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, a potent, 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). AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting 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, a potent, 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].

IC50 & Target[1][2]

p38α

0.5 nM (Ki)

p38β

3.6 nM (Ki)

p38δ

2600 nM (Ki)

p38γ

4100 nM (Ki)

dog p38α

5.0 nM (Ki)

JNK1

11480 nM (Ki)

JNK2

39 nM (Ki)

JNK3

61 nM (Ki)

CK1

 

In Vitro

AMG-548 hydrochloride shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 hydrochloride has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFa (IC50=3 nM) and IL1b (IC50=7 nM) as well as TNFa induced IL-8 (IC50=0.7 nM) and IL-1b induced IL-6 (IC5050=1.3 nM) in human whole blood[1].
AMG-548 hydrochloride (10 μM) inhibits the hDvl2 shift[2].

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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