GLUT 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.

Phlorizin (Floridzin) is an orally active non-selective sodium-glucose cotransporter (SGLT) inhibitor, with an IC₅₀ of 0.04 μM and a K_i of 39 nM against hSGLT2, and an IC₅₀ of 0.17 μM and a K_i of 0.31 μM against hSGLT1. Phlorizin promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

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.

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.

Xanthine oxidase-IN-23 (Compound BPF) is an orally active, reversible, mixed-type Xanthine oxidase inhibitor with an IC₅₀ of 3.33 μM. Xanthine oxidase-IN-23 directly binds to XOD in a reversible mixed-type manner to inhibit its catalytic activity. Xanthine oxidase-IN-23 upregulates ABCG2 and downregulates GLUT9 to promote renal urate excretion. Xanthine oxidase-IN-23 reduces serum urate levels and improves renal function in hyperuricemic mice. Xanthine oxidase-IN-23 can be used in the research of hyperuricemia.

(-)-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.

MSNBA is a potent and selective GLUT5 fructose transport inhibitor with an IC₅₀ of 0.10 mM. MSNBA does not affect the transport activity of human GLUT1, GLUT2, GLUT3, GLUT4 or bacterial GlcPSe. MSNBA competitively inhibits GLUT5 fructose uptake with a K_i of 3.2 μM in MCF7 cells. MSNBA can be used for the study of cancer or diabetes.

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.

Glutor is a selective GLUT 1/2/3 inhibitor that can suppress glucose uptake. Glutor can inhibit glycolysis and has anti-tumor activity, inducing cell apoptosis.

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.

Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase).

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.

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.

DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor 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.

(-)-Epicatechin gallate (Standard) is the analytical standard of (-)-Epicatechin gallate. This product is intended for research and analytical applications. (-)-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.

Flavokawain C is an orally active natural chalcone. Flavokawain C inhibits the proliferation of various cancer cells. Flavokawain C upregulates GADD153 in cancer cells, inhibits the phosphorylation of Akt and JNK, suppresses early ERK phosphorylation, activates late ERK phosphorylation, activates caspase related subtypes, induces PARP-1 cleavage, causes upregulation of p21 and p27, downregulation of mutant p53 and anti-apoptotic IAP proteins, elevates intracellular ROS levels, reduces SOD activity, and induces apoptosis. Flavokawain C downregulates FABP4, induces autophagy in cancer cells, and activates the AMPK/mTOR pathway. Flavokawain C decreases the expression of glycolysis-related proteins GLUT1 and HK2, and inhibits glycolysis in nasopharyngeal carcinoma cells. Flavokawain C inhibits the activation of the EGFR/PI3K/Akt/mTOR signaling pathway and reduces the expression of HSP90B1. Flavokawain C inhibits angiogenesis by decreasing the expression of angiogenic proteins Ang-1 and VEGF in human umbilical vein endothelial cells. Flavokawain C increases γ-H2AX levels in cells, inhibits the phosphorylation of FAK, PI3K and AKT in cells, and induces DNA damage in cells. Flavokawain C exerts anti-tumor activity in multiple tumor xenograft mouse models. Flavokawain C is applicable to research related to colorectal cancer, colon adenocarcinoma, nephroblastoma, nasopharyngeal carcinoma and liver cancer.