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ALX-270-179 Revised 30-Mar-07
SB203580
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SYNONYMS 4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY MAPK Pathway Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-179-M001   1 mg 60.00 USD Add To Cart
ALX-270-179-M005   5 mg 250.00 USD Add To Cart
ALX-270-179-M050   50 mg 1'200.00 USD Add To Cart
Product Specification
FORMULA: C21H16N3FOS
MW: 377.4
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Cell permeable, specific inhibitor of p38 (SAPK2a).  Can inhibit the key cell cycle event of retinoblastoma protein phosphorylation in interleukin-2-stimulated T cells. Studies on the proximal regulator of this event, the PI(3)K (phosphoinositide 3-kinase)/Akt (protein kinase B; PKB) pathway, showed that SB203580 blocks the phosphorylation and activation of Akt by inhibiting the Akt kinase, phosphoinositide-dependent protein kinase 1 (PDK1). The concentrations of SB203580 required to block Akt phosphorylation (IC50= 3-5µM) are only approximately 10-fold higher than those required to inhibit p38 MAP kinase (IC50=0.3-0.5µM). These data define a new activity for this drug and suggest that extreme caution should be used when interpreting data when SB203580 has been used at concentrations above 1-2µM [1].
Product Specific Literature References
A protein kinase involved in the regulation of inflammatory cytokine biosynthesis: J.C. Lee, et al.; Nature 372, 739 (1994) Abstract
SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1: A. Cuenda, et al.; FEBS Lett. 364, 229 (1995) Abstract
Characterization of the structure and function of a new mitogen-activated protein kinase (p38beta): Y. Jiang, et al.; J. Biol. Chem. 271, 17920 (1996) Abstract; Full Text
The primary structure of p38 gamma: a new member of p38 group of MAP kinases: Z. Li, et al.; BBRC 228, 334 (1996) Abstract
Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase: T.F. Gallagher, et al.; Bioorg. Med. Chem. 5, 49 (1997) Abstract
A p38 MAP kinase inhibitor SB203580 inhibits CD28-dependent T cell proliferation and IL-2 production: S.G. Ward, et al.; Biochem. Soc. Trans. 25, 304S (1997) Abstract
p38 mitogen activated protein kinase regulates endothelial VCAM-1 expression at the post-transcriptional level: A. Pietersma, et al.; BBRC 230, 44 (1997) Abstract
Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. SB 203580 also inhibits thromboxane synthase: A.G. Börsch-Haubold, et al.; J. Biol. Chem. 273, 28766 (1998) Abstract; Full Text
Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino-acid substitution: P.A. Eyers, et al.; Chem. Biol. 5, 321 (1998) Abstract
Low density lipoprotein phosphorylates the focal adhesion-associated kinase p125(FAK) in human platelets independent of integrin alphaIIb beta3: C.M. Hackeng, et al.; J. Biol. Chem. 274, 384 (1999) Abstract; Full Text
Effect of SB 203580 on the activity of c-Raf in vitro and in vivo: C.A. Hall-Jackson, et al.; Oncogene 18, 2047 (1999) Abstract
Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor, SB203580: A. Kalmes, et al.; FEBS Lett. 444, 71 (1999) Abstract
SB 203580, an inhibitor of p38 mitogen-activated protein kinase, enhances constitutive apoptosis of cytokine-deprived human eosinophils: H. Kankaanranta, et al.; J. Pharmacol. Exp. Ther. 290, 621 (1999) Abstract
[1] 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 mit: F.V. Lali, et al.; J. Biol. Chem. 275, 7395 (2000) Abstract; Full Text
 
 

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