SB 202190

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1264/10
1264/50
SB 202190 | CAS No. 152121-30-7 | p38 Inhibitors
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Description: Potent, selective inhibitor of p38 MAPK

Chemical Name: 4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol

Purity: ≥99%

Product Details
Citations (36)
Reviews (2)

Biological Activity

SB 202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase. Binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2 respectively). Promotes stability of naive human pluripotent stem cells in culture. Inhibits Yamanaka factor reprogramming of human fibroblasts to iPSCs. SB 202190 improves the self-renewal ability of neuronal stem cells from NPC1-deficient mice.

Technical Data

M.Wt:
331.35
Formula:
C20H14N3OF
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
152121-30-7

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline

Background References

  1. Derivation of novel human ground state naive pluripotent stem cells.
    Gafni O, Weinberger L, Mansour AA et al.
    Nature
  2. TGFbeta-mediated suppression of CD248 in non-cancer cells via canonical Smad-dependent signaling pathways is uncoupled in cancer cells.
    Suresh Babu S, Valdez Y, Xu A, O'Byrne A, Calvo F, Lei V, Conway E
    BMC Cancer, 2014;14(0):113.
  3. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
    Fox JT, Sakamuru S, Huang R
    Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8.
  4. FHL2 promotes tubular epithelial-to-mesenchymal transition through modulating ?-catenin signalling
    T Cai, D Sun, Y Duan, Y Qiu, C Dai, J Yang, W He
    J. Cell. Mol. Med., 2017;0(0):.
  5. IL-17A causes depression-like symptoms via NF?B and p38MAPK signaling pathways in mice: Implications for psoriasis associated depression
    A Nadeem, SF Ahmad, NO Al-Harbi, AS Fardan, AM El-Sherbee, KE Ibrahim, SM Attia
    Cytokine, 2017;97(0):14-24.
  6. Role of IL-18 induced Amphiregulin expression on virus induced ocular lesions
    SK Varanasi, NK Rajasagi, U Jaggi, BT Rouse
    Mucosal Immunol, 2018;0(0):.
  7. Three-Dimensional Organoids Reveal Therapy Resistance of Esophageal and Oropharyngeal Squamous Cell Carcinoma Cells
    T Kijima, H Nakagawa, M Shimonoson, PM Chandramou, T Hara, V Sahu, Y Kasagi, O Kikuchi, K Tanaka, V Giroux, AB Muir, KA Whelan, S Ohashi, S Naganuma, AJ Klein-Szan, Y Shinden, K Sasaki, I Omoto, Y Kita, M Muto, AJ Bass, JA Diehl, GG Ginsberg, Y Doki, M Mori, Y Uchikado, T Arigami, NG Avadhani, D Basu, AK Rustgi, S Natsugoe
    Cell Mol Gastroenterol Hepatol, 2019;7(1):73-91.
  8. Human SR-BII mediates SAA uptake and contributes to SAA pro-inflammatory signaling in vitro and in vivo
    IN Baranova, ACP Souza, AV Bocharov, TG Vishnyakov, X Hu, BL Vaisman, MJ Amar, Z Chen, AT Remaley, AP Patterson, PST Yuen, RA Star, TL Eggerman
    PLoS ONE, 2017;12(4):e0175824.
  9. BlyS is up-regulated by hypoxia and promotes migration of human breast cancer cells.
    Zhu J, Sun L, Lin S
    J. Exp. Clin. Cancer Res., 2012;31(0):31.
  10. Improving Cell Survival in Injected Embryos Allows Primed Pluripotent Stem Cells to Generate Chimeric Cynomolgus Monkeys
    Y Kang, Z Ai, K Duan, C Si, Y Wang, Y Zheng, J He, Y Yin, S Zhao, B Niu, X Zhu, L Liu, L Xiang, L Zhang, Y Niu, W Ji, T Li
    Cell Rep, 2018;25(9):2563-2576.e9.
  11. Evaluating S. flexneri pathogenesis in the human enteroid model
    S Ranganatha, M Doucet, CL Grassel, B Delaine-El, NC Zachos, EM Barry
    Infect. Immun., 2019;0(0):.
  12. Regulation of the CCL2 Gene in Pancreatic beta-Cells by IL-1beta and Glucocorticoids: Role of MKP-1.
    Burke S, Goff M, Updegraff B, Lu D, Brown P, Minkin S, Biggerstaff J, Zhao L, Karlstad M, Collier J
    PLoS ONE, 2012;7(10):e46986.
  13. Specificity and mechanism of action of some commonly used protein kinase inhibitors.
    Davies et al.
    Biochem.J., 2000;351:95
  14. The activation of p38 mitogen-activated protein kinase determines the efficiency of ATP competition for pyridinylimidazole inhibitor binding.
    Frantz et al.
    Biochemistry, 1998;37:13846
  15. Characterization of the structure and function of a new mitogen-activated protein kinase (p38β).
    Jiang et al.
    J.Biol.Chem., 1996;271:17920
  16. Induction of apoptosis by SB 202190 through inhibition of p38β mitogen-activated protein kinase.
    Nemoto et al.
    J.Biol.Chem., 1998;273:16415
  17. In vitro expansion of human gastric epithelial stem cells and their responses to bacterial infection.
    Bartfeld et al.
    Gastroenterology, 2015;148:126
  18. Identification of multipotent luminal progenitor cells in human prostate organoid cultures.
    Karthaus et al.
    Cell, 2014;159:163
  19. SnapShot: Growing Organoids from Stem Cells.
    Sato et al.
    Cell, 2015;161:1700
  20. A critical role for p38MAPK signalling pathway during reprogramming of human fibroblasts to iPSCs.
    Neganova et al.
    Sci.Rep., 2017;7:41693
  21. Long-term expansion of epithelial organoids from human colon, adenoma, adenocarcinoma, and Barrett's epithelium.
    Sato et al.
    Gastroenterology, 2011;141:1762
  22. NPC1 gene deficiency leads to lack of neural stem cell self-renewal and abnormal differentiation through activation of p38 mitogen-activated protein kinase signaling.
    Yang et al.
    Stem Cells, 2006;24:292
  23. A pan-cancer organoid platform for precision medicine
    BM Larsen, M Kannan, LF Langer, BD Leibowitz, A Bentaieb, A Cancino, I Dolgalev, BE Drummond, JR Dry, CS Ho, G Khullar, BA Krantz, B Mapes, KE McKinnon, J Metti, JF Perera, TA Rand, V Sanchez-Fr, JM Shaxted, MM Stein, MA Streit, YC Tan, Y Zhang, E Zhao, J Venkataram, MC Stumpe, JA Borgia, A Masood, DVT Catenacci, JV Mathews, DB Gursel, JJ Wei, TH Welling, DM Simeone, KP White, AA Khan, C Igartua, AA Salahudeen
    Cell Reports, 2021;36(4):109429.

