产品说明
一般描述
Reduces epirubicin-induced cell injury and caspase-3/7 activity. A highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 kinase (IC50 = 34 nM in vitro, 600 nM in cells). Also known as reactivating kinase (RK) and CSBP (cytokine synthesis anti-inflammatory drug binding protein). Does not significantly inhibit JNK or p42 MAP kinase even at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC50 = 50-100 nM). SB 203580 has also been shown to be an effective inhibitor of inflammatory cytokine production in vivo in both mice and rats.
Reduces epirubicin-induced cell injury and caspase-3/7 activity. A highly specific, potent, cell-permeable, selective, reversible, and ATP-competitive inhibitor of p38 MAP kinase (IC50 = 34 nM in vitro, 600 nM in cells). Does not significantly inhibit the JNK and p42 MAP kinase at 100 µM. Inhibits IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1 (IC50 = 50-100 nM). Inhibits bone morphogenetic protein-2-induced neurite outgrowth in PC12 cells. Also inhibits platelet aggregation caused by collagen (IC50 = 0.2-1.0 µM) or the thromboxane analog U-46619 (Cat. No. 538944). A 1 mg/ml solution of SB 203580 (Cat. No. 559398) in anhydrous DMSO is also available.
包装
1 mg in Plastic ampoule
5, 10 mg in Glass bottle
生化/生理作用
Cell permeable: yes
Target IC50: 34 nM against p38 MAP kinase in vitro, 600 nM in cells; 50-100 nM against IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1; 0.2-1.0 µM against platelet aggregation caused by collagen
Product competes with ATP.
Reversible: yes
警告
Toxicity: Irritant (B)
其他说明
Yamada. T., et al. 2012. Free Radic. Biol. Med. (In press)
Powell, D.J., et al. 2003. Mol. Cell Biol.23, 7794.
Davies, S.P., et al. 2000. Biochem. J.351, 95.
Iwasaki, S., et al. 1999. J. Biol. Chem.274, 26503.
Gallagher, T.F., et al. 1997. Bioorg. Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997. Biochem. 36, 10422.
Hazzalin, C.A., et al. 1996. Curr. Biol.6, 1028.
Kramer, R.M., et al. 1996. J. Biol. Chem.271, 27723.
Saklatvala, J., et al. 1996. J. Biol. Chem. 271, 6586.
Cuenda, A., et al. 1995. FEBS Lett.364, 229.
Gallagher, T.F., et al. 1995. Bioorg. Med. Chem. Lett. 5, 1171.
Lee, J.C., et al. 1994. Nature 372, 739.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C21H16FN3OS |
分子量 | 377.43 |
MDL编号 | MFCD00922198 |
产品性质
质量水平 | 100 |
测定 | ≥98% (HPLC) |
形式 | film (Thin) |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
溶解性 | DMSO: 30 mg/mL |
运输 | ambient |
储存温度 | −20℃ |
InChI | 1S/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) |
InChI key | CDMGBJANTYXAIV-UHFFFAOYSA-N |
安全信息
象形图 | |
警示用语: | Danger |
危险声明 | H302 - H318 |
预防措施声明 | P264 - P270 - P280 - P301 + P312 - P305 + P351 + P338 - P501 |
危险分类 | Acute Tox. 4 Oral - Eye Dam. 1 |
储存分类代码 | 13 - Non Combustible Solids |
WGK | WGK 3 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |
Sigma-Aldrich