Home NF-κB IκB/IKK inhibitor - Immunology & Inflammation related chemical Mesalazine (5-ASA) For research use only.

Mesalazine (5-ASA)

Synonyms: Mesalamine, 5-Aminosalicylic acid

Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.

Mesalazine (5-ASA) Chemical Structure

Mesalazine (5-ASA) Chemical Structure

CAS No. 89-57-6

Purity & Quality Control

Mesalazine (5-ASA) Related Products

Signaling Pathway

IκB/IKK Signaling Pathways

IκB/IKK Signaling Pathway

Biological Activity

Description Mesalazine (5-ASA) is a specific inhibitor of TNFα-induced IKK activity, used to treat inflammatory bowel disease.
Targets
IKK [1]
In vitro
In vitro

Mesalamine inhibits the enzyme 3-hydroxysteroid dehydrogenase, involved in the reversible conversion between DHP and THP, and therefore may affect the local actions of DHP and THP in the brain. Mesalamine, an anti-inflammatory aminosalicylate, dose-dependently inhibits IL-1-stimulated NF-kappaB-dependent transcription without preventing IkappaB degradation or nuclear translocation and DNA binding of the transcriptionally active NF-kappaB proteins, RelA, c-Rel, or RelB. Mesalamine is found to inhibit IL-1-stimulated RelA phosphorylation. [1]

Mesalamine increases cell adhesion which is measured by cell adhesion assay and transcellular-resistance measurement. Mesalamine treatment restores membranous expression of adhesion molecules E-cadherin and β-catenin. [2]

Mesalamine or sulfasalazine (2 mM), but not sulfapyridine, significantly reduces the expression of the TC22 transcript and significantly reduces the expression of TC22 protein in a dose-dependent and reversible manner. [3]

Mesalamine induces membranous expression of E-cadherin and increases intercellular adhesion. Mesalamine activity modulates E-cadherin glycosylation and increases both mRNA and protein levels of GnT-III and its activity as detected by increased E4-lectin reactivity. [4]

Mesalamine (0.1-1 mM) shows considerable inhibition of peroxynitrite-mediated luminol chemiluminescence in a dose-dependent fashion, suggesting that Mesalamine is able to directly scavenge the peroxynitrite. Mesalamine only at higher concentration (1 mM) inhibits the hydroxyl radical adduct while shifting Electron paramagnetic resonance (EPR) spectra. [5]
Cell Research Cell lines BVECs
Concentrations 1 mM
Incubation Time 1 h
Method

Cells were treated with indicated concentration of drug for an hour.
In Vivo
In vivo

5-ASA exerts potent antineoplastic effects that are mediated through PPARγ in an aberrant crypt mice model.
Animal Research Animal Models A/JOlaHsd mic
Dosages 200 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05992142 Completed
Ulcerative Colitis
Belgian Inflammatory Bowel Disease Research and Development (BIRD) VZW|Ferring Pharmaceuticals
 January 17 2023 Phase 4
NCT04499495 Completed
Ulcerative Colitis
Ferring Pharmaceuticals
 October 25 2021 --
NCT05213234 Recruiting
Ulcerative Colitis
Rush University Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
 July 9 2021 Not Applicable
NCT02277223 Withdrawn
Ulcerative Colitis
Schneider Children''s Medical Center Israel
 March 1 2020 Phase 3
NCT03415711 Terminated
Ulcerative Colitis
VSL Pharmaceuticals|Actial Farmaceutica S.r.l.
 April 28 2017 Not Applicable

Chemical Information & Solubility

Molecular Weight 153.14 Formula

C7H7NO3
CAS No. 89-57-6 SDF Download Mesalazine (5-ASA) SDF
Smiles C1=CC(=C(C=C1N)C(=O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 31 mg/mL ( (202.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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