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

HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .

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

HIF-1/2α-IN-1 Chemical Structure

HIF-1/2α-IN-1 Chemical Structure

CAS No. : 2827693-99-0

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HIF-1/2α-IN-1 Related Antibodies

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Description

HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) [1].

IC50 & Target[1]

HIF-2α

0.92 μM (IC50)

In Vitro

HIF-1/2α-IN-1 (compound #25) (0.01-100 μM) inhibits HIF-2α activity with an IC50 value of 0.92 μM[1].
HIF-1/2α-IN-1 (0-10 μM, 24 h) decrease HIF-2α by inhibiting IRE-dependent translation and also inhibit HIF-1α at higher concentrations，which effects mediates by inhibiting the function of iron sulfur cluster assembly 2 (ISCA2) [1].
HIF-1/2α-IN-1 (1 μM, 24 h) targets ISCA2 and trigger the iron starvation response[1].
HIF-1/2α-IN-1 (0-100 μM, 24 h) decreased cell viability in 786-0 cells (IC50=1.7 μM (786-0), 10.6 μM (786-0 VHL)) and RCC4 cells (IC50=4.8 μM (RCC4), 71.0 μM (RCC4 VHL)) [1].

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

HIF-1/2α-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: 786-0 cells and RCC4 cells
Concentration: 0.01-100 μM
Incubation Time: 24 h
Result: Decreased cell viability in 786-0 cells and RCC4 cells.

Western Blot Analysis[1]

Cell Line: 786-0 cells and RCC10 cells
Concentration: 0, 0.5, 1, 2.5, 10 μM
Incubation Time: 24 h
Result: Decreased HIF-2α activity and protein levels.
Decreased HIF-1α levels at higher concentrations or treatment durations, but do not promote proteasomal degradation of HIF-1/2α.
Inhibited the production of luciferase driven by the HIF-2α IRE (IRE-Luc).
Increasesed IRP2, TFRC in dose-dependent and decreased FTH.

RT-PCR[1]

Cell Line: 786-0 cells
Concentration: 0, 0.5, 1, 5 μM
Incubation Time: 24 h
Result: Resulted in a dose-dependent decrease in the transcription of HIF-2α target genes VEGFA and POU5F1, but not inhibited HIF-2α transcription.
In Vivo

HIF-1/2α-IN-1 (compound #25) (p.o.; 30, 60 mg/kg; daily) significantly reduced ccRCC xenograft growth in vivo[1].

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

Animal Model: NRG or Balb/c mice[1]
(6-8 week old, male, 10 per group)
Dosage: 30, 60 mg/kg
Administration: p.o., daily
Result: Significantly inhibited tumor growth.
Had well tolerated with no significant weight loss.
Molecular Weight

368.35

Formula

C17H16N6O4
CAS No.
SMILES

COC1=CC=C(C=C1OC)C2=NN=C(O2)NC3=NC4=C(N3)C=CN=C4OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HIF-1/2α-IN-1 Related Classifications

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Help & FAQs
  • 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-12827693-99-0HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHiron sulfur cluster assembly 2 (ISCA2)HIF-1/2αclear cell renal cell carcinoma (ccRCC)cancer786-0 cellsRCC10 cellsInhibitorinhibitorinhibit

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