SB 203580 hydrochloride

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Cat.No. 1402 - SB 203580 hydrochloride | C21H16FN3OS.HCl | CAS No. 869185-85-3
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)
Datasheet
Citations (11)
Reviews (4)
Literature (4)
Pathways (1)

Biological Activity

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.

Licensing Information

Sold with the permission of GlaxoSmithKline

Technical Data

M. Wt 413.89
Formula C21H16FN3OS.HCl
Storage Desiccate 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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 10.35 25 with gentle warming

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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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View all p38 MAPK Inhibitors

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:

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

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

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

PMID: 31626770
review image

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.

review image

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.

review image

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).

review image

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

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Kinases Product Listing

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MAPK Signaling

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

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.