GLUT4
GLUT4 is the principal insulin-responsive glucose transporter mediating glucose uptake in skeletal muscle and adipose tissue, thereby supporting whole-body glucose homeostasis[1]. Mechanistically, insulin increases glucose uptake by regulating the trafficking of GLUT4-containing vesicles to the plasma membrane through insulin signaling, including PI3K/Akt-linked processes[2][3]. This trafficking process matters for metabolic disease because impaired insulin-stimulated GLUT4 translocation in muscle and adipose tissue underlies insulin resistance, a major risk factor for type 2 diabetes and other metabolic disorders[3][4]. In disease models, GLUT4 heterozygous knockout mice develop muscle insulin resistance and diabetes, supporting the experimental value of GLUT4 expression and trafficking models[5]. Compared with related isoforms, GLUT4 differs from GLUT1 because its intracellular targeting is isoform specific, and GLUT1 and GLUT4 contain sequence information that directs them to distinct cellular compartments[6][7]. For research applications, human GLUT4 structural analysis with cytochalasin B and endogenous GLUT4 translocation assays provide tools for studying transporter inhibition, trafficking regulation, and insulin resistance in cell models[8][9]. WZB117 also inhibits insulin-regulated GLUT4 more potently than GLUT1 or GLUT3, making isoform selectivity an important variable in inhibitor-based study design[10].
References:
- [1]. Hoeffer CA, et al. Removal of FKBP12 enhances mTOR-Raptor interactions, LTP, memory, and perseverative/repetitive behavior. Neuron. 2008 Dec 10;60(5):832-45. [Content Brief]
- [2]. Leto D, et al. Regulation of glucose transport by insulin: traffic control of GLUT4. Nat Rev Mol Cell Biol. 2012 May 23;13(6):383-96. [Content Brief]
- [3]. van Gerwen J, et al. Insulin signalling and GLUT4 trafficking in insulin resistance. Biochem Soc Trans. 2023 Jun 28;51(3):1057-1069. [Content Brief]
- [4]. Shepherd PR, et al. Glucose transporters and insulin action--implications for insulin resistance and diabetes mellitus. N Engl J Med. 1999 Jul 22;341(4):248-57. [Content Brief]
- [5]. Stenbit AE, et al. GLUT4 heterozygous knockout mice develop muscle insulin resistance and diabetes. Nat Med. 1997 Oct;3(10):1096-101. [Content Brief]
- [6]. Haney PM, et al. Intracellular targeting of the insulin-regulatable glucose transporter (GLUT4) is isoform specific and independent of cell type. J Cell Biol. 1991 Aug;114(4):689-99. [Content Brief]
- [7]. Verhey KJ, et al. Distinct signals in the GLUT4 glucose transporter for internalization and for targeting to an insulin-responsive compartment. J Cell Biol. 1995 Sep;130(5):1071-9. [Content Brief]
- [8]. Yuan Y, et al. Cryo-EM structure of human glucose transporter GLUT4. Nat Commun. 2022 May 13;13(1):2671. [Content Brief]
- [9]. Diaz-Vegas A, et al. A high-content endogenous GLUT4 trafficking assay reveals new aspects of adipocyte biology. Life Sci Alliance. 2022 Oct 25;6(1):e202201585. [Content Brief]
- [10]. Ojelabi OA, et al. WZB117 (2-Fluoro-6-(m-hydroxybenzoyloxy) Phenyl m-Hydroxybenzoate) Inhibits GLUT1-mediated Sugar Transport by Binding Reversibly at the Exofacial Sugar Binding Site. J Biol Chem. 2016 Dec 23;291(52):26762-26772. [Content Brief]
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GLUT4 Related Products (28)
Related Products (28)
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Antibodies (2)
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DS-1150b
0 ImagesCat. No.: HY-173503CAS No.: 1598439-44-1DS-1150b is an orally active GLUT4 activator. DS-1150b has the activity of activating GLUT4 transport and can promote the translocation of GLUT4 to the cell membrane in skeletal muscle cells. DS-1150b has shown hypoglycemic effects in the Zucker obese rat model and can be used in the study of type 2 diabetes mellitus (T2DM).
