GS143, IkappaB Ubiquitination Inhibitor


Catalog No. size PriceQuantity
M60308-2S 2 mg solid $129
M60308-10S 10mg solid $529

Description

GS143 is selective β-TrCP1 ligase inhibitor, inhibits IκBα ubiquitination with IC50 ~5.2 μM without affecting proteasome activity. It blocks LPS-induced expression of inflammatory cytokines in human myelomonocytic cells. It suppresses antigen-induced NFκB expression, inflammation and mucus production in airways of OVA-sensitized mice.

Product information

CAS Number: 916232-21-8

Molecular Weight: 466.46

Formula: C28H19FN2O4

Chemical Name: 4-(3-benzyl-4-((5-(2-fluorophenyl)furan-2-yl)methylene)-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid

Smiles: OC(=O)C1C=CC(=CC=1)N1N=C(CC2C=CC=CC=2)C(=CC2=CC=C(O2)C2=CC=CC=C2F)C1=O

InChiKey: IZPMWFSVTDOCDI-HAVVHWLPSA-N

InChi: InChI=1S/C28H19FN2O4/c29-24-9-5-4-8-22(24)26-15-14-21(35-26)17-23-25(16-18-6-2-1-3-7-18)30-31(27(23)32)20-12-10-19(11-13-20)28(33)34/h1-15,17H,16H2,(H,33,34)/b23-17+

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GS143 was used at 10-20 µM final concentration in various assays.

In Vivo:

OVA-sensitized mice were given intranasally with GS143 (16 or 32 µg) and 2 h later, these mice were challenged with inhaled OVA.

References:

  1. Hirose K, et al. GS143, an IkappaB ubiquitination inhibitor, inhibits allergic airway inflammation in mice. Biochem Biophys Res Commun. (2008) 374(3):507-11.
  2. Nakajima H, et al. A novel small-molecule inhibitor of NF-kappaB signaling. (2008) Biochem Biophys Res Commun. 368(4):1007-13.

Products are for research use only. Not for human use.

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