GLUT Inhibitor

Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons.

GLUT1-IN-2 (compound 17) is a GLUT1 inhibitor with an IC₅₀ value of 12 μM. GLUT1-IN-2 shows inhibitory effect to Plasmodium falciparum hexose transporter PfHT with an IC₅₀ value of 13 μM. GLUT1-IN-2 can be used for the research of infection.

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.

Phlorizin (Floridzin) dihydrate 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 dihydrate promotes GLUT4 translocation, inhibits gluconeogenesis and promotes glycogen synthesis by activating the PI3K/Akt/mTOR pathway. Phlorizin dihydrate reduces DNA damage and apoptosis (apoptosis) by inhibiting the NF-κB inflammatory pathway. Phlorizin dihydrate induces apoptosis via activating the Caspase pathway by antagonizing the JAK/STAT3 and PCK pathways. Phlorizin dihydrate also exhibits antibacterial, anti-inflammatory and neuroprotective activities.

(R)-Glutor is the R-enantiomer of Glutor (HY-158302). 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.

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.

KPH2f is a safe, orally active, and effective dual URAT1/GLUT9 inhibitor with IC₅₀s of 0.24 μM and 9.37 μM for URAT1 and GLUT9, respectively. KPH2f shows little effects on OAT1 and ABCG2 (IC₅₀=32.14 and 26.74 μM).

MMV009085 is a potent PfHT1 (Plasmodium falciparum hexose transporter)-specific inhibitor and a potential anti-malarial agent . MMV009085 is also a human glucose transporter inhibitor, it has high potency in inhibiting both glucose uptake (IC₅₀: 2.6 μM in glucose uptake assay) and growth of the parasites (EC₅₀: 1.23±0.04 μM against 3D7).

TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC₅₀ = 33.06 nM), moderate to weak URAT1 (IC₅₀ = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.

1-O-p-Coumaroyl-β-D-glucose can promote glucose uptake in HuH7 cells, and be be extracted from Luffa cylindrica (L.) Roem (sponge gourds).

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.

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.

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.

SLC26A3-IN-3 (compound 4az) is a SLC26A3 inhibitor (IC₅₀: 40 nM). SLC26A3-IN-3 can be used for research of constipation, cystic fibrosis.

URAT1/GLUT9-IN-1 (compound 29) can inhibit both uric acid transporter 1 (URAT1) (IC₅₀=2.01 μM) and glucose transporter 9 (GLUT9) (IC₅₀=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research.

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.

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.

GLUT1-IN-3 (Compd 4b), an investigational compound associated with type 1 glucose transporter deficiency syndrome, potently suppresses seizures.

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.