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| | SB242235 Basic information |
| Product Name: | SB242235 | | Synonyms: | SB-242235; SB242235;CS-668;SB242235;4-[4-(4-Fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxypyrimidine;4-(4-(4-Fluorophenyl)-1-(piperidin-4-yl)-1H-iMidazol-5-yl)-2-MethoxypyriMidine;SB242235 ≥95%;Pyrimidine, 4-[4-(4-fluorophenyl)-1-(4-piperidinyl)-1H-imidazol-5-yl]-2-methoxy-;inhibit,SB 242235,Autophagy,Inhibitor,p38 MAPK | | CAS: | 193746-75-7 | | MF: | C19H20FN5O | | MW: | 353.39 | | EINECS: | | | Product Categories: | | | Mol File: | 193746-75-7.mol |  |
| | SB242235 Chemical Properties |
| Boiling point | 568.4±60.0 °C(Predicted) | | density | 1.34 | | storage temp. | 2-8°C(protect from light) | | solubility | DMF: 25 mg/ml; DMSO: 20 mg/ml; Ethanol: 30 mg/ml | | form | Powder | | pka | 9.91±0.10(Predicted) | | color | White to off-white |
| | SB242235 Usage And Synthesis |
| Uses | SB-242235 is a potent and selective p38 MAP kinase inhibitor, with an IC50 of 1.0 μM in primary human chondrocytes[1]. | | Biological Activity | SB-242235 is a potent and selective p38 MAP kinase inhibitor with IC50 of 1.0 μM in human chondrocytes. | | in vitro | SB 242235 (0-10 μM) dose-dependently inhibits the activation of MAPKAP K2 with an IC 50 of 1.0 μM in human chondrocytes stimulated with IL-1β.
SB 242235 inhibits intracellular p38 activity, MAPKAP K2 was then isolated from these cells and assayed using HSP27 as a substrate.
Western Blot Analysis | Cell Line: | Human chondrocytes | | Concentration: | 0 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM | | Incubation Time: | < td class="col2"> 15 minutes | Result: | Dose-dependently inhibited the activation of MAPKAP K2 with an IC 50 of 1.0 μM. | | | in vivo | SB242235 (100 mg/kg; p.o.) abolishes MAP-KAPK-2 activity and HSP27 phosphorylation[2].
SB242235 inhibits expression of the pro-inflammatory cytokines interleukin (IL)-6 and KC (murine IL-8) and COX-2[2].
SB-242235 is demonstrated non-linear elimination kinetics that manifested as a decrease in clearance with increasing dose and apparent oral bioavailability > 100% at high oral doses in rat and monkey[3].
| Animal Model: | Female SKH-1 hairless mice (4–6 weeks)[2] | | Dosage: | 100 mg/kg | | Administration: | Oral administered, 30 minutes prior to ultraviolet B (UVB) irradiation | | Result: | Abolished MAP-KAPK-2 activity and heat shock protein 27 (HSP27) phosphorylation. |
| | target | IC50: 1.0 μM (p38 MAPK, primary human chondrocytes) | | References | [1] Badger, A.M., et al., Differential effects of SB 242235, a selective p38 mitogen-activated protein kinase inhibitor, on IL-1 treated bovine and human cartilage/chondrocyte cultures. Osteoarthritis Cartilage, 2000. 8(6): p. 434-43. DOI:10.1053/joca.1999.0319
[2] Kim AL , et al. Role of p38 MAPK in UVB-induced inflammatory responses in the skin of SKH-1 hairless mice. J Invest Dermatol. 2005 Jun;124(6):1318-25. DOI:10.1111/j.0022-202X.2005.23747.x
[3] Ward, K.W., et al., SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics. Xenobiotica, 2002. 32(3): p. 221-33. DOI:10.1080/00498250110100720 |
| | SB242235 Preparation Products And Raw materials |
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