Replaces Prod. #: ALX-270-179
Cell permeable, specific inhibitor of p38 (SAPK2a). Inhibits p38 MAPK stimulation of MAPKAPK2 (IC50=70nM). 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. Non-specific effects include inhibition of COX-1 and -2. Enhances clonal growth of skin epithelial progenitor cells and stimulates neural stem cell proliferation.
Product Details
| Alternative Name: | 4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)1H-imidazole |
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| Formula: | C21H16N3FOS |
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| MW: | 377.4 |
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| CAS: | 152121-47-6 |
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| Purity: | ≥97% (HPLC) |
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| Appearance: | White to off-white powder. |
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| Solubility: | Soluble in DMSO (50mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Technical Info/Product Notes: | Replacement for ADI-HPK-110 |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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Mitigation of ER-stress and inflammation by chemokine (CC motif) ligand 21 during early pregnancy: H. Bae, et al.; Dev. Comp. Immunol.
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Chrysin attenuates progression of ovarian cancer cells by regulating signaling cascades and mitochondrial dysfunction: W. Lim, et al.; J. Cell. Physiol.
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Sideroxylin (Callistemon lanceolatus) suppressed cell proliferation and increased apoptosis in ovarian cancer cells accompanied by mitochondrialdysfunction, the generation of reactive oxygen species, and an increase of lipid peroxidation: S. Park, et al.; J. Cell. Physiol.
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Acinar-to-Ductal Metaplasia Induced by Transforming Growth Factor Beta Facilitates KRASG12D-driven Pancreatic Tumorigenesis: N. Chuvin, et al.; Cell. Mol. Gastroenterol. Hepatol.
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Balance between IL-3 and type Iinterferons and their interrelationship with FasL dictates lifespan and effector functions of human basophils: B.R. Hagmann, et al.; Clin. Exp. Allergy
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Full Text
Simvastatin induces differentiation of rabbit articular chondrocytes via the ERK-1/2 and p38 kinase pathways: Y. Han, et al.; Exp. Cell Res.
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Full Text
Amphiregulin may be a new biomarker of classically activated macrophages: C. Meng, et al.; Biochem. Biophys. Res. Commun.
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Areca nut exposure increases secretion of tumor‐promoting cytokines in gingival fibroblasts that trigger DNA damage in oral keratinocytes: R.P. Illeperuma, et al.; Int. J. Cancer
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Dibenzoylmethane Exerts Metabolic Activity through Regulation of AMP-Activated Protein Kinase (AMPK)-Mediated Glucose Uptake and Adipogenesis Pathways: N. Kim, et al.; PLoS One
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Glycated albumin triggers fibrosis and apoptosis via an NADPH oxidase/Nox4-MAPK pathway-dependent mechanism in renal proximal tubular cells: W. Qi, et al.; Mol. Cell. Endocrinol.
405, 74 (2015),
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Phloretin ameliorates chemokines and ICAM-1 expression via blocking of the NF-κB pathway in the TNF-α-induced HaCaT human keratinocytes: W.C. Huang, et al.; Int. Immunopharmacol.
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47, 660 (2012),
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Full Text
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.
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Full Text
Effect of SB 203580 on the activity of c-Raf in vitro and in vivo: C.A. Hall-Jackson, et al.; Oncogene
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Full Text
Raf-1 is activated by the p38 mitogen-activated protein kinase inhibitor, SB203580: A. Kalmes, et al.; FEBS Lett.
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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.
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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.
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Full Text
The p38-MAPK inhibitor, SB203580, inhibits cardiac stress-activated protein kinases/c-Jun N-terminal kinases (SAPKs/JNKs): A. Clerk & P.H. Sugden; FEBS Lett.
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Full Text
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