AMP-activated protein kinase (AMPK) activator. Stimulates AMPK heterotrimer (α
1) activity (EC50
= 0.3 μ
M). Selectively increases the activity of γ
1- but not γ
3-containing complexes. Thought to directly activate AMPK by antagonizing autoinhibition.
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Turning enzymes ON with small molecules.
Zorn and Wells
Small molecule antagonizes autoinhibition and activates AMP-activated protein kinase in cells.
Pang et al.
PT-1 selectively activates AMPK-γ1 complexes in mouse skeletal muscle, but activates all three γ subunit complexes in cultured human cells by inhibiting the respiratory chain.
Jensen et al.