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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:
152121-47-6
分子量:
377.43
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD00922198
Assay:
≥98% (HPLC)
Form:
film (Thin)
Quality level:
100
Storage condition:
OK to freeze, protect from light
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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 Level

100

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性：刺激性（B）

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pictograms

Exclamation mark
GHS07

signalword

Warning

hcodes

H302

Hazard Classifications

Acute Tox. 4 Oral

flash_point_f

Not applicable

flash_point_c

Not applicable

存储类别

11 - Combustible Solids

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货号GTIN
559389-10MG04055977192490
559389-1MG07790788051532
559389-5MG04055977192537