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Citations for SB 202190

The citations listed below are publications that use Tocris products. Selected citations for SB 202190 include:

36 Citations: Showing 1 - 10

  1. Evaluating Shigella flexneri Pathogenesis in the Human Enteroid Model.
    Authors: Ranganathan Et al.
    Infect Immun  2019;87
  2. P38 inhibition reverses TGFβ1 and TNFα-induced contraction in a model of proliferative vitreoretinopathy.
    Authors: Schiff Et al.
    Commun Biol  2019;2:162
  3. Improving Cell Survival in Injected Embryos Allows Primed Pluripotent Stem Cells to Generate Chimeric Cynomolgus Monkeys.
    Authors: Kang Et al.
    Cell Rep  2018;25:2563
  4. IL-17A causes depression-like symptoms via NFκB and p38MAPK signaling pathways in mice: Implications for psoriasis associated depression.
    Authors: Nadeem
    Cytokine  2017;97:14
  5. Type I and Type III IF.s Display Different Dependency on Mitogen-Activated Protein Kinases to Mount an Antiviral State in the Human Gut.
    Authors: Pervolaraki Et al.
    Front Immunol  2017;8:459
  6. TNFα induces tolerant production of CXC chemokines in colorectal cancer HCT116 cells via A20 inhibition of ERK signaling.
    Authors: Zhou
    Int Immunopharmacol  2017;54(296)
  7. p38 MAPK as an essential regulator of dorsal-ventral axis specification and skeletogenesis during sea urchin development: a re-evaluation.
    Authors: Molina Et al.
    Development  2017;144:2270
  8. Andrographolide induces Nrf2 and heme oxygenase 1 in astrocytes by activating p38 MAPK and ERK.
    Authors: Wong Et al.
    J Neuroinflammation  2016;13:251
  9. Tumour-derived SPARC drives vascular permeability and extravasation through endothelial VCAM1 signalling to promote metastasis.
    Authors: Tichet Et al.
    Nat Commun  2015;6:6993
  10. Matrix rigidity regulates the transition of tumor cells to a bone-destructive phenotype through integrin β3 and TGF-β receptor type II.
    Authors: Page Et al.
    Biomaterials  2015;64:33
  11. Excess salt exacerbates blood-brain barrier disruption via a p38/MAPK/SGK1-dependent pathway in permanent cerebral ischemia.
    Authors: Zhang Et al.
    PLoS One  2015;5:16548
  12. The role of Na+/K+-ATPase during chick skeletal myogenesis.
    Authors: Oliveira Et al.
    J Neurosci  2015;10:e0120940
  13. Modulation of radiation injury response in retinal endothelial cells by quinic acid derivative KZ-41 involves p38 MAPK.
    Authors: Toutounchian Et al.
    PLoS One  2014;9:e100210
  14. TGFβ-mediated suppression of CD248 in non-cancer cells via canonical Smad-dependent signaling pathways is uncoupled in cancer cells.
    Authors: Babu Et al.
    BMC Cancer  2014;14:113
  15. Sodium chloride drives autoimmune disease by the induction of pathogenic TH17 cells.
    Authors: Kleinewietfeld Et al.
    Sci Rep  2013;496:518
  16. 3,3'-diindolylmethane rapidly and selectively inhibits hepatocyte growth factor/c-Met signaling in breast cancer cells.
    Authors: Nicastro Et al.
    J Nutr Biochem  2013;24:1882
  17. Identification of repurposed small molecule drugs for chordoma therapy.
    Authors: Xia Et al.
    Cancer Biol Ther  2013;14:638
  18. Label-free integrative pharmacology on-target of opioid ligands at the opioid receptor family.
    Authors: Morse Et al.
    BMC Pharmacol Toxicol  2013;14:17
  19. Post-transcriptional regulation of placenta growth factor mRNA by hydrogen peroxide.
    Authors: Shaw and Lloyd
    Nature  2012;84:155
  20. Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis.
    Authors: Akhmetshina Et al.
    J Biol Chem  2012;3:735
