SB 203580

  ( 80 citations )    
Product Datasheet
Catalog Number:1202
Chemical Name:4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine
Product Details
Citations (80)
Reviews
Biological Activity
Selective inhibitor of p38 MAPK (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK-3β and PKBα. Shown to inhibit IL-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase. Enhances clonal growth of skin epithelial progenitor cells; stimulates neural stem cell (NSC) proliferation. Essential component of medium for maintaining stem cells in naive pluripotent state.

Available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Water-soluble Salt also available.

Technical Data
  • M.Wt:
    377.44
  • Formula:
    C21H16FN3OS
  • Solubility:
    Soluble to 25 mM in DMSO and to 100 mM in 1eq. HCl
  • Purity:
    >98
  • Storage:
    Desiccate at +4°C
  • CAS No:
    152121-47-6
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of GlaxoSmithKline
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Citations:

The citations listed below are publications that use Tocris products. Selected citations for SB 203580 include:

80 Citations: Showing 1 - 10
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  1. TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells.
    Authors: Wu
    Arch Biochem Biophys  2017;622:26
  2. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res  2017;1663:132
  3. The PDGF-BB-SOX7 axis-modulated IL-33 in pericytes and stromal cells promotes metastasis through tumour-associated macrophages.
    Authors: Yang Et al.
    Cardiorenal Med  2016;7:11385
  4. Derivation of Patient Specific Pluripotent Stem Cells Using Clinically Discarded Cumulus Cells.
    Authors: Chang Et al.
    PLoS One  2016;11:e0165715
  5. 18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis.
    Authors: Rahman Et al.
    Biochemical Pharmacology  2016;117:97
  6. STAT3 signaling contributes to the high effector activities of interleukin-15-derived dendritic cells.
    Authors: Okada Et al.
    Int J Mol Med  2015;93:461
  7. Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment.
    Authors: Liu Et al.
    Biogerontology  2015;5:79
  8. Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
    Authors: Koerber Et al.
    Mol Vis  2015;4:21
  9. MAPK signaling downstream to TLR4 contributes to paclitaxel-induced peripheral neuropathy.
    Authors: Li Et al.
    Brain Behav.Immun.  2015;49:255
  10. Developmental alterations in centrosome integrity contribute to the post-mitotic state of mammalian cardiomyocytes.
    Authors: Zebrowski Et al.
    Mol Vis  2015;4
  11. MFG-E8 inhibits neutrophil migration through αvβ3-integrin-dependent MAP kinase activation.
    Authors: Aziz Et al.
    Elife  2015;36:18
  12. Regulation of the hyperosmotic induction of aquaporin 5 and VEGF in retinal pigment epithelial cells: involvement of NFAT5.
    Authors: Hollborn Et al.
    Oncotarget  2015;21:360
  13. Gene expression regulation in retinal pigment epithelial cells induced by viral RNA and viral/bacterial DNA.
    Authors: Brosig Et al.
    Immunol Cell Biol  2015;21:1000
  14. P2X7 Receptor Regulates Internalization of Antimicrobial Peptide LL-37 by Human Macrophages That Promotes Intracellular Pathogen Clearance.
    Authors: Tang Et al.
    J Immunol  2015;195:1191
  15. Macrophage migration inhibitory factor-CXCR4 is the dominant chemotactic axis in human mesenchymal stem cell recruitment to tumors.
    Authors: Lourenco Et al.
    J Immunol  2015;194:3463
  16. Nijmegen breakage syndrome fibroblasts expressing the C-terminal truncated NBN(p70) protein undergo p38/MK2-dependent premature senescence.
    Authors: Davis Et al.
    Exp Hematol Oncol  2015;16:43
  17. JNK2 controls fragmentation of the Golgi complex and the G2/M transition through phosphorylation of GRASP65.
    Authors: Cervigni Et al.
    J Cell Sci  2015;128:2249
  18. 1α,25-Dihydroxyvitamin D3 Induces Neutrophil Apoptosis through the p38 MAPK Signaling Pathway in Chronic Obstructive Pulmonary Disease Patients.
