GS143

GS143 is a selec-tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup-presses NF-κB acti-va-tion and tran-scrip-tion of tar-get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect[1][2].

Product Specifications

CAS Number

[916232-21-8]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

E1/E2/E3 Enzyme; IKK; NF-κB

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gs143.html

Purity

99.09

Solubility

DMSO : 37.5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

FC(C=CC=C1)=C1C2=CC=C(O2)/C=C3C(CC4=CC=CC=C4)=NN(C5=CC=C(C(O)=O)C=C5)C\3=O

Molecular Formula

C28H19FN2O4

Molecular Weight

466.46

Precautions

H302, H315, H319, H335

References & Citations

[1]Koichi Hirose, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. 2008 Sep 26;374 (3) :507-11.|[2]Hiroto Nakajima, et al. A novel small-molecule inhibitor of NF-kappaB signaling. Biochem Biophys Res Commun. 2008 Apr 18;368 (4) :1007-13.