SB 202190

无

A specific and potent p38 MAP kinase inhibitor

SB 202190 is a selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively.1,2 When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).2 Pyridinyl imidazole inhibitors, including this compound, directly bind p38 MAP kinases in the ATP binding pocket.3 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.4,5,6

331.3

≥98%

4-[4-(4-氟苯基)-5-(4-吡啶基)-1H-咪唑-2-基]苯酚≥98%，杂质≤2%

FC(C=C1)=CC=C1C(N=C(C2=CC=C(O)C=C2)N3)=C3C4=CC=NC=C4

C20H14FN3O

152121-30-7

≥ 4 years

DMF: 10 mg/ml DMSO: 16 mg/ml DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml Ethanol: 0.25 mg/ml

1.Jiang, Y.,Chen, C.,Li, Z., et al. Characterization of the structure and function of a new mitogen-activated protein kinase (p38β). The Journal of Biological Chemisty 271(30), 17920-17926 (1996).
2.Davies, S.P.,Reddy, H.,Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochemistry Journal 351, 95-105 (2000).
3.Fox, T.,Coll, J.T.,Xie, X., et al. A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase. Protein Science 7, 2249-2255 (1998).
4.Fu, X.,Lawson, M.A.,Kelley, K.W., et al. HIV-1 Tat activates indoleamine 2,3 dioxygenase in murine organotypic hippocampal slice cultures in a p38 mitogen-activated protein kinase-dependent manner. Journal of Neuroinflammation 8(88), 1-12 (2011).
5.Riis, J.L.,Johansen, C.,Vestergaard, C., et al. CCL27 expression is regulated by both p38 MAPK and IKKβ signalling pathways. Cytokine 56(3), 699-707 (2011).
6.Röthig, A.,Schreckenberg, R.,Weber, K., et al. Effects of nicotine on PTHrP and PTHrP receptor expression in rat coronary endothelial cells. Cell Physiology and Biochemistry 29, 485-492 (2012).