Sulfasalazine (NSC 667219)

Licensed by Pfizer Catalog No.S1576 Synonyms: Azulfidine, Salazopyrin, Sulphasalazine

For research use only.

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 kappa B (NF-κB), TGF-β and COX-2. Sulfasalazine induces ferroptosis, apoptosis and autophagy.

Sulfasalazine (NSC 667219) Chemical Structure

CAS No. 599-79-1

Selleck's Sulfasalazine (NSC 667219) has been cited by 14 publications

Purity & Quality Control

Choose Selective Immunology & Inflammation related Inhibitors

Biological Activity

Description 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 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

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Flp-In MmDBSpVv[3Srb36gZZN{[Xl? MnTwTY5pcWKrdHnvckBw\iCqdX3hckBtcX[ncjDPRXRROUJzIHX4dJJme3OnZDDpckBJTUt{OUOgSoxxNUmwIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBGOTdvYnX0ZWchfXC2YXvlJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGtqRTBwNUROwG0> MlrlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEGwOlgoRjJ{NUSxNFY5RC:jPh?=
HEK293 Flp-In M3P0XmZ2dmO2aX;uJIF{e2G7 M3rCO2lvcGmkaYTpc44hd2ZiaIXtZY4hdGm4ZYKgU2FVWDGEMTDlfJBz\XO|ZXSgbY4hUEWNMkmzJGZteC2LbjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hTTF5LXLleIFIKHWydHHr[UBjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUCuOVbPxE1? NFHVeHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW0NVA3QCd-MkK1OFExPjh:L3G+
HepG2 M2e3NmZ2dmO2aX;uJIF{e2G7 M4PlRlEhcHJ? Ml;LTY5pcWKrdHnvckBw\iCQRj3rZZBx[UJiYXP0bZZifGmxbjDlfJBz\XO|ZXSgbY4hXE6IYXzwbIEue3SrbYXsZZRm\CCqdX3hckBJ\XCJMjDj[YxteyClbz30doFve2[nY4Tl[EB4cXSqIGDQVmUuVHWlIIDsZZNucWRicILleJJm[XSnZDDmc5IhOSCqcjDi[YZwemViVF7GZYxxcGFiY3jhcIxmdmenIH3lZZN2emWmIHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;MD65{txO NFS2UVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi4PVM{Pid-MkG4PFk{OzZ:L3G+
HepG2 M1XEOWZ2dmO2aX;uJIF{e2G7 M{noT|EhcHJ? NX\vPW9zUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSotieHCjQjDhZ5RqfmG2aX;uJIlvKGi3bXHuJGhmeEd{IHPlcIx{KGGodHXyJFEhcHJiYomgcJVkcW[ncnHz[UBz\XCxcoTldkBie3OjeTygTWM2OD1yLkpOwG0> NH\6Ooc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi3NFg{OSd-MkG4O|A5OzF:L3G+
HepG2 NGHnbmlHfW6ldHnvckBie3OjeR?= MXexJIhz MmLsTY5pcWKrdHnvckBw\iCWTl\hcJBp[S2rbnT1Z4VlKE6Ia3HwdIFDKHS{YX7zZ5JqeHSrb37hcEBi[3Srdnn0fUBqdiCqdX3hckBJ\XCJMjDj[YxteyCycnX0doVifGWmIH\vdkAyKGi{IHLl[o9z\SCWTl\hcJBp[SClaHHscIVv\2ViYomgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHuZYx6e2m|LDDJR|UxRTBwOd88US=> NX7iOlRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKzPFExPDdpPkKyN|gyODR5PD;hQi=>
HepG2 M1HVSWZ2dmO2aX;uJIF{e2G7 MmTVNUBpeg>? M{LITWlvcGmkaYTpc44hd2ZiTl[tb4FxeGGEIHX4dJJme3OnZDDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHRPTmGucHjhMYlv\HWlZXSgcJVkcW[ncnHz[UBi[3Srdnn0fUBxemWrbnP1ZoF1\WRiZn;yJFEhcHJiZn;scI94\WRiYomgWG5H[WyyaHGgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IEGgbJIh[nlicnXwc5J1\XJiZ3Xu[UBie3OjeTygTWM2OD1yLkpOwG0> MkPGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNyM{G1PVYoRjJ|MEOxOVk3RC:jPh?=
HepG2 M1vJN2Z2dmO2aX;uJIF{e2G7 NHi4dGoyKGi{ M2rBXWlvcGmkaYTpc44hd2ZiVF7GMYFteGijLXnu[JVk\WRiTl[tb4FxeGGEIITyZY5{[3KrcITpc45idCCjY4TpeoF1cW:wIHnuJIh2dWGwIFjldGczKGOnbHzzJJBz\WmwY4XiZZRm\CCob4KgNUBpeiCob3zsc5dm\CCkeTDUUmYu[WyyaHGgZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IEGgbJIh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuPe69VQ>? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDNzNEO5Okc,OjR|MUSzPVY9N2F-
