1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. HIF-1/2α-IN-2

HIF-1/2α-IN-2 

Cat. No.: HY-151344
Handling Instructions

HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2).

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

HIF-1/2α-IN-2 Chemical Structure

HIF-1/2α-IN-2 Chemical Structure

CAS No. : 862974-22-9

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Description

HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2)[1].

IC50 & Target

Iron Sulfur Cluster Assembly 2 (ISCA2), HIF-1/2α[1]

In Vitro

HIF-1/2α-IN-2 (compound #1) (0-25 μM; 24 h) decreases HIF-2α translation instead of transcription, with a downward trend in VEGFA and POU5F1 (HIF-2α target genes) transcription and insignificant effect on EPAS1 (HIF-2α)[1].
HIF-1/2α-IN-2 (0-100 μM, 24 h) inhibits the production of luciferase driven by the HIF-2α Iron-Responsive Element (IRE) luciferase reporter with an IC50 value of 3.9 μM, to block IRE-dependent translation of HIF-2α[1].
HIF-1/2α-IN-2 (0, 10, 50 μM) protects ISCA2 from Pronase-mediated (4 μg/mL) degradation, and (1.5 μM; 24 h) targets ISCA2 to induce iron and metals accumulation in normoxia 786-0 cells[1].
HIF-1/2α-IN-2 (0-100 μM; 24 h) results ISCA2 inhibition and promotes cell death via ferroptosis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Normoxia 786-0 cells (20%O2) and hypoxic ACHN cells (or 1%O2 for final 24 h to induce HIF expression)
Concentration: 0, 1, 5, 10, 25 μM
Incubation Time: 24 hours
Result: Decreased the protein level of HIF-2α, FTH1, ISCA2, and increased IRP2 protein level at high concentrations over 10 μM in normoxia 786-0 cells.
Dcreased the HIF-2α and FTH1 levels at 1 μM in hypoxic ACHN cells.

Cell Viability Assay[1]

Cell Line: Normoxia 786-0 cells
Concentration: 0-100 μM
Incubation Time: 24 hours
Result: Inhibited 786-0 cells viability by inducing ferroptosis, with an IC50 value of 22.0 μM.
Molecular Weight

342.35

Formula

C16H11FN4O2S

CAS No.
SMILES

COC1=C2N=C(NC3=NN=C(C4=CC=C(F)C=C4)O3)SC2=CC=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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HIF-1/2α-IN-2
Cat. No.:
HY-151344
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