AMPK α1β1γ1
AMPK α1β1γ1 represents a defined heterotrimeric AMPK isoform built from catalytic α and regulatory β/γ subunits, and AMPK functions as a central cellular energy sensor regulating energy homeostasis[1]. Mechanistically, AMP/ADP/ATP binding to the γ subunit modulates α-subunit kinase activity, while phosphorylation at Thr172 supports AMPK activation under energy stress[2]. In recombinant isoform comparisons, α1β1γ1 was directly evaluated with other AMPK complexes, and α1-containing complexes showed higher specific activity and lower SAMS-substrate Km values than α2 complexes[3]. Compared with related isoforms, β1-containing heterotrimers showed greater sensitivity to A769662 than β2-containing AMPK isoforms, supporting AMPK α1β1γ1 as a useful model for isoform-selective activator design[3]. Disease-relevant models connect AMPK activation with metabolic, inflammatory, cardiac, and cancer biology, including A769662 suppression of IL-6 expression in inflammatory arthritis and α1-mediated cardiomyocyte contractile regulation through troponin I phosphorylation[4][5]. For experimental applications, C2 and C13 act preferentially on α1-containing complexes, whereas LCFA-CoA esters activate β1-containing AMPK isoforms through the allosteric drug and metabolite site[6][7].
References:
- [1]. Viollet B, et al. AMPK inhibition in health and disease. Crit Rev Biochem Mol Biol. 2010 Aug;45(4):276-95. [Content Brief]
- [2]. Yan Y, et al. Structure and Physiological Regulation of AMPK. Int J Mol Sci. 2018 Nov 9;19(11):3534. [Content Brief]
- [3]. 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]
- [4]. Guma M, et al. AMPK Activation by A-769662 Controls IL-6 Expression in Inflammatory Arthritis. PLoS One. 2015 Oct 16;10(10):e0140452. [Content Brief]
- [5]. Chen S, et al. Alpha1 catalytic subunit of AMPK modulates contractile function of cardiomyocytes through phosphorylation of troponin I. Life Sci. 2014 Mar 11;98(2):75-82. [Content Brief]
- [6]. Hunter RW, et al. Mechanism of action of compound-13: an α1-selective small molecule activator of AMPK. Chem Biol. 2014 Jul 17;21(7):866-79. [Content Brief]
- [7]. Pinkosky SL, et al. Long-chain fatty acyl-CoA esters regulate metabolism via allosteric control of AMPK β1 isoforms. Nat Metab. 2020 Sep;2(9):873-881. [Content Brief]
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AMPK α1β1γ1 Related Products (12)
Related Products (12)
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Antibodies (6)
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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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PF-06685249
0 ImagesSynonyms: PF-249PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 improves renal function in ZSF-1 rats with diabetic nephropathy. PF-06685249 can be used for diabetic nephropathy research.
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HDAC11-IN-2
0 ImagesHDAC11-IN-2 (compound B6) is a high selective Histone Deacetylase 11 (HDAC11) inhibitor. HDAC11-IN-2 inhibits HDAC11 and HDAC8 with IC50s of 51.1 ×10-3 μM and 5 μM, respectively. HDAC11-IN-2 inhibits denovolipogenesis (DNL) and promotes fatty acid oxidation, thus mitigating hepaticlipid accumulation and pathological symptoms in MASLD mice. HDAC11-IN-2 enhances the phosphorylation of AMPKα1 at Thr172 through the inhibition of HDAC11, consequently modulating DNL and fatty acid oxidation in the liver.
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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 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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BI-9774
0 ImagesCat. No.: HY-171889CAS No.: 1644498-53-2BI-9774 is a potent, selective, and orally active AMPK activator, with EC50 values of 20.0 nM and 63.1 nM against human AMPK α1β1γ1 and AMPK α1β2γ1, respectively. BI-9774 binds to the allosteric drug and metabolite (ADaM) site and induces ACC Ser79 phosphorylation in HepG2 cells, with an EC50 of 83.2 nM. BI-9774 can be used in studies related to AMPK signaling, multiple sclerosis, and non-alcoholic fatty liver disease.
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PF-06679142
0 ImagesCat. No.: HY-120270CAS No.: 1467059-66-0PF-06679142 (Compound 10) is a potent, orally active AMPK activator with an EC50 of 22 nM against α1β1γ1-AMPK. PF-06679142 can be used for diabetic nephropathy research.
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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.
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