1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Anti-inflammatory agent 79

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body..

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Anti-inflammatory agent 79 Chemical Structure

Anti-inflammatory agent 79 Chemical Structure

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Description

Anti-inflammatory agent 79 (compound 17q) is an isoquinolinone derivative-based HIF-1 inhibitor (IC50: 0.55 μM), which can effectively block HIF-1 signals and increase HIF- Degradation of 1α. Anti-inflammatory agent 79 inhibits synovial invasion and migration and inhibits angiogenesis. Anti-inflammatory agent 79 also effectively reduced foot swelling and arthritis in a mouse inflammation model, and down-regulated the levels of inflammatory factors and blood vessel proliferation in the body.[13][1].

IC50 & Target

HIF-1α

.55 μM (IC50, [1])

In Vitro

Anti-inflammatory agent 79 (2.5-10 μM; 24 h) can concentration-dependently block hypoxia-induced HIF-1α protein accumulation, reduce inflammatory response, inhibit cell invasiveness and promote VHL-dependent HIF-1α degradation in human RA synovial cell lines[1].

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

Western Blot Analysis[1]

Cell Line: MH7A cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Decreased the protein level of HIF-1α
Decreased the secretion of cytokines, including IL-1β, IL-6 and TNF-α.
In Vivo

Anti-inflammatory agent 79 (30 mg/kg, 60 mg/kg; ip; once every 2 days for 16 days) improved pathological damage to the ankle joint and reduced vascularity in a rat model of adjuvant-induced arthritis (AIA) Generate and weaken inflammatory response[1].

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

Animal Model: Adjuvant-induced arthritic (AIA) model in SD rats[1]
Dosage: 30 mg/kg, 60 mg/kg
Administration: ip; once per two days; from 13 to 29 days after CFA injection (vehicle: 5 % ethanol and 5 % cremophor EL in FBS)
Result: Attenuated the development and severity of arthritis
Significantly decreased the HIF-1α expression and the percentage of HIF-1α positive cells.
Molecular Weight

315.37

Formula

C21H17NO2

Unlabeled CAS

SMILES

O=C(C1=CC=C(C2=COC=C2)C=C1C=C3)N3CCC4=CC=CC=C4

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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Anti-inflammatory agent 79 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.

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Product Name:
Anti-inflammatory agent 79
Cat. No.:
HY-163512
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