1. NF-κB
    Autophagy
  2. NF-κB
    Autophagy

Sulfasalazine (Synonyms: NSC 667219)

Cat. No.: HY-14655 Purity: >98.0%
Data Sheet SDS Handling Instructions

Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis.

For research use only. We do not sell to patients.
Sulfasalazine Chemical Structure

Sulfasalazine Chemical Structure

CAS No. : 599-79-1

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
1 g $50 In-stock
5 g $80 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Sulfasalazine is a drug for the treatment of rheumatoid arthritis and ulcerative colitis.

In Vitro

Treatment of SW620 colon cells with sulfasalazine inhibits TNFα-, LPS-, or phorbol ester-induced NFκB activation. NFκB–dependent transcription is inhibited by sulfasalazine at micro- to millimolar concentrations. TNFα-induced nuclear translocation of NFκB is prevented by sulfasalazine through inhibition of IκBα degradation[1]. Pre‐incubation with 5 mM of sulfasalazine alone significantly increases basal mRNA expression of all pro‐inflammatory cytokines with levels of IL‐6 mRNA increased by 80‐fold compared with vehicle control[2]. Once digested, sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity[3].

In Vivo

At low doses (0.25 mM), SAS is able to suppress glioma growth by over 60% compared to untreated controls[3].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00637780 Pfizer Arthritis, Juvenile Rheumatoid June 2010 Phase 4
NCT01577966 University of Alabama at Birmingham Brain Tumor January 2012
NCT01312129 The Mind Research Network Alcohol Dependence March 2010
NCT00554203 Boston University Coronary Artery Disease July 2003
NCT01198145 Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) Diarrhea|Gastrointestinal Complications|Unspecified Adult Solid Tumor, Protocol Specific April 2011 Phase 3
NCT01659242 Singapore General Hospital Rheumatoid Arthritis July 2012 Phase 4
NCT01667029 Massachusetts General Hospital Painful Neuropathy May 2013 Phase 2
NCT00844142 Charite University, Berlin, Germany|Wyeth is now a wholly owned subsidiary of Pfizer Moderate to Severe Active Axial Spondyloarthritis November 2005 Phase 2
NCT03012763 University Medicine Greifswald Pharmacokinetics|Magnetic Resonance Imaging|Administration, Oral April 2016 Phase 1
NCT00579878 University of Nebraska Rheumatoid Arthritis December 1999 Phase 3
NCT02434861 Tesaro, Inc. Chemotherapy-induced Nausea and Vomiting May 2015 Phase 1
NCT02930343 Jawaharlal Institute of Postgraduate Medical Education & Research Rheumatoid Arthritis September 2016 Phase 4
NCT02456363 Chung Shan Medical University Ankylosing Spondylitis November 2009 Phase 2
NCT02638896 Zhixiang Huang|Health and Family Planning Commission of Guangdong Ankylosing Spondylitis January 2016 Phase 4
NCT00405275 VA Office of Research and Development|Canadian Institutes of Health Research (CIHR)|Rheumatoid Arthritis Investigational Network (RAIN)|National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS) Rheumatoid Arthritis July 2007
NCT02374021 Brigham and Women's Hospital|Columbia University Arthritis, Rheumatoid July 2016 Phase 4
NCT00422227 Wyeth is now a wholly owned subsidiary of Pfizer Rheumatoid Arthritis June 2007 Phase 4
NCT00259610 University of Alabama at Birmingham|Amgen|Barr Laboratories|Pfizer Rheumatoid Arthritis May 2004 Phase 4
NCT00889694 Sun Yat-sen University Early Ankylosing Spondylitis October 2008 Phase 2|Phase 3
NCT00521924 Merck Sharp & Dohme Corp.|AESCA Pharma GmbH Rheumatoid Arthritis June 2007 Phase 3
NCT01709578 Sanofi Rheumatoid Arthritis October 2012 Phase 3
NCT01941095 Hoffmann-La Roche Rheumatoid Arthritis November 2013 Phase 3
NCT01768572 Sanofi|Regeneron Pharmaceuticals Rheumatoid Arthritis March 2013 Phase 3
NCT02057250 Sanofi|Regeneron Pharmaceuticals RA March 2014 Phase 3
NCT02373202 Sanofi|Regeneron Pharmaceuticals Rheumatoid Arthritis February 2015 Phase 3
NCT02433184 University of Leeds Rheumatoid Arthritis July 2011 Phase 4
NCT01596777 University Medicine Greifswald Intestinal Obstruction January 2010 Phase 1
NCT01596764 University Medicine Greifswald Intestinal Obstruction May 2011 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.5101 mL 12.5505 mL 25.1010 mL
5 mM 0.5020 mL 2.5101 mL 5.0202 mL
10 mM 0.2510 mL 1.2551 mL 2.5101 mL
Cell Assay
[1]

Sulfasalazine is dissolved in culture medium. SW620 cells are grown in Dulbecco’s modified Eagle medium, supplemented with 10% heat-inactivated FCS, 2 mmol/liter glutamine, and 1% (wt/vol) penicillin/streptomycin. SW620 cells are transfected with the 3xIgkBLuc reporter construct. After 18 h, cells are incubated with either medium alone or with sulfasalazine (0.1, 0.2, 0.5, 1, 2, 5 mM) before stimulation with TNFα, LPS, or PMA. Luciferase assay is performed[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mouse: Sulfasalazine is dissolved in 0.1 M NaOH, and then neutralized by titrating with 0.1 M HCl. U-87MG glioma cells are implanted into the cranium of a SCID mouse. After 7 days, animals are randomized into three groups of five animals each. One group receives 1 mL i.p. saline injections twice daily for 3 weeks. The two test groups receives 8 mg of sulfasalazine in 1 mL saline twice daily for 3 weeks. Tumor growth and animal health were monitored. After perfusion with 4% paraformaldehyde, mouse brains were collected, rinsed, and placed in 30% sucrose[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

398.39

Formula

C₁₈H₁₄N₄O₅S

CAS No.

599-79-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Sulfasalazine
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