CAS NO: | 227449-73-2 |
规格: | 98% |
分子量: | 413.2 |
包装 | 价格(元) |
500ug | 电议 |
1mg | 电议 |
5mg | 电议 |
Background:
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor II is a cell-permeable, pyrimidine-carboxamide compound that selectively and reversibly blocks Syk (IC50 = 41 nM) in an ATP-competitive manner. It is much less potent against PKCε, PKCβII, ZAP-70, Btk, and Itk (IC50s = 5.1, 11, 11.2, 15.5, and 22.6 µM, respectively). Syk inhibitor II has been shown to prevent FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and to inhibit passive cutaneous anaphylaxis reactions in mice (ID50 = 13.2 mg/kg, s.c.).