559389
SB 203580
≥98% (HPLC), film (Thin), p38 MAP kinase inhibitor, Calbiochem®
别名:
SB 203580, 4-(4-氟苯基)-2-(4-甲基亚磺酰基苯基)-5-(4-吡啶基)1H-咪唑，p38 MAP激酶抑制剂XVI
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关于此项目
经验公式（希尔记法）:
C21H16FN3OS
化学文摘社编号:
分子量:
377.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
film (Thin)
Storage condition:
OK to freeze, protect from light
产品名称
SB 203580, SB 203580, CAS 152121-47-6, is 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).
Quality Segment
assay
≥98% (HPLC)
form
film (Thin)
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
solubility
DMSO: 30 mg/mL
shipped in
ambient
storage temp.
−20°C
SMILES string
Fc1ccc(cc1)c2nc([nH]c2c4ccncc4)c3ccc(cc3)[S+]([O-])C
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
General description
降低表阿霉素诱导的细胞损伤和caspase-3/7活性。p38 MAP激酶的一种高度特异性、有效性、细胞渗透性、选择性、可逆性和ATP竞争性抑制剂（体外IC50=34 nM，细胞内为600 nM）。在100 µM时不会显著抑制JNK和p42 MAP激酶。抑制LPS刺激的人单核细胞和人单核细胞系THP-1产生IL-1和TNFα（IC50=50-100 nM）。抑制骨形态发生蛋白-2诱导的PC12细胞突起生长。还可抑制由胶原蛋白（IC50 = 0.2-1.0 µM）或血栓素类似物U-46619（目录号538944）引起的血小板聚集。也可提供SB 203580（目录号559398）在无水DMSO中的1 mg/ml溶液。
Biochem/physiol Actions
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：在体外对p38 MAP激酶为34 nM，在细胞中为600 nM；对LPS刺激的人单核细胞和人单核细胞系TNF-α产生的IL-1和TNF-为50-100 nM；对胶原蛋白引起的血小板聚集为0.2-1.0 µM
Other Notes
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.
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
毒性：刺激性（B）
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signalword
Warning
hcodes
Hazard Classifications
Acute Tox. 4 Oral
flash_point_f
Not applicable
flash_point_c
Not applicable
存储类别
11 - Combustible Solids