Sulfasalazine (NSC 667219) - Moligand™, 10mM in DMSO , Inhibitor of Proton-coupled folate transporter, CAS No.599-79-1, Inhibitor of Proton-coupled folate transporter

CAS: 599-79-1 Cat. No.: S409257 Molecular Weight: 398.39 Beilstein Registry Number: 356241 EC Number: 209-974-3 PubChem CID: 5339

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Azulfidine, Salazopyrin, Sulphasalazine | 2-​hydroxy-​5-​[2-​[4-​[(2-​pyridinylamino)​sulfonyl]​phenyl]​diazenyl]​-benzoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 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 ofnuclear factor
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. 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. 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.

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.
Cell Data

cell lines：p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines.

Concentrations：Concentrations:

Incubation Time：Incubation Time:

Powder Purity:≥98%

Specifications

Synonyms

Azulfidine, Salazopyrin, Sulphasalazine | 2-​hydroxy-​5-​[2-​[4-​[(2-​pyridinylamino)​sulfonyl]​phenyl]​diazenyl]​-benzoic acid

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) 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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of Proton-coupled folate transporter

Names and Identifiers

• Isomeric SMILES: C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O
• WGK Germany: 2
• RTECS: VO6250000
• PubChem CID: 5339
• Molecular Weight: 398.39
• Beilstein: 356241
• Reaxy-Rn: 356241

Associated Targets(Human)

SLC46A1 Tchem Proton-coupled folate transporter (1 Activities)

Discover Target: SLC46A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 47 mg/mL (197.24 mM)
• Melt Point(°C): 260-265°C

References

1. Lu Liu, Zhongxia Wang, Yulin Qi, Ang Huang, Caiping He, Xiaoyan Zhan, Xiaohe Xiao, Zhaofang Bai.  (2025)  Kurarinone Alleviates cGAS-STING-Triggered Inflammatory Diseases by Targeting STING.  PHYTOTHERAPY RESEARCH,      [PMID:40604353] [10.1002/ptr.70023]

2. Shutao Li, Pengyi Ma, Jinping Song, Xiaoting Guo, Jianhua Xue, Qi Ma.  (2025)  A simple low-temperature synthesis of fluorescent boron quantum dots for versatile applications.  CRYSTENGCOMM,      [PMID:] [10.1039/D5CE00616C]

3. Jia Jia, Qian Liu, Tao Wang, Borui Zou, Xiong Xiong, Jun Xu, Chenxi Wu.  (2025)  Multiple stressors enhance Microcystis dominance and modulate phycospheric antibiotic resistome in aquatic mesocosm.  JOURNAL OF HAZARDOUS MATERIALS,      [PMID:40865219] [10.1016/j.jhazmat.2025.139633]

4. Jingwei Liu, Cheng Qiu, Xiaoxiong Wang, Ziqian Xiang, Junyuan Sun, Mingzheng Chang, Qingliang Ma, Yan Zhuang, Yunpeng Zhao, Qiang Yang, Lianlei Wang, Xinyu Liu.  (2025)  Sulfasalazine disrupts the interaction between TNFα and TNFR1 thus inhibiting NF-kB signaling activation to promote bone fracture healing.  JOURNAL OF PHARMACOLOGICAL SCIENCES,      [PMID:40983456] [10.1016/j.jphs.2025.08.005]

5. Ke Ning, Chao Shi, Yan-Yu Chi, Yong-Fei Zhou, Weiwei Zheng, Yameng Duan, Weiwei Tong, Qiuhong Xie, Hongyu Xiang.  (2023)  Portulaca oleracea L. polysaccharide alleviates dextran sulfate sodium-induced ulcerative colitis by regulating intestinal homeostasis.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:38000581] [10.1016/j.ijbiomac.2023.128375]

6. Yiren Yang, Yuwei Zhang, Jiangping Song, Yaqian Li, Liuyang Zhou, Hongtao Xu, Kaizhang Wu, Jie Gao, Mouming Zhao, Yang Zheng.  (2023)  Bergamot polysaccharides relieve DSS-induced ulcerative colitis via regulating the gut microbiota and metabolites.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:37820919] [10.1016/j.ijbiomac.2023.127335]

