HIF-2α-IN-17
HIF-2α-IN-17 is a selective hypoxia-inducible factor 2α (HIF2α) inhibitor that binds to the PAS-B domain of HIF2α. HIF-2α-IN-17 disrupts the interaction between HIF2α and the molecular chaperone Hsp70, leading to proteasomal degradation of HIF2α. HIF-2α-IN-17 exhibits antitumor activity and induces apoptosis in cancer cells. HIF-2α-IN-17 is applicable for research on cancers such as clear cell renal cell carcinoma.
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- No. CAS: 861212-49-9
- Fòrmula: C17H14FN3O2
- Peso molecular:311.31
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
HSP70 |
HIF-2α |
Caspase-3 |
Caspase-7 |
In Vitro
HIF-2α-IN-17 (Compound-c2) (0-30 μM; 24 h) selectively inhibits the viability of VHL-deficient clear cell renal cell carcinoma (ccRCC) cell lines (786-O, A498), with no effect on VHL-positive Caki-1 cells or normal HEK293 cells[1].
HIF-2α-IN-17 (5-30 μM; 24 h) induces apoptosis in 786-O cells by activating caspase-3 and caspase-7[1].
HIF-2α-IN-17 (0-30 μM; 8-24 h) suppresses the transcriptional activity of HIF2α and reduces the expression levels of HIF2α target genes (VEGF, NDRG2, CCND1, GLUT1) in 786-O cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:786-O
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Concentration:0, 5, 10, 20 and 30 μM
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Incubation Time:24 h
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Result:Increased levels of cleaved caspase-3 and cleaved caspase-7 in a concentration-dependent manner.
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Cell Line:786-O
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Concentration:15 and 30 μM
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Incubation Time:24 h
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Result:Downregulated mRNA expression of VEGF, NDRG2, CCND1, and GLUT1 in a concentration-dependent manner.
Chemical Information
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No. CAS 861212-49-9
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Peso molecular 311.31
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Fòrmula C17H14FN3O2
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SMILES
CCN1C(NC(C2=CC=C(F)C=C2)=O)=C3C=CC=CC3=NC1=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HIF-2α-IN-17 Related Classifications
HY-W470101 Related Classifications
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