AMG-548 (dihydrochloride)

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

Product Specifications

CAS Number

[2518299-32-4]

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

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/amg-548-dihydrochloride.html

Concentration

10mM

Purity

99.86

Solubility

DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1N(C)C(NCC(N)CC2=CC=CC=C2)=NC(C3=CC=NC=C3)=C1C4=CC=C5C=CC=CC5=C4.Cl.Cl

Molecular Formula

C29H29Cl2N5O

Molecular Weight

534.48

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.