GLUT Inhibitor

URAT1/GLUT9-IN-3 is an orally active URAT1/GLUT9 dual inhibitor with IC₅₀ values of 4.01 and 1.60 μM. URAT1/GLUT9-IN-3 inhibits URAT1-mediated uric acid uptake and GLUT9-mediated uric acid transport, reducing renal urate reabsorption. URAT1/GLUT9-IN-3 reduces serum uric acid levels in hyperuricemic mice. URAT1/GLUT9-IN-3 can be used for the researches of gout and hyperuricemia.

Rapaglutin A is a glucose transporter (GLUT) inhibitor. Rapaglutin A is a pan-GLUT inhibitor of Class I isoforms GLUT1, GLUT3, and GLUT4 with an IC₅₀ of 12 nM. Rapaglutin A has an inhibitory effect on A549 proliferation.

NLRP3/URAT1-IN-1 is an orally active double inhibitor of NLRP3 and URAT1 (IC₅₀ = 3.81 μM). NLRP3/URAT1-IN-1 inhibits IL-1β release in LPS (HY-D1056) and ATP-stimulated mouse bone marrow-derived macrophages (BMDMs), with an IC₅₀ of 2.61 μM. NLRP3/URAT1-IN-1 reduces serum uric acid (SUA) and alleviates liver/kidney damage in mice with acute hyperuricemia (HUA). NLRP3/URAT1-IN-1can be used for the study of gout and hyperuricemia.

GLUT-1-IN-4 (Compound 13) is the p53 protein-dependent inhibitor for GLUT-1 glucose transporter. GLUT-1-IN-4 inhibits the proliferation of multiple cancer cells with IC₅₀ in submicromolar levels. GLUT-1-IN-4 arrests the cell cycle, stimulates oxidative stress, and induces apoptosis.

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.

URAT1/GLUT9-IN-2 is a selective, orally active URAT1/GLUT9 inhibitor, with an IC₅₀ of 2.81 μM against URAT1 and an IC₅₀ of 12.53 μM against GLUT9. URAT1/GLUT9-IN-2 reduces serum uric acid levels and protects renal function. URAT1/GLUT9-IN-2 can be used in research related to hyperuricemia and hyperuricemic nephropathy.

Antitumor agent-102 (compound 10) is a conjugate of Topoisomerase I inhibitor SN38 and glucose transporter inhibitor, targeting to colorectal cancer. Antitumor agent-102 induces higher concentrations of free SN38 in tumor tissues than Irinotecan (HY-16562).

WZB117-PPG is a glucose transporter 1 (GLUT1) inhibitor with anticancer activity. WZB117-PPG has remarkable photolysis efficiency and cytotoxicity to cancer cells under visible light irradiation.

hURAT1 inhibitor 1 (compound 27b) is an isomarine-based, orally active dual hURAT1/GLUT9 inhibitor with IC₅₀s of 0.16 μM and 4.47 μM, respectively, and has anti-hyperuricemia effects. hURAT1 inhibitor 1 showed significant uric acid-lowering activity in a hyperuricemia mouse model (10 mg/kg dose). hURAT1 inhibitor 1 had no significant in vitro cytotoxicity or in vivo hepatotoxicity and showed good PK characteristics.

URAT1 inhibitor 4, a Lesinurad derivative, is a potent and orally active URAT1 inhibitor with an IC₅₀ of 7.56 μM. URAT1 inhibitor 4 has higher in vivo urate-lowering efficacy than Lesinurad (HY-15258).

Hydrangeic 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.

VB1-050 is a human antibody expressed in CHO cells, targeting SLC2A8. VB1-050 is composed of huIgG1 heavy chains and huκ light chains, with a predicted molecular weight (MW) of 150 kDa. The isotype control for VB1-050 can refer to Human IgG1 kappa, Isotype Control (HY-P99001).

NV-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.

Rapaglutin E (RgE) is a glucose transporter (GLUT) inhibitor. Rapaglutin E exhibits dose-dependent inhibition of [³H]-2DG uptake in A549, Jurkat T, PANC10.05, and RBC, with IC₅₀ values 8.9 nM, 3.1 nM, 35.5 nM, 74.2 nM. Rapaglutin E inhibits cell proliferation in A549, PANC10.05, HeLa, Jurkat T, and HEK293T cells.

4'-Deoxyphlorizin is an inhibitor of the glucose transport system. 4'-Deoxyphlorizi has good phlorizin hydrolase inhibitory activity with the K_m value of 0.59 nM and the K_i value of 0.33 nM, respectively.

Avicularin (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.

ZINC08383544 is a PKM2 activator with anti-tumor activity. ZINC08383544 binds to the dimer-dimer interface of PKM2, promotes tetramer formation, blocks nuclear translocation, inhibits the expression of glycolysis-related genes such as GLUT1, and reduces T cell-mediated inflammatory responses. ZINC08383544 can be used in cancer-related research such as cervical cancer.

Xanthine oxidase-IN-21, a Genipin (HY-17389) derivative, is an orally active mixed competitive xanthine oxidase (XOD) inhibitor with an IC₅₀ of 0.68 μM. Xanthine oxidase-IN-21 reduces renal fibrosis by decreasing α-SMA expression and suppresses pro-inflammatory cytokines IL-1β, IL-6, and TNF-α through NF-κB pathway regulation. Xanthine oxidase-IN-21 also inhibits URAT1 and GLUT9 expression, promoting uric acid excretion and lowering serum uric acid levels. Xanthine oxidase-IN-21 shows significantly hepatorenal protection activity. Xanthine oxidase-IN-21 can be used for the research of hyperuricemia.

Physagulide Y (2), a withanolide with anticancer activity, is a GLUT1 inhibitor.

BAY-876 (Standard) is the analytical standard of BAY-876 (HY-100017). This product is intended for research and analytical applications. 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.