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product name
SB 202190, SB 202190, CAS 152121-30-7, is a potent, reversible, competitive inhibitor of p38. Inhibits p38 phosphorylation of myelin basic protein. Blocks the activity of p38β (Ki = 16 nM; IC₅₀ = 350 nM).
品質等級
化驗
≥98% (HPLC)
形狀
solid
效力
16 nM Ki
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
pale yellow
溶解度
DMSO: 50 mg/mL
運輸包裝
ambient
儲存溫度
−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 密鑰
NJNKPVPFGLGHPA-UHFFFAOYSA-N
一般說明
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）
重構
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。
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
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