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SB203580 | p38 MAPK inhibitor

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Price:
$89.00
Catalog #:
C7320-5
Quantity:


Product Description

SB203580 is a pyridinylimidazole-based inhibitor of p38-MAPK at an IC50 of 0.3-0.5 uM. [1] It also inhibits PKB phosphorylation at an IC50 of 3-5 uM and blocks the key cell cycle event of retinoblastoma protein phosphorylation in IL-2-stimulated T-cells. SB203580 was found to inhibit the activation of p70S6K, but at a location downstream of PI3K. [1]

Independent studies indicate at concentrations of 10 uM, SB203580 activates phosphorylation of ERK1/2 and JNK, which in turn may activate gene transcription regulated by NF-kB. [2] Similarly, SB203580 was shown to stimulate the phosphorylation and activation of cPLA2, CAMKIIa and arachidonic acid release. [3]

In an L1210 mouse leukemic cell line resistant to vincristine, SB203580 is believed to play a role in the reversal of Pgp-mediated multidrug resistance. [4]


Technical information:

Chemical Formula:   C21H16FN3OS
CAS #:   152121-47-6
Molecular Weight:   377.43
Purity:   >98%
Appearance:   White
Chemical Name:   4-(4-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine
Solubility:   Up to 100 mM in DMSO
Synonyms:   SB-203580, SB 203580, SB203580

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Lali et al., The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J. Biol. Chem. 2000, 275(10), 7395-7402. Pubmed ID: 10702313
2. Birkenkamp et al., The p38 MAP kinase inhibitor SB203580 enhances nuclear factor-kappa B transcriptional activity by a non-specific effect upon the ERK pathway. Br. J. Pharmacol. 2000, 131, 99-107. Pubmed ID: 10960075
3. Fatima et al., Cytosolic phospholipase A2 activation by the p38 kinase inhibitor SB203580 in rabbit aortic smooth muscle cells. J. Pharmacol. Exp. Ther. 2001, 298(1), 331-338. Pubmed ID: 11408559
4. Barancik et al., SB203580, a specific inhibitor of p38-MAPK pathway, is a new reversal agent of P-glycoprotein-mediated multidrug resistance. Eur. J. Pharmaceut. Sci. 2001, 14, 29-36. Pubmed ID: 10960075

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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