  21. BlyS is up-regulated by hypoxia and promotes migration of human breast cancer cells.
    Authors: Zhu Et al.
    Am J Physiol Lung Cell Mol Physiol  2012;31:31
  22. A screen for regulators of survival of motor neuron protein levels.
    Authors: Makhortova Et al.
    Nat Chem Biol  2011;7:544
  23. Ligand-directed functional selectivity at the mu opioid receptor revealed by label-free integrative pharmacology on-target.
    Authors: Morse Et al.
    PLoS One  2011;6:e25643
  24. Transforming growth factor-β2 promotes Snail-mediated endothelial-mesenchymal transition through convergence of Smad-dependent and Smad-independent signalling.
    Authors: Medici Et al.
    J Exp Clin Cancer Res  2011;437:515
  25. Dermatophagoides pteronyssinus 2 regulates nerve growth factor release to induce airway inflammation via a reactive oxygen species-dependent pathway.
    Authors: Ye Et al.
    Am J Physiol Regul Integr Comp Physiol  2011;300:L216
  26. Dual specificity phosphatase 1 regulates human inducible nitric oxide synthase expression by p38 MAP kinase.
    Authors: Turpeinen Et al.
    J Neurosci  2011;2011:127587
  27. Bone morphogenic protein-4 impairs endothelial function through oxidative stress-dependent cyclooxygenase-2 upregulation: implications on hypertension.
    Authors: Wong Et al.
    Circ Res  2010;107:984
  28. Proteomic analysis uncovers novel actions of the neurosecretory protein VGF in nociceptive processing.
    Authors: Riedl Et al.
    Nat Commun  2009;29:13377
  29. PLZF is a regulator of homeostatic and cytokine-induced myeloid development.
    Authors: Doulatov Et al.
    Genes Dev  2009;23:2076
  30. Cingulin regulates claudin-2 expression and cell proliferation through the small GTPase RhoA.
    Authors: Guillemot and Citi
    Mol Biol Cell  2006;17:3569
  31. Temporally and spatially coordinated roles for Rho, Rac, Cdc42 and their effectors in growth cone guidance by a physiological electric field.
    Authors: Rajnicek Et al.
    J Cell Sci  2006;119:1723
  32. Oxygen-sensitive {δ}-opioid receptor-regulated survival and death signals: novel insights into neuronal preconditioning and protection.
    Authors: Ma Et al.
    Mediators Inflamm  2005;280:16208
  33. Intracellular pathways triggered by the selective FLT-1-agonist placental growth factor in vascular smooth muscle cells exposed to hypoxia.
    Authors: Bellik Et al.
    Br J Pharmacol  2005;146:568
  34. Extracellular signal-regulated protein kinase activation is required for metabotropic glutamate receptor-dependent long-term depression in hippocampal area CA1.
    Authors: Gallagher Et al.
    Biochem J  2004;24:4859
  35. Calcineurin-independent inhibition of mitochondrial Ca2+ uptake by cyclosporin A.
    Authors: Montero Et al.
    Br J Pharmacol  2004;141:263
  36. IL-13-induced changes in the goblet cell density of human bronchial epithelial cell cultures: MAP kinase and phosphatidylinositol 3-kinase regulation.
    Authors: Atherton Et al.
    Am J Physiol Lung Cell Mol Physiol  2003;285:L730

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Reviews for SB 202190

Average Rating: 3.5 (Based on 2 Reviews)

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Easy to store and use
By Anonymous on 02/07/2019
Species: Human

I used this to test the potency of this to kill of COLO 205 cells with the addition of TNF in a dose dependent manner.


Good inhibitor for cell studies
By Samantha Scarneo on 12/26/2018

I compared this inhibitor to a TAK1 inhibitor to compared effects on cell death.


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