GLUT1
GLUT1 (SLC2A1) provides basal glucose uptake and supports cellular glucose transport across physiological and pathological contexts[1]. Mechanistically, GLUT1 belongs to the sugar porter family, where glucose transport depends on conserved substrate coordination and conformational regulation[2]. In disease models, impaired GLUT1 function causes Glut1 deficiency syndrome, a brain energy failure syndrome driven by reduced glucose transport across brain tissue barriers[3][4]. Compared with GLUT3, GLUT1 shares a conserved substrate-binding site but differs in transport affinity, making isoform distinction essential for transporter-specific experimental design[2]. GLUT1 and GLUT3 also transport dehydroascorbic acid, whereas GLUT2, GLUT5, and SGLT1 do not transport DHA in the tested oocyte system[5]. For experimental applications, WZB117 inhibits GLUT1-mediated sugar transport and downregulates glycolysis, supporting its use in glucose uptake and cancer metabolism studies[6][7].
References:
- [1]. Pragallapati S, et al. Glucose transporter 1 in health and disease. J Oral Maxillofac Pathol. 2019 Sep-Dec;23(3):443-449. [Content Brief]
- [2]. Custódio TF, et al. Structural comparison of GLUT1 to GLUT3 reveal transport regulation mechanism in sugar porter family. Life Sci Alliance. 2021 Feb 3;4(4):e202000858. [Content Brief]
- [3]. Klepper J, et al. Glut1 Deficiency Syndrome (Glut1DS): State of the art in 2020 and recommendations of the international Glut1DS study group. Epilepsia Open. 2020 Aug 13;5(3):354-365. [Content Brief]
- [4]. Tang M, et al. Brain microvasculature defects and Glut1 deficiency syndrome averted by early repletion of the glucose transporter-1 protein. Nat Commun. 2017 Jan 20;8:14152. [Content Brief]
- [5]. Rumsey SC, et al. Glucose transporter isoforms GLUT1 and GLUT3 transport dehydroascorbic acid. J Biol Chem. 1997 Jul 25;272(30):18982-9. [Content Brief]
- [6]. Liu Y, et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol Cancer Ther. 2012 Aug;11(8):1672-82. [Content Brief]
- [7]. 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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GLUT1 Related Products (26)
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Antibodies (1)
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BAY-876
0 ImagesBAY-876, a chemical probe, is an orally active and selective glucose transporter 1 (GLUT1) inhibitor with an IC50 of 2 nM. BAY-876 is >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth. In addition, BAY-876 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis. -
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Phloretin
0 ImagesPhloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill.，has anti-inflammatory activities. Phloridzin is a specific，competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM，respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation. -
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KL-11743
0 ImagesKL-11743 is a potent, orally active, and glucose-competitive inhibitor of the class I glucose transporters, with IC50s of 115, 137, 90, and 68 nM for GLUT1, GLUT2, GLUT3, and GLUT4, respectively. KL-11743 specifically blocks glucose metabolism. KL-11743 can synergize with electron transport inhibitors to induce cell death. In addition, KL-11743 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis. -
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(-)-Epicatechin gallate
0 ImagesSynonyms: Epicatechin gallate; ECG; (-)-Epicatechin 3-O-gallate -
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FKL-137
0 ImagesCat. No.: HY-183069FKL-137 is a GLUT1 and PI3K/AKT signaling pathway inhibitor. FKL-137 binds to GLUT1, reduces glucose uptake and lactate secretion, downregulates glucose metabolism-related proteins, and inhibits erythroleukemia cell proliferation. FKL-137 downregulates PI3K, p-PI3K, AKT, p-AKT levels, disrupts the PI3K/AKT-GLUT1 positive feedback loop, and suppresses erythroleukemia cell proliferation. FKL-137 induces apoptosis via upregulated Bax, Cleaved-PARP and downregulated Bcl-2, PARP. FKL-137 can be used for the research of erythroleukemia. -
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HK2-IN-3
0 ImagesCat. No.: HY-180805CAS No.: 2679261-30-2HK2-IN-3 (compound 12) is a potent hexokinase 2 (HK2) inhibitor with an IC50 of 56.4 nM. HK2-IN-3 reduces glucose uptake and downregulated GLUT1/GLUT4 in oral squamous cell carcinoma (OSCC). HK2-IN-3 induces mitophagy and apoptosis. HK2-IN-3 suppresses tumor growth and angiogenesis in OSCC xenograft mouse models. HK2-IN-3 can be used for OSCC research. -
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CDr17
0 ImagesCat. No.: HY-D3410CAS No.: 2991899-29-5CDr17 is a GLUT1 substrate and selective fluorescent dye staining M1 microphages. CDr17 utilizes the Gating-Oriented Live-cell Distinction (GOLD) mechanism to enter M1 macrophages (Ex/Em = 646/662 nm). -
