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

AMG-548 

Cat. No.: HY-108642 Purity: >99.0% ee.: 100%
Handling Instructions

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). AMG-548 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 Chemical Structure

AMG-548 Chemical Structure

CAS No. : 864249-60-5

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Description

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].

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 shows >1000 fold selective against p38γ (Ki=2600 nM) and p38δ (ki=4100 nM). AMG-548 has an modest selectivity against JNK2 (ki=39 nM) and JNK3 (ki=61 nM). AMG-548 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 (10 μM) inhibits the hDvl2 shift[2].

In Vivo

AMG-548 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

461.56

Formula

C₂₉H₂₇N₅O

CAS No.

864249-60-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0% ee.: 100%

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Keywords:

AMG-548AMG548AMG 548p38 MAPKCasein Kinaseselectivep38αp38βTNFαWntdevelopmentstemcellsInhibitorinhibitorinhibit

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AMG-548
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HY-108642
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