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Hydrangeic acid
0 ImagesHydrangeic acid is an orally effective stilbene-type glycolipid metabolism regulator that lowers blood glucose and lipids. It can be isolated from processed leaves of Hydrangea macrophylla var. thunbergii. Hydrangeic acid is associated with glycolipid metabolism and insulin sensitivity regulation. Hydrangeic acid does not directly activate PPARγ or PPARα, but instead upregulates the mRNA expression of adiponectin, PPARγ2, GLUT4, and fatty acid-binding protein aP2, and downregulates TNF-α mRNA expression, promoting adipogenesis, glucose uptake, and GLUT4 translocation in 3T3-L1 cells. Simultaneously, Hydrangeic acid inhibits inflammatory factor-induced NO production, exerting activity in improving insulin resistance. Hydrangeic acid can be used in research related to type 2 diabetes and does not cause liver weight gain as a side effect.
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NV-5440
0 ImagesCat. No.: HY-138976CAS No.: 2226614-88-4NV-5440 (Compound I-120) is an mTORC1 inhibitor and glucose transporter inhibitor. NV-5440 targets GLUT-1, -2, -3, and -4, and shows no activity against GLUT-5. NV-5440 inhibits glucose uptake.
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Avicularin (Standard)
0 ImagesAvicularin (Standard) is the analytical standard of Avicularin. This product is intended for research and analytical applications. Avicularin is an orally active flavonoid. Avicularin inhibits NF-κB (p65), COX-2 and PPAR-γ activities. Avicularin has anti-inflammatory, anti-infectious anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities.
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Chiisanogenin
0 ImagesCat. No.: HY-N20708CAS No.: 89353-99-1Chiisanogenin is an orally active triterpenoid. Chiisanogenin reduces postprandial blood glucose by promoting GLUT4 translocation and glucose uptake via activation of the IRS-1/PI3K/Akt signaling pathway. Chiisanogenin binds to MLKL and inhibits its phosphorylation and oligomerization, maintains lysosomal integrity, restores autophagic flux, and suppresses NLRP3 inflammasome activation and pyroptosis. Chiisanogenin inhibits xanthine oxidase activity and regulates oxidative stress and ion pump activity. Chiisanogenin binds to or inhibits PKA, H+/K+-ATPase and β-glucuronidase. Chiisanogenin possesses multiple pharmacological activities, including broad-spectrum antibacterial activity, anticancer, anti-inflammatory, antirheumatic, renoprotective, cardioprotective and antiarrhythmic effects. Chiisanogenin can be used in research related to type 2 diabetes, rheumatoid arthritis, myocardial injury, hepatocellular carcinoma and ventricular arrhythmia.
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GLUT4 activator 3
0 ImagesCat. No.: HY-174145CAS No.: 3088771-32-5GLUT4 activator 3 (Compound 13a) is an antidiabetic agent targeting GLUT4 translocation in skeletal muscle. GLUT4 activator 3 can promote the translocation of glucose transporter 4 (GLUT4) in skeletal muscle cells. GLUT4 activator 3 reduces blood glucose in STZ-induced diabetic rats.
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Antidiabetic agent 7
0 ImagesCat. No.: HY-170943Antidiabetic agent 7 (Compound 5m) is hyperglycemic inhibitor. Antidiabetic agent 7 exhibits promising potency to stimulate GLUT4 translocation in skeletal muscle cells via activating AMPK-dependent pathway. Antidiabetic agent 7 reduces blood glucose levels. Antidiabetic agent 7 shows favorable pharmacokinetic properties. Antidiabetic agent 7 is potential to be used for anti-hyperglycemic research.
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Sennidin A
0 ImagesSennidin A is an anthraquinone derivative and a HCV NS3 helicase inhibitor with an IC50 of 0.8 μM against HCV NS3 helicase. Sennidin A induces Akt phosphorylation at Ser-473 and Thr-308 and promotes GLUT4 translocation to the plasma membrane. Sennidin A inhibits HCV replication. Sennidin A stimulates glucose incorporation and 2-Deoxyglucose uptake in cells. Sennidin A does not induce tyrosine phosphorylation of the insulin receptor or insulin receptor substrate-1. Sennidin A can be used for research on type 2 diabetes and hepatitis C.
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