An inhibitor of IκBα ubiquitylation; inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM); reduces TNF-α-induced degradation of phosphorylated IκBα

GS-143 – 5 mg

Brand:
Cayman
CAS:
916232-21-8
Storage:
-20
UN-No:
Non-Hazardous - /

GS-143 is an inhibitor of IκBα ubiquitylation.{45272} It inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM) and reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, another SCFβTrCP1 substrate, in HeLa S3 cells. GS-143 inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells in a concentration-dependent manner. Intranasal administration of GS-143 (32 μg/animal) reduces the number of eosinophils, lymphocytes, and total cells in bronchoalveolar lavage fluid (BALF) in an ovalbumin-sensitized mouse model of allergic asthma.{45273}  

 

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Description

An inhibitor of IκBα ubiquitylation; inhibits ubiquitylation of phosphorylated IκBα mediated by the SCFβTrCP1 E3 ubiquitin ligase complex in vitro (IC50 = 5.2 μM); reduces TNF-α-induced degradation of phosphorylated IκBα, but not β-catenin, in HeLa S3 cells; inhibits LPS-induced expression of TNF-α, IL-6, IL-12, ICAM-1, and NF-κB in THP-1 cells a concentration-dependent manner; intranasal administration reduces the number of eosinophils, lymphocytes, and total cells in BALF in an ovalbumin-sensitized mouse model of allergic asthma at 32 μg/animal

Formal name: 4-[4-[[5-(2-fluorophenyl)-2-furanyl]methylene]-4,5-dihydro-5-oxo-3-(phenylmethyl)-1H-pyrazol-1-yl]-benzoic acid

Synonyms: 

Molecular weight: 466.5

CAS: 916232-21-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Immunology & Inflammation|Allergy||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Immunology & Inflammation|Pulmonary Diseases|Asthma

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