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质量水平
检测方案
≥98% (HPLC)
形式
solid
效能
16 nM Ki
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale yellow
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
−20°C
InChI
1S/C20H14FN3O/c21-16-5-1-13(2-6-16)18-19(14-9-11-22-12-10-14)24-20(23-18)15-3-7-17(25)8-4-15/h1-12,23-24H
InChI key
NJNKPVPFGLGHPA-UHFFFAOYSA-N
一般描述
一种有效的、可逆的、竞争性的、细胞渗透性p38 MAP激酶抑制剂。抑制髓鞘碱性蛋白（MBP）的p38磷酸化，而不影响ERK或JNK MAP激酶亚群的活性。还抑制p38β的激酶活性（Ki=16 nM；IC50 = 350 nM）和激活转录因子2的p38磷酸化（ATF-2；IC50 = 280 nM）。阻断LPS诱导的TNF-α和白细胞介素生物合成已报道在Hep52细胞中诱导LDL受体表达。
一种有效的、可逆的、竞争性的、细胞渗透性p38 MAP激酶抑制剂。抑制髓鞘碱性蛋白（MBP）的p38磷酸化，而不影响ERK或JNK MAP激酶亚群的活性。还抑制p38β的激酶活性（Ki=16 nM；IC50=350 nM）和激活转录因子2的p38磷酸化（ATF-2；IC50=280 nM）。阻断LPS诱导的TNF-α和白细胞介素生物合成已报道在Hep52细胞中诱导LDL受体表达。也可提供SB 202190（目录号559397）在无水DMSO中的1 mg/ml溶液。
生化/生理作用
主要靶标
p38β
p38β
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：针对p38β的激酶活性，为350 nM；针对激活转录因子2(ATF-2)的p38磷酸化，为280 nM
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。贮备溶液在-20°C下可稳定保存至多6个月。
其他说明
Davies, S.P., et al. 2000.Biochem.J.351, 95.
Ajizian, S.J., et al. 1999.J. Infect.Dis.179, 939.
Singh, R.P., et al. 1999.J. Biol. Chem.274, 19593.
Wang, S.W., et al. 1999.Inflamm.Res.48, 533.
Gallagher, T.F., et al. 1997.Bioorg.Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997.Biochem.36, 10422.
Jiang, Y., et al. 1996.J. Biol. Chem. 271, 17920.
Kramer, R.M., et al. 1996.J. Biol. Chem.271, 27723.
Li, Z., et al. 1996.Biochem.Biophys.Res.Commun.228, 334.
Lee, J.C., et al. 1994.Nature 372, 739.
Ajizian, S.J., et al. 1999.J. Infect.Dis.179, 939.
Singh, R.P., et al. 1999.J. Biol. Chem.274, 19593.
Wang, S.W., et al. 1999.Inflamm.Res.48, 533.
Gallagher, T.F., et al. 1997.Bioorg.Med. Chem. 5, 49.
LoGrasso, P.V., et al. 1997.Biochem.36, 10422.
Jiang, Y., et al. 1996.J. Biol. Chem. 271, 17920.
Kramer, R.M., et al. 1996.J. Biol. Chem.271, 27723.
Li, Z., et al. 1996.Biochem.Biophys.Res.Commun.228, 334.
Lee, J.C., et al. 1994.Nature 372, 739.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
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