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- GLUT inhibitor-1
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Fasentin
0 ImagesFasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity. -
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- GLUT4-IN-2
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Hydroxylamine (50% w/w in water)
0 ImagesHydroxylamine (50% w/w in water) is an inorganic highly reactive compound and antibacterial agent. Hydroxylamine (50% w/w in water) acutely activates the transport activity of GLUT1, inhibits Monoamine oxidase activity. Hydroxylamine (50% w/w in water) inhibits nitrite oxidizing bacteria. Hydroxylamine (50% w/w in water) activates glucose uptake. Hydroxylamine (50% w/w in water) can be used in the research of inflammatory diseases and allergies[1][2][3][4]. -
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Zingibroside R1
0 ImagesZingibroside R1 is an orally active triterpene saponin with multiple biological activities including antioxidant, anti-inflammatory, antiviral, and metabolic regulatory properties. Zingibroside R1 reduces the expression of PIN family members, inhibits the expression of PLT1/PLT2, WOX5, SHR, and SCR, disrupts auxin transport and distribution, triggers plant ROS responses, and inhibits root growth. Zingibroside R1 extends the lifespan of Caenorhabditis elegans, enhances its heat stress resistance, and improves its motor ability. Hydrogel derivatives of Zingibroside R1 inhibit the proliferation of Candida albicans by binding to its β-1,3-glucan and exhibit antifungal activity. Zingibroside R1 inhibits GLUT1-mediated uptake and alleviates liver injury. Zingibroside R1 can be used in research related to neurodegenerative diseases, vulvovaginal candidiasis, acute liver injury, Ehrlich ascites tumor and HIV-1 infection. -
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4'-Bromo-resveratrol
0 ImagesSynonyms: 4′‐BR4'-Bromo-resveratrol (4′‐BR) is a dual SIRT1/SIRT3 inhibitor with an IC50 of 0.2 mM for both targets. 4'-Bromo-resveratrol induces caspase-dependent apoptosis, induces G0/G1 cell cycle arrest, and inhiibits proliferation. 4'-Bromo-resveratrol reduces lactate production, glucose uptake, and NAD+/NADH ratio, and downregulates lactate dehydrogenase A and glucose transporter 1 (GLUT1). 4'-Bromo-resveratrol can be used for the research of melanoma. -
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NGI-235
0 ImagesNGI-235 is an STT3A-selective oligosaccharyltransferase complex OST-A inhibitor. NGI-235 preferentially inhibits OST-A catalytic activity, impairing N-glycosylation of OST-A substrates. NGI-235 causes the hypoglycosylation of both TLR4, GLUT1 and inhibits NF-κB signaling. NGI-235 can be used for the research of inflammation. -
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2-Amino-2-deoxyglucose hydrochloride
0 ImagesSynonyms: D-Glucosamine Hydrochloride2-Amino-2-deoxyglucose hydrochloride (D-Glucosamine Hydrochloride) is a glucose analog that is specifically recognized and transported by the cell membrane GLUT1. 2-Amino-2-deoxyglucose hydrochloride acts as a tumor-targeting ligand and a guiding molecule for the synthesis of prodrug conjugates, thus delivering drugs precisely to tumor cells. 2-Amino-2-deoxyglucose hydrochloride is applicable to diagnostic imaging and therapeutic efficacy monitoring of solid tumors and various cancers (e.g., breast cancer, glioblastoma). 2-Amino-2-deoxyglucose hydrochloride also helps bacteria resist lysozyme digestion by integrating into the non-N-acetylated residues of Streptococcus pneumoniae peptidoglycan. 2-Amino-2-deoxyglucose hydrochloride is used in studies on tumor metabolism and the exploration of bacterial drug resistance mechanisms. -
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Phloretin (Standard)
0 ImagesSynonyms: NSC 407292 (Standard); RJC 02792 (Standard)Phloretin (Standard) is the analytical standard of Phloretin. This product is intended for research and analytical applications. Phloretin (NSC 407292; RJC 02792) is a flavonoid extracted from Malus pumila Mill., has anti-inflammatory activities. Phloridzin is a specific, competitive and orally active inhibitor of sodium/glucose cotransporters in the intestine (SGLT1) and kidney (SGLT2). Phloretin inhibits Yeast-made GLUT1 as well as Human erythrocyte GLUT1 with IC50values of 49 μM and 61 μM, respectively.Phloretin has the potential for the treatment of rheumatoid arthritis (RA) and allergic airway inflammation. -
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- Lavendustin B
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- 4,6-O-Ethylidene-α-D-glucose
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