| 应用 |
A p38 MAP Kinase inhibitor with IC50 of 70nM |
| 产品介绍 |
LY2228820是p38MAPK抑制剂，对p38αMAPK和p38βMAPK的IC50分别为7 nM和3 nM。 |
| 生化机理 |
SB 202190 is a p38 MAP (mitogen activated protein) Kinase inhibitor with an IC50 of 7 nm. LY2228820 inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. In multiple myeloma (MM) cells, LY2228820 significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. LY2228820 enhances bortezomib-induced cytotoxicity and apoptosis, but it alone doesn't inhibit the growth of MM.1S cells. LY2228820 also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138? or PB CD14+ cells. LY2228820 also blocks osteoclastogenesis from CD14+ cells. |
| 别名 |
LY 2228820;LY-2228820;5-[2-(叔丁基)-4-(4-氟苯基)-1H-咪唑-5-基]-3-(2,2-二甲基丙基)-3H-咪唑并[4,5-b]吡啶-2-胺二甲磺酸盐;Ralimetinib dimesylate；LY2228820 dimesylate;LY2228820 2MsOH;LY 2228820;LY-2228820；5-[2-(tert-Butyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)-3H-imidazo[4,5-b]pyridin-2-amine dimethanesulfonate |
