1. PROTAC Metabolic Enzyme/Protease Apoptosis Cell Cycle/DNA Damage
  2. Hsp-targeting Chimeras HIF/HIF Prolyl-Hydroxylase Apoptosis HSP Caspase
  3. 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.

For research use only. We do not sell to patients.

HIF-2α-IN-17

HIF-2α-IN-17 Chemical Structure

CAS No. : 861212-49-9

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Description

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[1].

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.

Western Blot Analysis[1]

Cell Line: 786-O
Concentration: 0, 5, 10, 20 and 30 μM
Incubation Time: 24 h
Result: Increased levels of cleaved caspase-3 and cleaved caspase-7 in a concentration-dependent manner.

Real Time qPCR[1]

Cell Line: 786-O
Concentration: 15 and 30 μM
Incubation Time: 24 h
Result: Downregulated mRNA expression of VEGF, NDRG2, CCND1, and GLUT1 in a concentration-dependent manner.
Molecular Weight

311.31

Formula

C17H14FN3O2

CAS No.
SMILES

CCN1C(NC(C2=CC=C(F)C=C2)=O)=C3C=CC=CC3=NC1=O

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HIF-2α-IN-17
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HY-W470101
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