Syk Inhibitor II 是一种有效的、高选择性和 ATP 竞争性的 Syk 抑制剂,IC50 为 41 nM。
Cas No. | 726695-51-8 |
Canonical SMILES | NCCNC1=NC(NC2=CC(C(F)(F)F)=CC=C2)=C(C(N)=O)C=N1 |
分子式 | C14H15F3N6O |
分子量 | 340.3 |
溶解度 | DMF: 25 mg/ml,DMSO: 15 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs and mediates downstream signaling. 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.). |