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AMG 548

カタログ番号GC14899

AMG 548、経口活性および選択的 p38α 阻害剤 (Ki = 0.5 nM) は、p38β (Ki = 36 nM) に対してわずかに選択的であり、p38γ および p38δ に対して >1000 倍選択的です。

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AMG 548 化学構造

Cas No.: 864249-60-5

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1mg
$81.00
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5mg
$243.00
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10mg
$405.00
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25mg
$810.00
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50mg
$1,305.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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:
[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/ɛ. Chem Biol, 2011, 18(4): 485-494.

Chemical Properties

Cas No. 864249-60-5 SDF
Chemical Name (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
Formula C29H27N5O M.Wt 461.56
溶解度 <49.8mg/ml in DMSO; <49.8mg/ml in ethanol Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.1666 mL 10.8328 mL 21.6657 mL
5 mM 0.4333 mL 2.1666 mL 4.3331 mL
10 mM 0.2167 mL 1.0833 mL 2.1666 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 10 reference(s) in Google Scholar.)

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