1. Epigenetics PI3K/Akt/mTOR Metabolic Enzyme/Protease
  2. AMPK Acetyl-CoA Carboxylase
  3. AMPK activator 18

AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes.

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AMPK activator 18

AMPK activator 18 Chemical Structure

CAS No. : 1364692-88-5

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Based on 1 publication(s) in Google Scholar

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Description

AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes[1].

IC50 & Target[1]

AMPK α2β2γ1

17.2 nM (EC50)

α2β2γ3

82.1 nM (EC50)

In Vitro

AMPK activator 18 potently and selectively activates α2-containing AMPK complexes, particularly the skeletal muscle-enriched α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 ± 1.6 nM and 82.1 ± 1.3 nM respectively, and its activation is dependent on the β2-D111 residue but not the β2 N-terminal helix[1].
AMPK activator 18 (0.03-10 μM; 1 h) triggers AMPK signaling in differentiated C2C12 myotubes and β2-reconstituted iMEFs via an allosteric mechanism independent of changes to intracellular AMP/ATP ratio or AMPK α-T172 phosphorylation, inducing dose-dependent ACC phosphorylation[1].
AMPK activator 18 (1-2 μM) increases ACC phosphorylation and AMPK α-T172 phosphorylation levels in Epitrochlearis muscles[1].
AMPK activator 18 (10 μM) reduces 2-deoxyglucose (2DG) uptake in soleus and extensor digitorum longus muscles[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: β2-expressing b1/2 dKO iMEFs
Concentration: 1 μM; 10 μM
Incubation Time: 1 h
Result: Induced a significant increase in ACC phosphorylation without altering AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 1 μM.
Induced ACC phosphorylation associated with an increase in AMPK α-T172 phosphorylation in β2-reconstituted iMEFs at 10 μM.
Molecular Weight

471.90

Formula

C26H18ClN3O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC(OC2=NC3=NC(=C(Cl)C=C3N2)C4=CC=C(C=C4)C5=CC=CC=C5O)=CC=C1C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Purity & Documentation
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AMPK activator 18
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HY-115549
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