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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. Find out more about compound libraries available from Tocris.
M. Wt | 461.56 |
Formula | C29H27N5O |
Storage | Store at -20°C |
Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 49.8 | 100 | |
ethanol | 49.8 | 100 |
The following data is based on the product molecular weight 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.
Concentration / Solvent Volume / Mass | 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 |
References are publications that support the biological activity of the product.
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.
Keywords: AMG 548, AMG 548 supplier, AMG548, potent, selective, p38alpha, p38a, p38α, inhibitors, inhibits, p38, 3920, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for AMG 548 include:
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
Do you know of a great paper that uses AMG 548 from Tocris? Please let us know.
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.