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Submit ReviewSB 203580 hydrochloride
Description: Selective inhibitor of p38 MAPK; water-soluble
Chemical Name: 4-[5-(4-Fluorophenyl)-2-[4-(methylsulphonyl)phenyl]-1H-imidazol-4-yl]pyridine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for SB 203580 hydrochloride
SB 203580 hydrochloride is a water-soluble salt of SB 203580 (Cat. No. 1202). Selective inhibitor of p38 mitogen-activated protein kinase (IC50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38β2 respectively). Displays 100-500-fold selectivity over LCK, GSK3β and PKBα. Shown to inhibit interleukin-2-induced T cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase.
Technical Data for SB 203580 hydrochloride
| M. Wt | 413.89 |
| Formula | C21H16FN3OS.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 869185-85-3 |
| PubChem ID | 16760644 |
| InChI Key | WOSGGXINSLMASH-UHFFFAOYSA-N |
| Smiles | Cl.CS(=O)C1=CC=C(C=C1)C1=NC(=C(N1)C1=CC=NC=C1)C1=CC=C(F)C=C1 |
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.
Solubility Data for SB 203580 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 10.35 | 25 |
Preparing Stock Solutions for SB 203580 hydrochloride
The following data is based on the product molecular weight 413.89. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.25 mM | 9.66 mL | 48.32 mL | 96.64 mL |
| 1.25 mM | 1.93 mL | 9.66 mL | 19.33 mL |
| 2.5 mM | 0.97 mL | 4.83 mL | 9.66 mL |
| 12.5 mM | 0.19 mL | 0.97 mL | 1.93 mL |
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Product Datasheets for SB 203580 hydrochloride
References for SB 203580 hydrochloride
References are publications that support the biological activity of the product.
Borsch-Haubold et al (1998) Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. J.Biol.Chem. 273 28766 PMID: 9786874
Cuenda et al (1995) SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1. FEBS Lett. 364 229 PMID: 7750577
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Saklatvala et al (1996) Role for p38 mitogen-activated protein kinase in platelet aggregation caused by collagen on a thromboxane analogue. J.Biol.Chem. 271 6586 PMID: 8636072
If you know of a relevant reference for SB 203580 hydrochloride, please let us know.
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Keywords: SB 203580 hydrochloride, SB 203580 hydrochloride supplier, Selective, inhibitors, inhibits, p38, MAPK, water-soluble, Signaling, Signalling, Mitogen-Activated, Protein, Kinases, SB203580, hydrochloride, GlaxoSmithKline, GSK, 1402, Tocris Bioscience
11 Citations for SB 203580 hydrochloride
Citations are publications that use Tocris products. Selected citations for SB 203580 hydrochloride include:
Yang et al (2017) Establishment of mouse expanded potential stem cells. Nature 550 393 PMID: 29019987
Edén et al (2015) Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated Ins secretion from human pancreatic islets. Diabetologia 58 2563 PMID: 26271343
Mans et al (2014) An acetylcholinesterase inhibitor, eserine, induces long-term depression at CA3-CA1 synapses in the hippocampus of adult rats. J Neurophysiol 112 2388 PMID: 25143547
Nguyen et al (2014) Transient receptor potential vanilloid type 1 channel may modulate opioid reward. Neuropsychopharmacology 39 2414 PMID: 24732880
Zhang et al (2018) Elevated sodium chloride drives type I IF. signaling in macrophages and increases antiviral resistance. J Biol Chem 293 1030 PMID: 29203528
Silpanisong et al (2017) Chronic hypoxia alters fetal cerebrovascular responses to endothelin-1. Am J Physiol Cell Physiol 313 C207 PMID: 28566491
Li et al (2019) Generation of blastocyst-like structures from mouse embryonic and adult cell cultures. Cell 179 687 PMID: 31626770
Williams et al (2012) Inhibition of stathmin1 accelerates the metastatic process. Cancer Res 72 5407 PMID: 22915755
Lukjanenko et al (2016) Loss of fibronectin from the aged stem cell niche affects the regenerative capacity of skeletal muscle in mice. Nat Med 22 897 PMID: 27376579
Engel et al (2006) FGF1/p38 MAP kinase inhibitor therapy induces cardiomyocyte mitosis, reduces scarring, and rescues function after myocardial infarction. Proc Natl Acad Sci U S A 103 15546 PMID: 17032753
Schlemper et al (2005) Mechanisms underlying the relaxation response induced by bradykinin in the epithelium-intact guinea-pig trachea in vitro. Br J Pharmacol 145 740 PMID: 15852038
Do you know of a great paper that uses SB 203580 hydrochloride from Tocris? Please let us know.
Reviews for SB 203580 hydrochloride
Average Rating: 4.8 (Based on 4 Reviews.)
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Generation of EPS-blastoids.
By
Anonymous on 02/27/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: EPS
10uM
p38 MAPK pathway does not influence the LPA induced AMPK phosphorylation in microglia cells..
By
lisha joshi on 06/18/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: BV2 microglia cells
We investigate the effect of LPA on microglia metabolic states. Trying to unravel possible pathways that maybe involved in this process, we used LPAR inhibitors and downstream inhibitors of MAPKs pathway. SB 203580 was used at a concentration of 10µM yet couldn't inhibit the expression of pAMPK. However the inhibitor was well tolerated by the cells.
SB 203580 ameliorates LPA-induced COX-2 expression.
By
Anonymous on 12/13/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Osteosarcoma
MG-63 cells were pre-incubated with 10 µM SB 203580 for 30 min followed by treatment with 10 µM LPA for 3 h to follow COX-2 expression using Western blot. SB 203580 inhibited COX-2 induction by LPA.
SB 203580 blunts 15d-PGJ2 induced pp38 expression.
By
Chintan Koyani on 10/13/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: HL-1 cardiomyocytes
HL-1 cells were incubated with p38 MAPK inhibitor (10 µM SB203580, 25 µMPD169316) or p42/44 MAPK kinase inhibitor (25 µM PD98059) for 30 min prior to 15dPGJ2 treatment (15 µM, 1 h). Immunoreactive bands for pp38 and pp42/44 MAPK expressions were followed by Western blot. SB203580 completely inhibited 15d-PGJ2 induced p38 phosphorylation (shown in Image).
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for SB 203580 hydrochloride
