1. Signaling Pathways
  2. Epigenetics
    PI3K/Akt/mTOR
  3. AMPK
  4. AMPK α1β2γ1 Isoform

AMPK α1β2γ1

AMPK α1β2γ1 is an AMP-activated protein kinase heterotrimer composed of catalytic α and regulatory β/γ subunits, linking cellular energy sensing with energy homeostasis[1]. Mechanistically, AMP and glycogen regulate human α1β2γ1 holo-AMPK through nucleotide-dependent and glycogen-mimic interactions, supporting its use in structural studies of allosteric regulation[1]. In human liver, chemoproteomic profiling identified α1β2γ1 as the predominant AMPK heterotrimer, whereas dog and rat livers mainly contained α1β1γ1 and α2β1γ1 forms[2]. In human skeletal muscle, only three AMPK trimer combinations were detected, and α1β2γ1 appeared with α2β2γ1 and α2β2γ3, providing a disease-relevant context for type 2 diabetes and training studies[3]. Compared with α2 complexes, α1-containing AMPK complexes showed higher specific activity and lower Km for SAMS peptide, while β2-containing isoforms were less sensitive to A769662 than β1 isoforms[4]. For agonist design, C2 activated α1β1γ1 and α1β2γ1 γ1 complexes, whereas SC4 showed poor activation potential against α1β2γ1[5][6].

AMPK α1β2γ1 관련 제품 (4):

Cat. No. 상품명 효과 Purity
  • HY-112769
    EX229
    Activator 99.44%
    EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
  • HY-117755
    PF-739
    Activator 99.79%
    PF-739 is an orally active and non-selective activator of AMPK. PF-739 activates 12 heterotrimeric AMPK complexes and significantly reduces the level of glucose in plasma complexes.
  • HY-160004
    PXL770
    Activator 99.56%
    PXL770 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).
  • HY-147038
    AMPK activator 8
    Activator
    AMPK 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.