7. Guangshuai Zhang, Dandan Song, Ruilong Ma, Mo Li, Bingyang Liu, Zhonggui He, Qiang Fu.  (2024)  Artificial mucus layer formed in response to ROS for the oral treatment of inflammatory bowel disease.  Science Advances,  10  (30):   [PMID:39058786] [10.1126/sciadv.ado8222]

8. Xiaoxun Lu, Jiabin Hong, Jing Zhang, Qian Liu, Ganzhong Liao, Yanwei Shi, Huanwen Tang, Xiaoshan Liu.  (2023)  Triphenyl phosphate disrupts placental tryptophan metabolism by activating MAOA/ROS/NFκB.  SCIENCE OF THE TOTAL ENVIRONMENT,      [PMID:37659542] [10.1016/j.scitotenv.2023.166688]

9. Yajing Wang, Tao Zhang, Jie Liu, Xianfeng Huang, Xiaojing Yan.  (2023)  Investigations of the gingerol oil colon targeting pellets for the treatment of ulcerative colitis.  FITOTERAPIA,      [PMID:37442485] [10.1016/j.fitote.2023.105607]

10. Ke Ning, Yameng Duan, Weiwei Tong, Yue Chen, Qinghui Zhang, Qiuhong Xie, Hongyu Xiang.  (2023)  Protective Effects of Different Molecular Weights of Purslane (Portulaca oleracea L.) Aqueous Extract on DSS-Induced Ulcerative Colitis in Mice.  Antioxidants,  12  (7): (1400).  [PMID:37507939] [10.3390/antiox12071400]

11. Chunhong Wu, Yifei Xiao, Caimei Wu, Dihao Xie, Meixue Luo, Dingyi Yao, Min Chen, Danyi Lu.  (2023)  Regulation of BCRP expression and sulfasalazine pharmacokinetics by the nuclear receptor REV-ERBα.  XENOBIOTICA,      [PMID:37039301] [10.1080/00498254.2023.2200839]

12. Wang Li, Shao Li, Chen Man-Yun, Wang Lin, Zhang Wei, Tan Feng-Bo, Huang Wei-Hua.  (2022)  Effect of ginsenoside compound K on alleviating colitis via modulating gut microbiota.  Chinese Medicine,  17  (1): (1-12).  [PMID:36578000] [10.1186/s13020-022-00701-9]

13. Li Wang, Li Shao, Man-Yun Chen, Lin Wang, Pu Yang, Feng-Bo Tan, Wei Zhang, Wei-Hua Huang.  (2022)  Panax notoginseng Alleviates Colitis via the Regulation of Gut Microbiota.  AMERICAN JOURNAL OF CHINESE MEDICINE,  51  (01): (107-127).  [PMID:36408726] [10.1142/S0192415X23500076]

14. Xiaomeng Tang, Meng Yang, Yongwei Gu, Liangdi Jiang, Yue Du, Jiyong Liu.  (2022)  Orally Deliverable Dual-Targeted Pellets for the Synergistic Treatment of Ulcerative Colitis.  Drug Design Development and Therapy,      [PMID:34616144] [10.2147/DDDT.S322702]

15. Sa-sa Zhang, Yi-jin Wu, Shu Pan, Qi-hai Wang, Wen-gang Chen, Zhong-fang Wang, Jin-ying Xu, Jian Zuo, Qin Yin.  (2022)  Xanthones from securidaca inappendiculata antagonizes the anti-rheumatic effect of methotrexate by inhibiting reduced folate carrier 1.  IMMUNOPHARMACOLOGY AND IMMUNOTOXICOLOGY,      [PMID:35850595] [10.1080/08923973.2022.2103707]

16. Yuanfang Kong, Yulong Hu, Jieming Li, Juntao Cai, Yuanhao Qiu, Chunhong Dong.  (2022)  Anti-inflammatory Effect of a Novel Pectin Polysaccharide From Rubus chingii Hu on Colitis Mice.  Frontiers in Nutrition,      [PMID:35571944] [10.3389/fnut.2022.868657]

17. Jieru Han, Wenhao Li, Guangyu Shi, Yunlei Huang, Xutao Sun, Na Sun, Deyou Jiang.  (2022)  Atractylenolide III Improves Mitochondrial Function and Protects Against Ulcerative Colitis by Activating AMPK/SIRT1/PGC-1α.  MEDIATORS OF INFLAMMATION,      [PMID:35431653] [10.1155/2022/9129984]