    Authors: Yang Et al.
    PLoS One  2015;10:e0120515
  19. Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation.
    Authors: Yu Et al.
    PLoS One  2014;9:e112989
  20. Distinct signalling pathways of murine histamine H1- and H4-receptors expressed at comparable levels in HEK293 cells.
    Authors: Beermann Et al.
    Respir Res  2014;9:e107481
  21. Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α.
    Authors: Gonsalves Et al.
    Am J Hematol  2014;89:273
  22. AMP-activated protein kinase determines apoptotic sensitivity of cancer cells to ginsenoside-Rh2.
    Authors: Kim Et al.
    J Ginseng Res  2014;38:16
  23. Central SDF-1/CXCL12 expression and its cardiovascular and sympathetic effects: the role of angiotensin II, TNF-α, and MAP kinase signaling.
    Authors: Wei Et al.
    Am J Physiol Heart Circ Physiol  2014;307:H1643
  24. Activation of pattern recognition receptors in brown adipocytes induces inflammation and suppresses uncoupling protein 1 expression and mitochondrial respiration.
    Authors: Bae Et al.
    Am J Physiol Cell Physiol  2014;306:C918
  25. Cathelicidin LL-37 induces time-resolved release of LTB4 and TXA2 by human macrophages and triggers eicosanoid generation in vivo.
    Authors: Wan Et al.
    FASEB J  2014;28:3456
  26. Network dynamics determine the autocrine and paracrine signaling functions of TNF.
    Authors: Caldwell Et al.
    Genes Dev  2014;28:2120
  27. ERK/MAPK regulates ERRγ expression, transcriptional activity and receptor-mediated tamoxifen resistance in ER+ breast cancer.
    Authors: Heckler Et al.
    FEBS J  2014;281:2431
  28. Decrease of PKB/Akt Phosphorylation is Partially Mediated by SAPK/JNK Activation in Serum-free L6 Myoblasts Starved with Low Glucose.
    Authors: Kim Et al.
    J Phys Ther Sci  2014;26:1757
  29. p38 MAPK signaling underlies a cell-autonomous loss of stem cell self-renewal in skeletal muscle of aged mice.
    Authors: Bernet Et al.
    Korean J Physiol Pharmacol  2014;20:265
  30. δ-Opioid receptors up-regulate excitatory amino acid transporters in mouse astrocytes.
    Authors: Liang Et al.
    Exp Eye Res  2014;171:5417
  31. Transcriptional regulation of an insulin-sensitizing adipokine adipolin/CTRP12 in adipocytes by Krüppel-like factor 15.
    Authors: Enomoto Et al.
    Mol Med  2013;8:e83183
  32. A novel model of dormancy for bone metastatic breast cancer cells.
    Authors: Marlow Et al.
    Cancer Res  2013;73:6886
  33. Effect of thioridazine on erythrocytes.
    Authors: Lang Et al.
    Toxins (Basel)  2013;5:1918
  34. EI24 regulates epithelial-to-mesenchymal transition and tumor progression by suppressing TRAF2-mediated NF-κB activity.
    Authors: Choi Et al.
    PLoS One  2013;4:2383
  35. Epigallocatechin gallate (EGCG) stimulates autophagy in vascular endothelial cells: a potential role for reducing lipid accumulation.
    Authors: Kim Et al.
    J Biol Chem  2013;288:22693
  36. A Taiwanese Propolis Derivative Induces Apoptosis through Inducing Endoplasmic Reticular Stress and Activating Transcription Factor-3 in Human Hepatoma Cells.
    Authors: Suk Et al.
    Evid Based Complement Alternat Med  2013;2013:658370
  37. p38α senses environmental stress to control innate immune responses via mechanistic target of rapamycin.
    Authors: Katholnig Et al.
    J Immunol  2013;190:1519
  38. An ERK-p38 subnetwork coordinates host cell apoptosis and necrosis during coxsackievirus B3 infection.
    Authors: Jensen Et al.
