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SB 202190 is a potent p38 MAPK inhibitor. SB 202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38α and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2 respectively). SB 202190 by itself was sufficient to induce cell death, with typical apoptotic features such as nucleus condensation and intranucleosomal DNA fragmentation. SB 202190 stimulated the activity of CPP32-like caspases, and its apoptotic effect was completely blocked by the expression of bcl-2. When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs). Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.
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Dexmedetomidine preconditioning alleviates H2O2-induced oxidative stress and apoptosis in human umbilical vein endothelial cells via p38MAPK signaling pathway
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5-Fluorouracil enhances the chemosensitivity of gastric cancer to TRAIL via inhibition of the MAPK pathway
SB 202190 purchased from AbMole
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Source | Br J Pharmacol (2006). Figure 1. SB 202190 |
| Method | FLIPR | |
| Cell Lines | HEK293 cells | |
| Concentrations | 10 μM | |
| Incubation Time | 18 h | |
| Results | The MAPK inhibitor, SB-202190, also antagonized human P2X7 receptor-mediated responses but was generally less potent than SB-203580 with pIC50 values varying from 6.2 to 4.8, depending on BzATP concentration. |
| Molecular Weight | 331.34 |
| Formula | C20H14FN3O |
| CAS Number | 152121-30-7 |
| Solubility (25°C) | DMSO 36 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related p38 MAPK Products |
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SSK1 is a senescence-specific killing compound and is a precursor for β-galactosidase, which can reduce the inflammatory response. SSK1 can activate the phosphorylation of p38 MAPK and MKK3/MKK6 in senescent cells, promote mitochondrial DNA damage and selectively killed senescent cells. |
| p38 MAP Kinase Inhibitor III
p38 MAP Kinase Inhibitor III is a p38 MAPK inhibitor with an IC50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with IC50 values of 0.37 μM and 0.044 μM, respectively. |
| (R)-STU104
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| SB 706504
SB 706504 is a potent p38 MAPK inhibitor that inhibits Lipopolysaccharides-stimulated inflammatory gene expression in macrophages in chronic obstructive pulmonary disease (COPD). |
| RWJ-67657
RWJ-67657 (JNJ 3026582) is an orally active and selective p38α and p38β MAPK inhibitor with IC50s of 1 and 11 μM, respectively. |
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