18. Hui Chen, Han Zhang, Lixing Cao, Jinling Cui, Xuan Ma, Chong Zhao, Shutao Yin, Hongbo Hu.  (2022)  Glucose Limitation Sensitizes Cancer Cells to Selenite-Induced Cytotoxicity via SLC7A11-Mediated Redox Collapse.  Cancers,  14  (2): (345).  [PMID:35053507] [10.3390/cancers14020345]

19. Jingjing Li, Suiyuan Ren, Meng Li, Jingai Bi, Guang Yang, Erguang Li.  (2021)  Paeoniflorin protects against dextran sulfate sodium (DSS)-induced colitis in mice through inhibition of inflammation and eosinophil infiltration.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:33887576] [10.1016/j.intimp.2021.107667]

20. Yajie Cai, Bing Xu, Fei Zhou, Jianzhi Wu, Shuo Li, Qi Zheng, Yajing Li, Xiaojiaoyang Li, Feng Gao, Shifen Dong, Runping Liu.  (2021)  Si-Ni-San ameliorates chronic colitis by modulating type I interferons-mediated inflammation.  PHYTOMEDICINE,      [PMID:33611210] [10.1016/j.phymed.2021.153495]

21. Longfa Kou, Rui Sun, Shuyi Xiao, Yawen Zheng, Zhiwei Chen, Aimin Cai, Hailun Zheng, Qing Yao, Vadivel Ganapathy, Ruijie Chen.  (2019)  Ambidextrous Approach To Disrupt Redox Balance in Tumor Cells with Increased ROS Production and Decreased GSH Synthesis for Cancer Therapy.  ACS Applied Materials & Interfaces,      [PMID:31276364] [10.1021/acsami.9b09784]

22. Yan Liu, Wenji Kang, Libo Nie, Fen Xiao, Yilong Li, Qinbin Ma, Danqi Lin, Guiyin Zhou, Sihua Liu, Kehui Sun, Xiangqian Li.  (2024)  Alginate/methacrylic acid/calcium ion-based pH-sensitive drug delivery hydrogel for the treatment of ulcerative colitis.  REACTIVE & FUNCTIONAL POLYMERS,      [PMID:] [10.1016/j.reactfunctpolym.2024.106025]

23. Yueqi Hu, Li Zhou, Jian Yang, Ruibin Bai, Eric Marchioni, Minjie Zhao, Li Zhou.  (2024)  Anti-inflammatory mechanism of Houttuynia cordata polysaccharides against ulcerative colitis based on multi-omics conjoint analysis.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:39521219] [10.1016/j.ijbiomac.2024.137311]

24. Shuang Li, Bingjie Wang, Jiaojiao Tao, Yu Dong, Teng Wang, Xia Zhao, Tianze Jiang, Lianxiao Zhang, Hai Yang.  (2024)  Chemodynamic therapy combined with endogenous ferroptosis based on “sea urchin-like” copper sulfide hydrogel for enhancing anti-tumor efficacy.  INTERNATIONAL JOURNAL OF PHARMACEUTICS,      [PMID:38866081] [10.1016/j.ijpharm.2024.124330]

25. Mengru Bai, Qian Shen, Yong Wu, Zhiyuan Ma, Yuqing Wang, Mingyang Chen, Dan Liu, Lin Zhou.  (2024)  Evaluation of transport mechanisms of methotrexate in human choriocarcinoma cell lines by LC-MS/MS.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:38823222] [10.1016/j.jpba.2024.116268]

26. Jingwen Guo, Yuanzhi He, Jiaqi Li, Min Lin, Yihan Wu, Jiayi Yang, Zehui He, Long Meng, Zhi Wang, Qing Xia, Chunyun Zhu, Yongtai Zhang, Nianping Feng.  (2025)  In Situ Hydrogel Transformed from Dicarboxylic Anhydride-Cross-Linked Cyclodextrin Nanosponge-Encapsulated Parthenolide Restored the Intestinal Mucosal Barrier of Ulcerative Colitis.  ACS Applied Materials & Interfaces,      [PMID:40096675] [10.1021/acsami.4c21687]