    J Neurosci  2013;13:67
  39. Inhibition of a novel specific neuroglial integrin signaling pathway increases STAT3-mediated CNTF expression.
    Authors: Keasey Et al.
    Cell Commun Signal  2013;11:35
  40. Gremlin utilizes canonical and non-canonical TGFβ signaling to induce lysyl oxidase (LOX) genes in human trabecular meshwork cells.
    Authors: Sethi Et al.
    J Neuroinflammation  2013;113:117
  41. Distinct regulatory functions of calpain 1 and 2 during neural stem cell self-renewal and differentiation.
    Authors: Santos Et al.
    PLoS One  2012;7:e33468
  42. TLR signaling paralyzes monocyte chemotaxis through synergized effects of p38 MAPK and global Rap-1 activation.
    Authors: Yi Et al.
    PLoS One  2012;7:e30404
  43. Rit GTPase regulates a p38 MAPK-dependent neuronal survival pathway.
    Authors: Cai Et al.
    J Cell Mol Med  2012;531:125
  44. Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice.
    Authors: Khuituan Et al.
    Am J Physiol Endocrinol Metab  2012;302:E903
  45. TAK-1/p38/nNFκB signaling inhibits myoblast differentiation by increasing levels of Activin A.
    Authors: Trendelenburg Et al.
    Skelet Muscle  2012;2:3
  46. Inhibition of α-SMA by the ectodomain of FGFR2c attenuates lung fibrosis.
    Authors: Ju Et al.
    Diabetologia  2012;18:992
  47. Cyclic AMP increases COX-2 expression via mitogen-activated kinase in human myometrial cells.
    Authors: Chen Et al.
    PLoS One  2012;16:1447
  48. Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways.
    Authors: Meotti Et al.
    Br J Pharmacol  2012;166:1127
  49. The neuropeptide PACAP38 induces dendritic spine remodeling through ADAM10-N-cadherin signaling pathway.
    Authors: Gardoni Et al.
    J Cell Sci  2012;125:1401
  50. Brain microvascular pericytes are immunoactive in culture: cytokine, chemokine, nitric oxide, and LRP-1 expression in response to lipopolysaccharide.
    Authors: Kovac Et al.
    J Biol Chem  2011;8:139
  51. Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth.
    Authors: Zhou and Too
    Nat Med  2011;6:e21680
  52. Role of TGFβ/Smad signaling in gremlin induction of human trabecular meshwork extracellular matrix proteins.
    Authors: Sethi Et al.
    PLoS One  2011;52:5251
  53. Induction of steroid sulfatase expression by tumor necrosis factor-α through phosphatidylinositol 3-kinase/Akt signaling pathway in PC-3 human prostate cancer cells.
    Authors: Suh Et al.
    Exp Mol Med  2011;43:646
  54. Reversible differentiation of myofibroblasts by MyoD.
    Authors: Hecker Et al.
    J Neurosci  2011;317:1914
  55. Real-time imaging reveals that P2Y2 and P2Y12 receptor agonists are not chemoattractants and macrophage chemotaxis to complement C5a is phosphatidylinositol 3-kinase (PI3K)- and p38 mitogen-activated protein kinase (MAPK)-independent.
    Authors: Isfort Et al.
    J Biol Chem  2011;286:44776
  56. MUC5AC expression through bidirectional communication of Notch and epidermal growth factor receptor pathways.
    Authors: Kang Et al.
    J Immunol  2011;187:222
  57. Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells.
    Authors: Kim Et al.
    Mol Cancer  2011;15:211
  58. Carnosic acid induces the NAD(P)H: quinone oxidoreductase 1 expression in rat clone 9 cells through the p38/nuclear factor erythroid-2 related factor 2 pathway.
    Authors: Tsai Et al.
    J Nutr  2011;141:2119
  59. TWEAK is a positive regulator of cardiomyocyte proliferation.
    Authors: Novoyatleva Et al.
    Toxins (Basel)  2010;85:681
  60. Redox Factor-1 Inhibits Cyclooxygenase-2 Expression via Inhibiting of p38 MAPK in the A549 Cells.
    Authors: Yoo Et al.
