GLUT1 Inhibitor

BAY-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.

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.

WZB117 is a glucose transporter 1 (Glut1) inhibitor, which downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo.

KL-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.

(-)-Epicatechin gallate (Epicatechin gallate) inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 7.5 μM. (-)-Epicatechin gallate is a GLUT1 and GLUT5 inhibitor. (-)-Epicatechin gallate decreases cell growth of GLUT5-expressing hxt⁰ yeast cells.

FKL-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.

Glutoborin is an orally active GLUT1-specific proteasome inhibitor with a K_d value of 119 nM for GLUT1. Glutoborin binds to GLUT1, inhibits proteasome activity, restricts IκBα degradation, blocks NF-κB activation, and inhibits GLUT1-mediated glucose transport to elevate blood glucose levels. Glutoborin inhibits pro-inflammatory gene expression, B cell activation, autoantibody production and macrophage function, disrupts the interaction between macrophages and B cells, and alleviates systemic inflammation, neuroinflammation and blood-brain barrier damage. Glutoborin can be used in research related to cerebral malaria.

STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC₅₀ of 1 μM. STF-31 is also a NAMPT inhibitor. STF-31 inhibits glucose uptake in renal cell carcinoma (RCC) 4 cells.

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC₅₀s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases.

Fasentin, 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.

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC₅₀s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity.

Zingibroside 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.

Licoflavone A is an orally active PTP1B/VEGFR-2 inhibitor, with an IC₅₀ of 54.5 μM against PTP1B, an IC₅₀ of 14.36 μM and a K_d of 142.38 nM against human VEGFR-2. Licoflavone A blocks the PI3K/AKT and MEK/ERK signaling pathways. Licoflavone A induces G1 phase cell cycle arrest, apoptosis via the intrinsic mitochondrial pathway (apoptosis), and inhibits migration, invasion and epithelial-mesenchymal transition (EMT) of gastric cancer cells. Licoflavone A inhibits the proliferation of gastric cancer cells in vitro and in xenograft models. Licoflavone A reduces the expression levels of HIF-1α, GLUT1, LDHA, PKM2 and HK2 in hypoxic gastric cancer cells, decreases glucose uptake and suppresses glycolysis. Licoflavone A can be used in research related to gastric cancer, type 2 diabetes and obesity.

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.

Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC₅₀ of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a K_i of 15 μM. Lavendustin B is also a weak inhibitor of tyrosine kinases.

4,6-O-ethylidene-α-D-glucose (Ethylidene-glucose), a glucose derivative, is a competitive exofacial binding-site inhibitor on glucose transporter 1 (GLUT1) with a K_i of 12 mM for wild-type 2-deoxy-D-glucose transport.

HK2-IN-3 is a selective HK2 inhibitor with a human IC₅₀ of 0.0564 μM (56.4 nM). HK2-IN-3 induces mitophagy in oral squamous cell carcinoma cells. HK2-IN-3 exerts anti-cancer activity in oral squamous cell carcinoma cells. HK2-IN-3 can be used for the research of oral squamous cell carcinoma.

GLUT1/EGFR-IN-1 (compound H) is a potent inhibitor of GLUT1 and EGFR. GLUT1/EGFR-IN-1 can simultaneously act on the EGFR tyrosine kinase ATP-binding site and inhibit GLUT1-mediated energy metabolism, resulting in reductions in ATP, MMP, intra-cellular lactic acid, and EGFR nuclear transfer. GLUT1/EGFR-IN-1 can be used for nasopharyngeal carcinoma (NPC) and triple-negative breast cancer (TNBC) research.

GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC₅₀ values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer.

KCN1 is a p300/HIF-1α interaction inhibitor with a K_d value of 345 nM for p300-CH1. KCN1 binds to the CH1 domain of p300, blocks the assembly of the p300/HIF-1α complex, and disrupts the HIF-1α-p300/CBP interaction. KCN1 inhibits cancer cell growth, induces cancer cell cycle arrest and apoptosis. KCN1 inhibits β-galactosidase activity and downregulates the expression of VEGF, Glut1, CA9 and CAIX. KCN1 exerts anticancer activity in mouse tumor xenograft models. KCN1 can be used in research related to malignant glioma, pancreatic cancer and metastatic uveal melanoma.