27. Lian Xu, Yan Xiao, Kun Yu, Hongshuo Pan, Jiayi Xu, Yiyun Guan, Mengke Wang, Xiangyu Xu, Hao Wang.  (2025)  Machine Learning-Assisted Chemical Tongues Based on Dual-channel Inclusion Complexes for Rapid Identification of Nonsteroidal Anti-inflammatory Drugs in Food.  ACS Sensors,      [PMID:39992799] [10.1021/acssensors.4c02806]

28. Cong Yuan, Xiaoxiao Zhu, Jiaqi Pan, Minghao Xu, Yongjun Jiang, Sheng Dai, Yikai Huang, Leixi Lu, Lei Zhou, Chengcheng Tian.  (2024)  Mechanical insight into direct singlet oxygen generation pathway: The significance of Co-O-X bond formation anchored by cobalt single atoms on mesoporous oxides.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2024.149364]

29. Tingting Chen, Gaoxiang Ai, Guihong Liang, Lingfeng Zeng, Di Zhao, Jun Liu, Yaoxing Dou.  (2024)  Mitigation of inflammatory bowel disease-related osteoporosis by oxyberberine: Insights into the RANKL/NF-κB signaling pathway.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:38574627] [10.1016/j.biopha.2024.116523]

30. Heung Lam MOK, Ka Wing CHENG, Yiqi XU, Chunhua HUANG, Cheng LYU, Jiaruo XU, Die HU, Lin ZHU, Chengyuan LIN, Hor-Yue TAN, Zhaoxiang BIAN.  (2024)  Modified Zhenwu Decoction suppresses chronic colitis via targeting macrophage CCR2/Fyn/p38 MAPK signaling axis.  PHYTOMEDICINE,      [PMID:38733904] [10.1016/j.phymed.2024.155694]

31. Yuzhen Kang, Dongyu Wu, Tiantian Zhang, Yue Zhang, Yan Zhong, Shiqi Chen, Xiaoyu Wang, Xuyu Chai.  (2025)  Synthesis and characterization of Poly(N-Acryloyl 6-aminocaproic acid) for intestine-specific drug delivery.  JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY,      [PMID:] [10.1016/j.jddst.2025.106760]

32. Chunhua Huang, Cheng Lyu, Heung-Lam Mok, Yiqi Xu, Ka-Wing Cheng, Cheng Zhang, Die Hu, Lin Zhu, Chengyuan Lin, Xin Chen, Hor-Yue Tan, Zhaoxiang Bian.  (2024)  Tolerogenic dendritic cell-mediated regulatory T cell differentiation by Chinese herbal formulation attenuates colitis progression.  Journal of Advanced Research,      [PMID:38677546] [10.1016/j.jare.2024.04.023]

33. Zhuyun Wang, Weiyan Yan, Xiaojing Lin, Guangcheng Qin, Kemeng Li, Lincheng Jiang, Xingwang Li, Xiaoqiu Xiao, Ting Luo, Yi Hou.  (2025)  Forsythiaside A Alleviates Ulcerative Colitis and Inhibits Neutrophil Extracellular Traps Formation in the Mice.  PHYTOTHERAPY RESEARCH,      [PMID:40099671] [10.1002/ptr.8440]

34. Jie Yuan, Chongyong Gao, Wang Xin, Fanlin Meng, Hong Zhang.  (2025)  Screening and validation of 3’-Methoxydaidzein as a therapeutic agent in ulcerative colitis based on disulfidptosis-associated molecular clusters.  PLoS One,  20  (6): (e0324586).  [PMID:40478904] [10.1371/journal.pone.0324586]

35. Chunxiao Tao, Fazhen Luo, Yaxin Wang, Xiaoya Gao, Yuqi Cao, Keke Wang, Yan Xie.  (2025)  Mannose-modified Prunus persica kernel protein nanoparticles loading baicalin coated with Lycium barbarum polysaccharide for ulcerative colitis treatment.  CARBOHYDRATE POLYMERS,      [PMID:41198305] [10.1016/j.carbpol.2025.124489]

36. Lu Li, Qinglin Fei, Xuwen Sun, Qiaochun Wang, Jianhua Su, Longyun Ye, Weiding Wu, Lifang Guo.  (2025)  Ferroptosis Pathway Discrimination and Anticancer Therapeutic Screening Enabled by Cascade-Activated Fluorescence Reporting of Cysteine-Viscosity Dynamics.  ANALYTICAL CHEMISTRY,      [PMID:41191406] [10.1021/acs.analchem.5c03834]

