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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) [1]. AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].

Product Specifications

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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