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Submit ReviewAMG 548 is a potent and selective inhibitor of p38α (Ki values are 0.5, 3.6, 2600 and 4100 nM for p38α, p38β, p38γ and p38δ respectively). Displays >1000-fold selectivity against 36 other kinases; inhibits whole blood LPS-stimulated TNFα (IC50 = 3 nM). Efficacious in acute and chronic models of arthritis.
AMG 548 is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 461.56 |
公式 | C29H27N5O |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 864249-60-5 |
PubChem ID | 11167112 |
InChI Key | RQVKVJIRFKVPBF-VWLOTQADSA-N |
Smiles | O=C1N(C)C(NC[C@@H](N)CC5=CC=CC=C5)=NC(C4=CC=NC=C4)=C1C3=CC2=C(C=C3)C=CC=C2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 49.8 | 100 | |
ethanol | 49.8 | 100 |
以下数据基于产品分子量 461.56。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.17 mL | 10.83 mL | 21.67 mL |
5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Dominguez et al (2005) p38 MAP kinase inhibitors: many are made, but few are chosen. Curr.Opin.Drug Discov.Devel. 8 421 PMID: 16022178
Lee and Dominguez (2005) MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38α protein. Curr.Med.Chem. 12 2979 PMID: 16378500
If you know of a relevant reference for AMG 548, please let us know.
关键词: AMG 548, AMG 548 supplier, AMG548, potent, selective, p38alpha, p38a, p38α, inhibitors, inhibits, p38, 3920, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AMG 548 的部分引用包括:
Rozbeh et al (2014) The cellular thermal shift assay for evaluating drug target interactions in cells. Nat Protoc 9 2100-22 PMID: 25101824
Kai et al (2022) Small Molecule Arranged Thermal Proximity Coaggregation (smarTPCA)-A Novel Approach to Characterize Protein-Protein Interactions in Living Cells by Similar Isothermal Dose-Responses. Int J Mol Sci 23 PMID: 35628420
Eckle et al (2013) HIF1A reduces acute lung injury by optimizing carbohydrate metabolism in the alveolar epithelium. J Biol Chem 11 e1001665 PMID: 24086109
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.