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AMG-548 (hydrochloride)

CAT: 0804-HY-108642ASize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-108642ASize:1 Each
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Description
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].
CAS Number
2437438-16-7
UNSPSC
12352005
Target
Casein Kinase; p38 MAPK
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; MAPK/ERK Pathway; Stem Cell/Wnt
Applications
COVID-19-anti-virus
Field of Research
Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/amg-548-hydrochloride.html
Solubility
10 mM in DMSO
Smiles
O=C1N(C)C(NCC(N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4.Cl
Molecular Formula
C29H28ClN5O
Molecular Weight
498.02
References & Citations
[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.|[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CK1; p38α; p38β; p38γ; p38δ

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