1. MAPK/ERK Pathway
    Stem Cell/Wnt
    Cell Cycle/DNA Damage
  2. p38 MAPK
    Casein Kinase
  3. AMG-548 hydrochloride

AMG-548 hydrochloride 

Cat. No.: HY-108642A
Handling Instructions

AMG-548 hydrochloride is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand 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 direcly inhibing Casein kinase 1 isoforms δ and ε.

For research use only. We do not sell to patients.

AMG-548 hydrochloride Chemical Structure

AMG-548 hydrochloride Chemical Structure

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Description

AMG-548 hydrochloride is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand 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 direcly inhibing Casein kinase 1 isoforms δ and ε[2].

IC50 & Target[1,2]

p38α

0.5 nM (Ki)

p38β

3.6 nM (Ki)

CK1

 

In Vivo

AMG-548 hydrochloride has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1].

Molecular Weight

498.02

Formula

C₂₉H₂₈ClN₅O

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
AMG-548 hydrochloride
Cat. No.:
HY-108642A
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