AMPK α2β1γ1
AMPK α2β1γ1 is a heterotrimeric serine/threonine kinase complex that supports cellular energy homeostasis through catalytic α2 and regulatory β1/γ1 subunits[1][2]. Mechanistically, AMPK complexes respond to AMP, ADP, ATP, phosphorylation, dephosphorylation, and small-molecule allosteric activation, making subunit composition central to pathway design[2][3]. In recombinant isoform studies, α2-containing complexes showed higher AMP-mediated activation than α1 complexes, while α1 complexes showed higher intrinsic activity and greater phosphatase protection[2]. Compared with β2-containing heterotrimers, β1-containing AMPK isoforms were more sensitive to A-769662 activation, supporting β1-focused assay selection for AMPK α2β1γ1 studies[2]. Structurally, full-length phosphorylated AMPK α2β1γ1 has been used to visualize drug-binding sites and guide crystallographic analysis of activator interactions[4]. For experimental applications, PF-06409577 directly activated AMPK and was developed for diabetic nephropathy research, while SC4-related structures supported design principles for isoform-selective AMPK activators[5][6].
References:
- [1]. Smiles WJ, et al. The metabolic sensor AMPK: Twelve enzymes in one. Mol Metab. 2024 Dec;90:102042. [Content Brief]
- [2]. Rajamohan F, et al. Probing the enzyme kinetics, allosteric modulation and activation of α1- and α2-subunit-containing AMP-activated protein kinase (AMPK) heterotrimeric complexes by pharmacological and physiological activators. Biochem J. 2016 Mar 1;473(5):581-92. [Content Brief]
- [3]. Xiao B, et al. Structural basis of AMPK regulation by small molecule activators. Nat Commun. 2013;4:3017. [Content Brief]
- [4]. Langendorf CG, et al. Visualizing AMPK Drug Binding Sites Through Crystallization of Full-Length Phosphorylated α2β1γ1 Heterotrimer. Methods Mol Biol. 2018;1732:15-27. [Content Brief]
- [5]. Cameron KO, et al. Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy. J Med Chem. 2016 Sep 8;59(17):8068-81.
- [6]. Ngoei KRW, et al. Structural Determinants for Small-Molecule Activation of Skeletal Muscle AMPK α2β2γ1 by the Glucose Importagog SC4. Cell Chem Biol. 2018 Jun 21;25(6):728-737.e9. [Content Brief]
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AMPK α2β1γ1 Related Products (8)
Related Products (8)
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Antibodies (2)
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PXL770
0 ImagesPXL770 is an orally active, direct allosteric AMP-activated protein kinase (AMPK) activator. PXL770 decreases C26:0 levels, improves mitochondrial respiration, reduces expression of proinflammatory genes and induces expression of compensatory transporters (ABCD2/3) in ALD fibroblasts/lymphocytes. PXL770 normalizes plasma VLCFA levels, significantly reduces elevated VLCFA levels in brain and spinal cord in Abcd1 KO mice. PXL770 improves glycemia, dyslipidemia, and insulin resistance in ob/ob and high-fat diet (HFD)-fed mice. PXL770 can be used for the study of X-linked adrenoleukodystrophy (ALD), autosomal dominant polycystic kidney disease and nonalcoholic steatohepatitis (NASH).
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ZLN024 hydrochloride
0 ImagesZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
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AMPKα1 activator 1
0 ImagesCat. No.: HY-181077AMPKα1 activator 1 is a selective and orally active AMPKα1 activator with an EC50 of 35.1 nM. AMPKα1 activator 1 shows 176-fold selectivity over AMPKα2. AMPKα1 activator 1 can be used as a cell protectant and a kidney protectant. AMPKα1 activator 1 attenuates elevation of serum creatinine and blood urea nitrogen levels, alleviates kidney damage, and reduces cellular infiltration in renal ischemia-reperfusion injury contexts. AMPKα1 activator 1 can be associated with renal ischemia-reperfusion injury research.
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AMPK activator 9
0 ImagesCat. No.: HY-148210CAS No.: 1858204-23-5AMPK activator 9 (ZM-6) is a potent AMPK (α2β1γ1) activator with an EC50 value of 1.1 µM. AMPK activator 9 has the potential for the research of type 2 diabetes.
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AMPK activator 8
0 ImagesCat. No.: HY-147038CAS No.: 1852451-96-7AMPK activator 8 (compound 2) is an AMP-activated protein kinase (AMPK) activator with EC50s of 11, 27, 4, 2, and 4 nM for rAMPK α1β1γ1, rAMPK α2β1γ1, rAMPK α1β2γ1, rAMPK α2β2γ1, rAMPK α2β2γ3, respectively. AMPK activator 8 can be used for the research of type 2 diabetes.
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ZLN024
0 ImagesCat. No.: HY-16708CAS No.: 723249-01-2ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