HEK293 Flp-In MXzGeY5kfGmxbjDhd5NigQ>? MmLzOUBucW6| NXzYSW11UW6qaXLpeIlwdiCxZjDoeY1idiCuaY\ldkBQSVSSMlKxJIV5eHKnc4Pl[EBqdiCKRVuyPVMhTmyyLVnuJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCdM1jdSVNUKHWydHHr[UBqdmO3YnH0[YQh\m:{IEWgcYlveyCkeTDzZ4lvfGmubHH0bY9vKGOxdX70bY5oNCCNaU2z{txO M3e5T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSxNFY5Lz5{MkW0NVA3QDxxYU6=
HEK293 Flp-In MWXGeY5kfGmxbjDhd5NigQ>? MUi1JI1qdnN? Mmm3TY5pcWKrdHnvckBw\iCqdX3hckBtcX[ncjDPRXRROkJzIHX4dJJme3OnZDDpckBJTUt{OUOgSoxxNUmwIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBcO0ifRUPTJJVxfGGtZTDpcoN2[mG2ZXSg[o9zKDVibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUROwG0> M2ixV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSxNFY5Lz5{MkW0NVA3QDxxYU6=
U2OS NX;mfXdrTnWwY4Tpc44h[XO|YYm= M1LlWVExKG2rboO= NIDKOpFKdmirYnn0bY9vKG:oIFjBMZRi\2enZDDoeY1idiCQVFPQJIV5eHKnc4Pl[EBqdiCqdX3hckBWOk:VIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBcOTSFXYTheZJw[2ixbHH0[UB2eHSja3WgdJJmcW6ldXLheIVlKG[xcjCxNEBucW6|IH\vcIxwf2WmIHL5JHsyPEOfIITheZJw[2ixbHH0[UBi\GSrdHnvckBidmRiZoXyeIhmeiCrbnP1ZoF1cW:wIH\vdkAyOCCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR|UxRTlwNt88US=> MlzVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzF2M{mzO|koRjNzNEO5N|c6RC:jPh?=
HEK293 Flp-In MYXGeY5kfGmxbjDhd5NigQ>? NUn1OHdQPSCvaX7z NEX5eodKdmirYnn0bY9vKG:oIHj1cYFvKGyrdnXyJG9CXFBzQkOg[ZhxemW|c3XkJIlvKEiHS{K5N{BHdHBvSX6gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJIlvKFt|SG3FNVcu[mW2YVegeZB1[WunIHnuZ5Vj[XSnZDDmc5IhPSCvaX7zJIJ6KHOlaX70bYxt[XSrb36gZ492dnSrbnesJGtqRTFzzszN M{PTXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{NUSxNFY5Lz5{MkW0NVA3QDxxYU6=
HEK293 Flp-In NIrJUVFHfW6ldHnvckBie3OjeR?= MXq1JI1qdnN? NYLZcWxUUW6qaXLpeIlwdiCxZjDoeY1idiCuaY\ldkBQSVSSMVKzJIV5eHKnc4Pl[EBqdiCKRVuyPVMhTmyyLVnuJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCdM1jdSVE4NWKndHHHJJVxfGGtZTDpcoN2[mG2ZXSg[o9zKDVibXnud{BjgSC|Y3nueIltdGG2aX;uJINwfW62aX7nMEBKSzVyPUGy{txO MnS4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ3NEGwOlgoRjJ{NUSxNFY5RC:jPh?=
U87 NHLvfFlHfW6ldHnvckBie3OjeR?= MonCNVUhdWmwcx?= MknETY5pcWKrdHnvckBw\iC6Yz3jfZN1cW6nLXfseZRidWG2ZTDhcpRqeG:{dHXyMY1m\GmjdHXkJIN6e3SrbnWgeZB1[WunIHnuJIh2dWGwIGW4O{Bk\WyuczD1d4lv\yCOLWuxOGNe[3m|dHnu[UBieyC|dXLzeJJifGViYX\0[ZIhOTVibXnud{BjgSCuaYH1bYQhe2OrboTpcIxifGmxbjDjc5VvfGmwZzygTWM2OD1|MN88US=> MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTh6OUOzO{c,OjF6OEmzN|c9N2F-
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]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 80 mg/mL
(200.8 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 398.39
Formula

C18H14N4O5S

CAS No. 599-79-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04720183 Completed Drug: Sulfasalazine|Drug: GLPG3970 Healthy Galapagos NV January 11 2021 Phase 1
NCT03487926 Active not recruiting Radiation: [18F]FEPPA Major Depressive Episode|Inflammatory Bowel Diseases Centre for Addiction and Mental Health|McMaster University January 1 2019 --
NCT01577966 Completed Drug: Sulfasalazine Brain Tumor University of Alabama at Birmingham January 2012 Not Applicable
NCT01474291 Completed Biological: Tocilizumab Rheumatoid Arthritis Hoffmann-La Roche January 2012 --
NCT00637780 Terminated Drug: Sulfasalazine Arthritis Juvenile Rheumatoid Pfizer June 2010 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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