AMG 548
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AMG 548是p38α的强效选择性抑制剂,对p38α\p38β\p38γ和p38δ的IC50值分别为0.5\3.6\2600和4100 nM.
P38促分裂原活化蛋白激酶(P38)是一种丝氨酸/苏氨酸激酶,响应于多种细胞应激,包括炎性细胞因子\渗透压休克\紫外线\脂多糖(LPS)和生长因子.P38α激酶在转录和翻译水平参与TNFα和IL-1β的生物合成[1][2].
AMG 548是p38α的强效选择性抑制剂.在拮抗酶片段互补(EFC)和β连环蛋白驱动的萤光素酶(SuperTOPflash)报告基因实验中,由于与另一个激酶的交叉反应,AMG 548抑制Wnt/β-catenin信号.AMG 548 对17种激酶的抑制超过80％.在U2OS-EFC细胞中,AMG 548抑制在Wnt/β-catenin信号传导活化中起重要作用的CKIδ和CKIε.此外,抑制细胞中CKIδ/ε所需要的AMG 548浓度与EFC和TOPflash实验中抑制Wnt/β-catenin信号传导的AMG 548浓度接近,这表明AMG548抑制Wnt/β-catenin信号是由对CKIδ/ε的抑制介导的[3].
参考文献：
[1]. Dominguez C, Powers DA, Tamayo N. p38 MAP kinase inhibitors: many are made, but few are chosen. Curr Opin Drug Discov Devel, 2005, 8(4): 421-430.
[2]. Lee MR, Dominguez C. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alpha protein. Curr Med Chem, 2005, 12(25): 2979-2994.
[3]. Verkaar F, van der Doelen AA, Smits JF, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/. Chem Biol, 2011, 18(4): 485-494.
| Physical Appearance | Yellow solid |
| Storage | Store at -20°C |
| M.Wt | 461.56 |
| Cas No. | 864249-60-5 |
| Formula | C29H27N5O |
| Solubility | <49.8mg/ml in DMSO; <49.8mg/ml in ethanol |
| Chemical Name | (S)-2-((2-amino-3-phenylpropyl)amino)-3-methyl-5-(naphthalen-2-yl)-6-(pyridin-4-yl)pyrimidin-4(3H)-one |
| SDF | Download SDF |
| 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 |
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化学结构