    Korean J Physiol Pharmacol  2010;14:139
  61. Cigarette smoke and lipopolysaccharide induce a proliferative airway smooth muscle phenotype.
    Authors: Pera Et al.
    Exp Cell Res  2010;11:48
  62. miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon production by human plasmacytoid dendritic cells.
    Authors: Zhou Et al.
    Blood  2010;116:5885
  63. PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
    Authors: Doulatov Et al.
    Genes Dev  2009;23:2076
  64. Ethanol augments RANTES/CCL5 expression in rat liver sinusoidal endothelial cells and human endothelial cells via activation of NF-kappa B, HIF-1 alpha, and AP-1.
    Authors: Yeligar Et al.
    J Immunol  2009;183:5964
  65. The expression of the beta-defensins hBD-2 and hBD-3 is differentially regulated by NF-kappaB and MAPK/AP-1 pathways in an in vitro model of Candida esophagitis.
    Authors: Steubesand Et al.
    BMC Immunol  2009;10:36
  66. Assessing the role of stress signalling via p38 MAP kinase in the premature senescence of ataxia telangiectasia and Werner syndrome fibroblasts.
    Authors: Davis and Kipling
    Biogerontology  2009;10:253
  67. Mitogen-activated protein kinases mediate upregulation of hypothalamic angiotensin II type 1 receptors in heart failure rats.
    Authors: Wei Et al.
    Hypertension  2008;52:679
  68. Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells.
    Authors: Jung Et al.
    Carcinogenesis  2008;29:713
  69. Induction of human beta-defensin 2 by the probiotic Escherichia coli Nissle 1917 is mediated through flagellin.
    Authors: Schlee Et al.
    Infect Immun  2007;75:2399
  70. Delayed and persistent ERK1/2 activation is required for 4-hydroxytamoxifen-induced cell death.
    Authors: Zhou Et al.
    Invest Ophthalmol Vis Sci  2007;72:765
  71. Requirement of extracellular signal-regulated kinase/mitogen-activated protein kinase for long-term potentiation in adult mouse anterior cingulate cortex.
    Authors: Toyoda Et al.
    Mol Pain  2007;3:36
  72. Somatic excision demonstrates that c-Jun induces cellular migration and invasion through induction of stem cell factor.
    Authors: Katiyar Et al.
    Mol Cell Biol  2007;27:1356
  73. Paclitaxel-induced nuclear translocation of FOXO3a in breast cancer cells is mediated by c-Jun NH2-terminal kinase and Akt.
    Authors: Sunters Et al.
    Cancer Res  2006;66:212
  74. Role of glycogen synthase kinase 3 β (GSK3β) in mediating the cytotoxic effects of the histone deacetylase inhibitor trichostatin A (TSA) in MCF-7 breast cancer cells.
    Authors: Alao Et al.
    Steroids  2006;5:40
  75. The role of protein kinase B/Akt in insulin-induced inactivation of phosphorylase in rat hepatocytes.
    Authors: Aiston Et al.
    Cardiovasc Res  2006;49:174
  76. Regulation of nuclear factor κB in the hippocampus by group I metabotropic glutamate receptors.
    Authors: O'Riordan Et al.
    Cell Host Microbe  2006;26:4870
  77. Direct phosphorylation and regulation of poly(ADP-ribose) polymerase-1 by extracellular signal-regulated kinases 1/2.
    Authors: Kauppinen Et al.
    Proc Natl Acad Sci U S A  2006;103:7136
  78. beta-Amyloid peptides impair PKC-dependent functions of metabotropic glutamate receptors in prefrontal cortical neurons.
    Authors: Tyszkiewicz and Yan
    J Neurophysiol  2005;93:3102
  79. Glucose deprivation increases mRNA stability of vascular endothelial growth factor through activation of AMP-activated protein kinase in DU145 prostate carcinoma.
    Authors: Yun Et al.
    Nat Commun  2005;280:9963
  80. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1.
    Authors: Gallagher Et al.
    Neurosci Lett  2004;24:4859
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