product name
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).
质量水平
检测方案
≥98% (HPLC)
形式
film (Thin)
制造商/商品名称
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°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
一般描述
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。
降低表阿霉素诱导的细胞损伤和caspase-3/7活性。p38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）。也称为再激活激酶（RK）和CSBP（细胞因子合成抗炎药物结合蛋白）。即使在100 µM时也不会显著抑制JNK或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）。SB203580也被证明是小鼠和大鼠体内炎症细胞因子产生的有效抑制剂。
生化/生理作用
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
警告
毒性：刺激性（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.
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
警示用语：
Warning
危险声明
危险分类
Acute Tox. 4 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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