37. Junwei Liu, Xinyue Yang, Tao Gao, Yuehan Zhang, Dandan Pan, Jian He, Xiangwei Wu.  (2025)  Revealing the anaerobic biodegradation pathway and mechanism of sulfamethoxazole by a novel Cupidesulfovibrio sp. strain SA-9.  WATER RESEARCH,      [PMID:41389422] [10.1016/j.watres.2025.125118]

38. Zhou Qiao, Huan Tong, Ziyuan Wang, Jia Liu, Xi Chen, Zhe Song, Yun Wang.  (2025)  Dehydrodiisoeugenol attenuates ulcerative colitis via regulating Anaerostipes caccae-mediated uric acid metabolism.  PHYTOMEDICINE,      [PMID:41447836] [10.1016/j.phymed.2025.157721]

39. Si-yu Liu, Chang-qing Wang, Tong-tong Luo, Gui-juan Cui, Yuan Zhang, Xing-ju Zou, Zi-jian Zhang, Wen-xiu Liu, Chen Sun, Cheng Peng.  (2025)  Baicalin ameliorates ulcerative colitis by regulating macrophage polarization through the JAK1/STAT1/SOCS1 pathway.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:41423154] [10.1016/j.jep.2025.121057]

40. SiJia Lin, Lin Wang, Xue Dong, ZiYi Wang, Jin Cao, Xueyong Qi, Lin Wu, Jing Zhang, Song Shen.  (2025)  Precision Ferroptosis Amplification via SLC7A11-Directed Proteasomal Degradation for Enhanced Cancer Therapy.  Advanced Healthcare Materials,      [PMID:41467569] [10.1002/adhm.202504602]

41. Ji Wanli, Song Xingyue, Liang Xinning, Zheng Yashuo, Qian Xiaojing, Hu Cheng, Huo Yan.  (2026)  Banxia Xiexin Decoction modulates short-chain fatty acid metabolism and mitigates ulcerative colitis by reshaping the intestinal microbiota.  JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS,      [PMID:41500036] [10.1016/j.jpba.2025.117332]

42. Cong Yuan, Xiaoxiao Zhu, Xuyang Xu, Fengyun Ding, Lei Zhou, Jean-Marc Chovelon, Wanglai Cen, Chengcheng Tian.  (2026)  Dual Anchoring Strategy for Single-Atom Fe Catalysts: Insights into 1O2-Driven Oxidation of Organic Contaminants.  Journal of Environmental Chemical Engineering,      [PMID:] [10.1016/j.jece.2026.121190]

43. Yuzhe Wang, Lu sheng, Lin Bu, Huijuan Li, Jianxin Wu, Qing Huang.  (2026)  A novel epidermal mimicking phospholipid vesicle-based permeation assay: EpiPVPA for in vitro permeation evaluation.  INTERNATIONAL JOURNAL OF PHARMACEUTICS,      [PMID:41558553] [10.1016/j.ijpharm.2026.126595]

44. Weiying Liu, Zijian Zhang, Wanxing Wu, Xiaoyu Yan, Yijia Huang, Han Feng, Qiaoxing Mou, Jie Wan, Mengfan Yan, Huayang Tang, Jie Liang, Ying Zhang, Cheng Peng, Xiaoqi Pan.  (2026)  Ligilactobacillus murinus Confers a Dual Benefit: Counteracting Crotonis Fructus-induced Intestinal Toxicity and Synergizing with Its Processed Form against Ulcerative Colitis.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:41730403] [10.1016/j.jep.2026.121420]

45. Yu Liao, Weipeng Wei, Fuli Qin, Yusheng Ruan, Ting He, Jiansong He, Mingchao Wang, Taotao Liu, Jiemei Chen.  (2026)  Cordycepin Ameliorates Dextran Sulfate Sodium-Induced Ulcerative Colitis in Mice by Inhibiting IL-6/IL-6R-Mediated p38 MAPK and NF-κB Activation Through Adenosine A2A Receptor Stimulation.  Drug Design Development and Therapy,      [PMID:] [10.2147/DDDT.S575035]