| Identification | Back Directory | [Name]
2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone dihydrochloride | [CAS]
864249-60-5 | [Synonyms]
AMG 548
AMG-548
(AMG548)
AMG-548 dihydrochloride
2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone
4(3H)-Pyrimidinone, 2-[[(2S)-2-amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-
2-[[(2S)-2-Amino-3-phenylpropyl]amino]-3-methyl-5-(2-naphthalenyl)-6-(4-pyridinyl)-4(3H)-pyrimidinone dihydrochloride | [Molecular Formula]
C29H27N5O | [MDL Number]
MFCD26792556 | [MOL File]
864249-60-5.mol | [Molecular Weight]
461.56 |
| Hazard Information | Back Directory | [Uses]
AMG 548 is a selective and efficacious p38 mitogen-activated protein (MAP) kinase inhibitor, which are a class of inhibitors that are investigated towards treating inflammatory diseases. | [Biological Activity]
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]. | [storage]
Store at -20°C | [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/?. chem biol, 2011, 18(4): 485-494. |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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DC Chemicals
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021-58447131 13564518121 |
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www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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cjbscvictory
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13348960310 13348960310; |
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https://www.weikeqi-biotech.com/ |
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