2. Metabolic Enzyme/Protease NF-κB Apoptosis Immunology/Inflammation
  3. HIF/HIF Prolyl-Hydroxylase IKK NF-κB Apoptosis Reactive Oxygen Species (ROS)
  4. HIF-1α-IN-8

HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE).

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HIF-1α-IN-8

HIF-1α-IN-8 Chemical Structure

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HIF-1α-IN-8 Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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Description

HIF-1α-IN-8 is an orally active HIF-1α inhibitor, with an IC50 of 2.02 μM. HIF-1α-IN-8 significantly suppresses the expression of inflammation factors of IL-6 and NO, reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells. HIF-1α-IN-8 inhibits HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins. HIF-1α-IN-8 reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model. HIF-1α-IN-8 can be used for the study of high altitude cerebral edema (HACE)[1].

IC50 & Target[1]

HIF-1α

2.02 μM (IC50)

IKKα

 

In Vitro

HIF-1α-IN-8 (Compound N41) (20 μM, 48 h) suppresses the secretion of inflammatory factors IL-6 and NO in C8-D1A cells[1].
HIF-1α-IN-8 (5-50 μM, 12 h) reduces hypoxia-induced ROS production and apoptosis in C8-D1A cells[1].
HIF-1α-IN-8 (5-20 μM, 24 h) inhibits the expression of key proteins (HIF-1α, IKKα, p65, IκBα) in the HIF-1α/IKKα/NF-κB signaling pathway and reduces the expression of blood-brain barrier permeability-related proteins MMP-9 and AQP-4 in C8-D1A cells[1].

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

HIF-1α-IN-8 Related Antibodies

Apoptosis Analysis[1]

Cell Line: C8-D1A cells
Concentration: 5, 10, 20, 50 μM
Incubation Time: 12 h
Result: Reduced apoptosis in C8-D1A cells.

Western Blot Analysis[1]

Cell Line: C8-D1A cells
Concentration: 5, 10, 20 μM
Incubation Time: 24 h
Result: Inhibited the expression of key proteins (HIF-1α, IKKα, p65, IκBα) in the HIF-1α/IKKα/NF-κB signaling pathway.
Reduced the expression of blood-brain barrier permeability-related proteins MMP-9 and AQP-4 in C8-D1A cells.
In Vivo

HIF-1α-IN-8 (Compound N41) (25-100 mg/kg, i.g., once daily, 3 days) reduces brain water content and oxidative stress level in mice with high altitude cerebral edema (HACE) model[1].

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

Animal Model: Adult male C57BL/6 mice were intraperitoneally injected with 0.5 mg/kg LPS (HY-D1056) and after 30 min of adaptation, mice were placed in a ProOx-810 Animal Low-Pressure Oxygen Control System to simulate a 7000 m high-altitude environment for 12 h to establish the HACE model[1]
Dosage: 25 mg/kg, 50 mg/kg, 100 mg/kg
Administration: i.g. once daily, 3 days
Result: Reduced weight loss in a dose-dependent manner.
Decreased brain water content (BWC) dose-dependently.
Regulated oxidative stress in brain tissue.
Suppressed inflammatory factor (IL-6, TNF-α)levels.
Alleviated brain tissue pathological damage.
Inhibited protein expression in the HIF-1α/IKKα/NF-κB signaling pathway.
Molecular Weight

523.55

Formula

C29H30FNO7
SMILES

O=C(NC1=CC=C(C2=CC=C(CCO[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O3)C=C2)C=C1)/C=C/C4=CC=CC=C4F
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-1α-IN-8 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-1α-IN-8HIF/HIF Prolyl-HydroxylaseIKKNF-κBApoptosisReactive Oxygen Species (ROS)Hypoxia-inducible factorsHIFsHIF-PHIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBhigh altitude cerebral edema (HACE)HIF-1αROSIKKαC8-D1A cellsInhibitorinhibitorinhibit

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