CAS NO: | 864249-60-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 864249-60-5 |
化学名 | (S)-2-((2-amino-3-phenylpropyl)amino)-3-methyl-5-(naphthalen-2-yl)-6-(pyridin-4-yl)pyrimidin-4(3H)-one |
Canonical SMILES | O=C1N(C)C(NC[C@H](CC2=CC=CC=C2)N)=NC(C3=CC=NC=C3)=C1C4=CC=C5C(C=CC=C5)=C4 |
分子式 | C29H27N5O |
分子量 | 461.56 |
溶解度 | <49.8mg/ml in DMSO;<49.8mg/ml in ethanol |
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 | AMG 548 is a potent and selective inhibitor of p38α with IC50 values of 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ, respectively. P38 mitogen-activated protein kinase (p38) is a serine/threonine kinase and is responsive to a variety of cellular stresses including inflammatory cytokines, osmotic shock, ultraviolet light, lipopolysaccharides (LPS) and growth factors. P38α kinase involved in the biosynthesis of TNFα and IL-1β at the transcriptional and translational level [1][2]. AMG 548 is a potent and selective p38α inhibitor. In the antagonistic enzyme fragment complementation (EFC) and β-catenin-driven luciferase (SuperTOPflash) reporter gene assays, AMG 548 inhibited Wnt/β-catenin signaling, which was due to cross-reactivity with another kinase. AMG 548 inhibited 17 kinases by more than 80%. In U2OS-EFC cells, AMG 548 inhibited CKIδ and CKIε, which played an important role in the activation of Wnt/b-catenin signaling. Also, the concentration of AMG 548 needed to inhibit CKIδ/ε in cells was closely approximate that required to inhibit Wnt/b-catenin signaling in the EFC and TOPflash assays, which suggested AMG 548 inhibited Wnt/b-catenin signaling mediated by the inhibition of CKIδ/ε [3]. References: |