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

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).

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HIF-1/2α-IN-2 Chemical Structure

HIF-1/2α-IN-2 Chemical Structure

CAS No. : 862974-22-9

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Based on 1 publication(s) in Google Scholar

HIF-1/2α-IN-2 Related Antibodies

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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].

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

HIF-1/2α-IN-2 Related Antibodies

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.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Purity & Documentation
References
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HIF-1/2α-IN-2 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HIF-1/2α-IN-2862974-22-9HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHclear cell renal cell carcinomaccRCClipid peroxidationferroptosisxenograft modelorally activeInhibitorinhibitorinhibit

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