Home Immunology & Inflammation Immunology & Inflammation related inhibitor - NF-κB inhibitor - TGF-beta/Smad inhibitor - COX inhibitor - Ferroptosis activator - Autophagy activator - Apoptosis related activator Sulfasalazine For research use only.

Sulfasalazine

Synonyms: NSC 667219, Sulphasalazine

Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.

Sulfasalazine Chemical Structure

Sulfasalazine Chemical Structure

CAS No. 599-79-1

Purity & Quality Control

Sulfasalazine Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki=0.53μM 22541068
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50=0.56μM 22541068
HepG2 Function assay 1 hr Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay, IC50=0.9μM 21889336
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay, IC50=0.9μM 21870831
HepG2 Function assay 1 hr Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis, IC50=0.9μM 22381047
HepG2 Function assay 1 hr Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay, IC50=0.9μM 23031596
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay, IC50=0.9μM 24314396
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki=3μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50=3μM 22541068
U2OS Function assay 10 mins Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method, IC50=9.6μM 31439379
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki=11μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50=12μM 22541068
U87 Function assay 15 mins Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting, IC50=30μM 21889337
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Biological Activity

Description Sulfasalazine is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor of nuclear factor kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.
Targets
NF-κB [4] COX-2 [4] TGF-β [4]
In vitro
In vitro

Sulfasalazine, like methotrexate, enhances adenosine release at an inflamed site and that adenosine diminishes inflammation via occupancy of A2 receptors on inflammatory cells. [1] Sulfasalazine treatment for 4 hours inhibits kappaB-dependent transcription with an IC50 value of approximately 0.625 mM. Sulfasalazine (2.5 mM) results in cell death of T-lymphocytes in a dose- and time-dependent manner. Sulfasalazine but not 5ASA or sulfapyridine, strongly inhibits NF-kappaB activation and potently induces apoptosis in T-lymphocytes. [2] Sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid (5-ASA; mesalamine) by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity. Sulfasalazine but not its cleaved form 5-ASA causes a dose-dependent inhibition of glioma growth, this effect is entirely attributable to the inhibition of cystine uptake via the system x(c)(-) cystine-glutamate transporter. Sulfasalazine inhibits cystine uptake causing a chronic depletion of intracellular GSH and consequently compromised cellular redox defense which stymied tumor growth. [3]
In Vivo
In vivo

Sulfasalazine markedly decreases the number of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch in the murine air pouch model of inflammation. Sulfasalazine treatment promotes a marked increase in splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR) concentration, which is consistent with the in vitro observation that sulfasalazine inhibits AICAR transformylase. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06134388 Recruiting
Metastatic Colorectal Cancer
Tanta University
 September 1 2023 Phase 3
NCT03487926 Active not recruiting
Major Depressive Episode|Inflammatory Bowel Diseases
Centre for Addiction and Mental Health|McMaster University
 September 14 2022 --
NCT04720183 Completed
Healthy
Galapagos NV
 January 11 2021 Phase 1
NCT01577966 Completed
Brain Tumor
University of Alabama at Birmingham
 January 2012 Not Applicable

Chemical Information & Solubility

Molecular Weight 398.39 Formula

C18H14N4O5S
CAS No. 599-79-1 SDF Download Sulfasalazine SDF Download Sulfasalazine SDF
Smiles C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (200.8 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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