152121-47-6 Usage
Description
SB 203580, also known as a pyridinyl imidazole, is a potent and selective inhibitor of p38 MAP kinase. It is a white to off-white solid and is a member of the class of imidazoles with specific substituents. SB 203580 is highly specific, cell-permeable, and ATP-competitive, with an IC50 range of 0.3-0.5 μM for p38 MAPK inhibition and 3-5 μM for blocking PKB phosphorylation. It does not significantly inhibit JNK or p42 MAP kinase even at 100 μM.
Uses
1. Used in Pharmaceutical Applications:
SB 203580 is used as a specific inhibitor of p38 MAP kinase for studying the role of this enzyme in various cellular processes and diseases. It helps in understanding the signaling pathways and potential therapeutic targets for conditions involving p38 MAP kinase activation.
2. Used in Inflammatory Research:
SB 203580 is used as an inhibitor of inflammatory cytokine production in animal models of arthritis, bone resorption, endotoxin shock, and immune function. It has an IC50 of 15-25 mg/kg in mice and rats, making it a valuable tool for studying the inflammatory response and potential anti-inflammatory treatments.
3. Used in Cell Biology Research:
SB 203580 is used to inhibit MAPK signaling in various cell types, such as MDCK cells, mouse cortical neurons, and human hepatocellular carcinoma cell lines. This helps researchers investigate the role of MAPK signaling in cell membrane hypertonicity, potassium depletion, and other cellular processes.
4. Used in Anticancer Research:
SB 203580 is used to reduce epirubicin-induced cell injury and caspase-3/7 activity, providing insights into the potential use of p38 MAP kinase inhibitors in cancer therapy.
5. Used in Drug Delivery Systems:
Although not explicitly mentioned in the provided materials, SB 203580's properties as a potent and selective inhibitor of p38 MAP kinase suggest its potential use in the development of drug delivery systems targeting specific cellular pathways involved in various diseases, including cancer and inflammatory conditions.
Biological Activity
Water-soluble salt of SB 203580 (4-[5-(4-Fluorophenyl)-2-[4-(methylsulfonyl)phenyl]-1H-imidazol-4-yl]pyridine ). Selective inhibitor of p38 mitogen-activated protein kinase (IC 50 values are 50 and 500 nM for SAPK2a/p38 and SAPK2b/p38 β 2 respectively). Displays 100-500-fold selectivity over LCK, GSK3 β and PKB α . Shown to inhibit interleukin-2-induced T-cell proliferation, cyclooxygenase-1 and -2, and thromboxane synthase.
Biochem/physiol Actions
SB 203580 is a pyridinyl imidazole that suppresses the activation of MAPKAP kinase-2 and inhibits the phosphorylation of heat shock protein (HSP) 27 in response to IL-1, cellular stresses and bacterial endotoxin in vivo. It does not inhibit JNK or p42 MAP kinase and therefore, is useful for studying the physiological roles and targets of p38 MAPK and MAPKAP kinase-2. It has been shown to induce the activation of the serine/threonine kinase Raf-1 and has been reported to inhibit cytokine production.
References
1) 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
2) Davies et al. (2000), Specificity and mechanism of action of some commonly used protein kinase inhibitors; Biochem. J., 351 95
3) Badger et al. (1996), Pharmacological profile of SB 203580, a selective inhibitor of cytokine suppressive binding protein/p38 kinase, in animal models of arthritis, bone resorption, endotoxin shock and immune function; Pharmacol. Exp. Ther. 279 1453
Check Digit Verification of cas no
The CAS Registry Mumber 152121-47-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,2,1,2 and 1 respectively; the second part has 2 digits, 4 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 152121-47:
(8*1)+(7*5)+(6*2)+(5*1)+(4*2)+(3*1)+(2*4)+(1*7)=86
86 % 10 = 6
So 152121-47-6 is a valid CAS Registry Number.
InChI:InChI=1/C21H16FN3OS/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15/h2-13H,1H3,(H,24,25)
152121-47-6Relevant articles and documents
Treatment for CNS injuries
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, (2008/06/13)
The present invention is directed to the use of 2,4,5-trisubstituted imidazole compounds and compositions in the treatment of CNS injuries to the brain.
Pyrimidinyl imidazoles
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, (2008/06/13)
Novel 2,4,5-triaryl imidazole compounds and compositions for use in therapy.
Imidazole derivatives and their use as cytokine inhibitors
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, (2008/06/13)
As cytokine inhibitors 2,4,5-triarylimidazole compounds and compositions for use as cytokine inhibitors.
