AMG-548

AMG-548, 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 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε[2].

Product Specifications

CAS Number

[864249-60-5]

UNSPSC

12352005

Hazard Statement

H301, H315, H319, H335

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.html

Purity

99.0

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C1N(C)C(NC[C@@H](N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4

Molecular Formula

C29H27N5O

Molecular Weight

461.56

Precautions

H301, H315, H319, H335

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.