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

AMG-548 dihydrochloride 

Cat. No.: HY-108642B Purity: >98.0%
Handling Instructions

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). AMG-548 dihydrochloride 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 dihydrochloride Chemical Structure

AMG-548 dihydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 317 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 270 In-stock
Estimated Time of Arrival: December 31
10 mg USD 450 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

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].

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)

JNK 1

11480 nM (Ki)

JNK 2

39 nM (Ki)

JNK 3

61 nM (Ki)

CK1

 

In Vitro

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

In Vivo

AMG-548 dihydrochloride 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

534.48

Formula

C₂₉H₂₉Cl₂N₅O

SMILES

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

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: >98.0%

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Keywords:

AMG-548AMG548AMG 548p38 MAPKCasein Kinaseselectivep38αp38βTNFαWntdevelopmentstemcellsInhibitorinhibitorinhibit

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Product name:
AMG-548 dihydrochloride
Cat. No.:
HY-108642B
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