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General description
A highly specific, cell-permeable 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.
Biochem/physiol Actions
Cell permeable: yes
Product competes with ATP.
Reversible: yes
Target IC50: 34 nM in vitro, 600 nM in cells against p38 MAPK; 50-100 nM Inhibiting IL-1 and TNF-α production from LPS-stimulated human monocytes and the human monocyte cell line THP-1; 0.2-1.0 µM inhibiting platelet aggregation by collagen
Packaging
Packaged under inert gas
Physical form
A 1 mg/ml solution of SB 203580 (Cat. No. 559389) in anhydrous DMSO.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Irritant (B)
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | liquid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| shipped in | wet ice |
| storage temp. | −20°C |
| 长度(mm) | |
| 宽度(mm) | |
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| 重量(kg) |
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¥ 1259.40
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¥ 9207.92
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¥ 3152.47
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¥ 2883.61
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无菌，PETG 方形有刻度培养基瓶，带盖，聚对苯二酸乙二醇酯共聚物，天然高密度聚乙烯盖，500毫升容量，每箱40，40/箱，342020-0500，Nalgene，Thermofisher，赛默飞世尔¥ 3684.34
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