SB202190 化学特性,用途語,生産方法
外観
白色〜うすい黄褐色, 結晶〜粉末又は塊
溶解性
メタノールに溶ける。
説明
SB 202190 is a selective, potent, cell-
permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC
50 values of 50 and 100 nM, respectively. When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs). Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket. Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-
induced receptor expression, and HIV-
mediated depressive disorder.
定義
ChEBI: A member of the class of imidazoles that is 1H-imidazole in which the hydrogens at positions 2, 4, and 5 are replaced by 4-hydroxyphenyl, pyridin-4-yl, and 4-fluorophenyl groups, respectively. It is a widely used inhibitor of mitogen-act
vated protein kinase (MAPK) alpha and beta.
一般的な説明
A potent, reversible, competitive, and cell-permeable inhibitor of p38 MAP kinase. Inhibits p38 phosphorylation of myelin basic protein (MBP) with no effect on the activity of the ERK or JNK MAP kinase subgroups. Also inhibits the kinase activity of p38β (K
i = 16 nM; IC
50 = 350 nM) and p38 phosphorylation of activating transcription factor 2 (ATF-2; IC
50 = 280 nM). Blocks LPS-induced TNF-α and interleukin biosynthesis. Reported to induce LDL receptor expression in Hep52 cells. A 1 mg/ml solution of SB 202190 (Cat. No.
559397) in anhydrous DMSO is also available.
生物活性
A highly selective, potent and cell-permeable inhibitor of p38 MAP kinase. Binds within the ATP pocket of the active kinase (K d = 38 nM, as measured in recombinant human p38), and selectively inhibits the p38 α and β isoforms (IC 50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38 β 2 respectively). Also available as part of the MAPK Inhibitor Tocriset™ .
SB202190 上流と下流の製品情報
原材料
準備製品