 (i.p.; twice daily; 5 days) significantly inhibited the growth of human HCT116 colorectal cancer xenografts in nude mice and reduced the protein expression of HIF-1α and HIF-2α in tumor tissues[1].
HIF-IN-4 inhibits the growth of CT26 colorectal tumors in Balb/c mice[1].
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 inoculated with HNSCC cells, and the experiment began when the tumor volume reached 150 mm3
[1] -
Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; twice daily; 5 days
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Result:Inhibited tumor volume compared with vehicle.
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Animal Model:Syngeneic C3H mice were inoculated with HNSCC cells, and the experiment began when the tumor volume reached 150 mm3
[1] -
Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; twice daily; 5 days
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Result:Inhibited tumor volume compared with vehicle.
- RT-PCR
- RNA extraction experimental
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Real Time qPCR (Q-PCR)
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 401642-27-1
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Molecular Weight 480.73
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Formula C27H36N4S2
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SMILES
S=C(N1CCC(CCCC2CCN(CC2)C(NC3=CC=CC=C3)=S)CC1)NC4=CC=CC=C4
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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-4 Related Classifications
HY-189520 Related Classifications
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