2437438-16-7
Chemical Structure
AMG-548 hydrochloride
- CAS 番号: 2437438-16-7
- Formula:C29H28ClN5O
- Molecular Weight:498.02
IUPAC Name: (S)-2-((2-amino-3-phenylpropyl)amino)-3-methyl-5-(naphthalen-2-yl)-6-(pyridin-4-yl)pyrimidin-4(3H)-one hydrochloride
InChIKey: OZNZBRANICIEBZ-UQIIZPHYSA-N
SMILES: O=C1N(C)C(NCC(N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4.Cl
Biological Activity: AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM)[1]. AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].
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AMG-548 hydrochloride | AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε. | |||||||||||||||||||||
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- [1]. Lee MR, et al. MAP kinase p38 inhibitors: clinical results and an intimate look at their interactions with p38alphaprotein. Curr Med Chem. 2005;12(25):2979-94. [Content Brief]
- [2]. Verkaar F, 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 Apr 22;18(4):485-94. [Content Brief]
Keywords
