Galectin Inhibitor

GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a K_d of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.

TD139 is a synthetic galectin-3 inhibitor. TD139 has high affinity for galectin-3 with a K_d of 68 nM, a K_d of 0.22 μM for galectin-1, and a K_d of 38 μM for galectin-7.

Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with K_d values of 24 μM, 49 μM for GAL1 and GAL3, respectively. Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats.

OTX008 is a selective inhibitor of galectin-1.

Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC₅₀ value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis.

Gal-1-IN-1 is a potent and selective human galectin-1 (hGal-1) inhibitor with a K_i of 0.022 μM. Gal-1-IN-1 blocks hGal-1 binding to tumor cells and suppresses human galectin-1-induced pre-apoptosis state. Gal-1-IN-1 reduces hGal-1-expressing cancer cell viability. Gal-1-IN-1 can be used for the research of breast cancer.

GB1841 is an orally active and selective galectin inhibitor with human galectin-1 K_d of 0.027 μM, human galectin-3 K_d of 0.14 μM, mouse galectin-1 K_d of 0.034 μM and mouse galectin-3 K_d of 1.170 μM. GB1841 can be used for the research of lung cancer.

N-Acetyl-D-galactosamine (GalNAc) is a terminal essential amino sugar derived from galactose and forms the antigens of blood group A in humans. N-Acetyl-D-galactosamine (GalNAc) interact with Soya bean agglutinin (SBA), hence decreasing the effects of SBA on cellular membrane permeability and tight junction protein expression in piglets. N-Acetyl-D-galactosamine (GalNAc) inhibits the hemagglutinating activity by the lectin.

Belapectin (GR-MD-02) is a Galectin-3 (Gal-3) inhibitor. Belapectin drives tumor-induced immunosuppression by inducing T cell Apoptosis. Belapectin promotes tumor regression and improves survival of tumor-bearing mice through a CD8+ T cell-dependent mechanism. Belapectin binds to Gal-3 with affinity K_i of 2.8 μM.

N-Acetyllactosamine (N-Acetyl-D-lactosamine), a nitrogen-containing disaccharide, is a galectin-3 inhibitor, which is an important component of various oligosaccharides such as glycoproteins and sialyl Lewis X. N-Acetyllactosamine can be used as the starting material for the synthesis of various oligosaccharides. N-Acetyllactosamine has prebiotic effects.

β-Lactose is a disaccharide commonly found in milk and dairy products. It consists of two monosaccharides, glucose and galactose, linked by β-glycosidic bonds. β-Lactose has various applications in the food industry, especially as a sweetener and bulking agent. Furthermore, it can be used as a substrate for enzymes involved in lactose metabolism and as a model compound for studying carbohydrate-protein interactions.

Anti-Mouse Galectin-9 Antibody (RG9-1) is an anti-mouse Galectin-9 IgG2b monoclonal antibody. Anti-Mouse Galectin-9 Antibody (RG9-1) promotes inflammatory response by enhancing the secretion of IFN-γ, TNF-α, and IL-6. Anti-Mouse Galectin-9 Antibody (RG9-1) can increase CD8 T cell and Treg frequency. Anti-Mouse Galectin-9 Antibody (RG9-1) reduces graft survival time by increasing CD4⁺ and CD8⁺ T cell infiltration. Anti-Mouse Galectin-9 Antibody (RG9-1) can be used for researches on inflammation conditions, cancer and xenotransplantation such as ischemia-reperfusion, colon cancer, breast cancer and leukemia.

GB1908 is a selective and orally active galectin-1 inhibitor with K_i values of 57 nM and 72 nM for human and mouse galectin-1, respectively. GB1908 displays >50-fold selectivity over galectin-3. GB1908 can be used for the study of lung cancer.

Anti-Mouse/Human Mac-2/Galectin-3 Antibody (TIB-166) is a rat-derived anti-mouse/human Mac-2/Galectin-3 IgG2a monoclonal antibody. Anti-Mouse/Human Mac-2/Galectin-3 Antibody (TIB-166) significantly inhibits IL-6 expression (inhibition rates 34.7% and 55.3%). Anti-Mouse/Human Mac-2/Galectin-3 Antibody (TIB-166) is often used for immunoprecipitation, western blot, immunofluorescence, and flow cytometry.

Galectin-8N-IN-1 (compound 19a) is a potent and selective galectin-8N inhibitor with a K_d value of 1.8 μM. Galectin-8N-IN-1 is a galectin-8N ligand. Galectin-8N-IN-1 can be used in research of immune system.

Galectin-3/galectin-8-IN-1 (Compound 53) is a dual Galectin-3 and galectin-8 C-terminal domain inhibitor, with K_d values of 4.12 μM and 6.04 μM respectively. Galectin-3/galectin-8-IN-1 inhibits the MRC-5 lung fibroblast cells migration. Galectin-3/galectin-8-IN-1 can be used for research of cancer and tissue fibrosis.

GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (K_D = 0.036 μM) and mouse galectin-3 (K_D = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research.

Thiobis-β-Galactose-propyne is an effective multivalent galectin-3 (Gal-3) inhibitor. Galectin-3 is involved in many metabolism processes related to cancer. Galectin-3-IN-1 is a click chemistry reagent. It contains an alkyne group that can undergo a copper-catalyzed azide-alkyne cycloaddition (CuAAc) reaction with molecules that have an azide group.

DB21, Galectin-1 Antagonist is a dibenzofuran conjugated peptidomimetic that acts as an allosteric inhibitor of galectin-1 (GAL1)binding to cell surface glycans. DB21, Galectin-1 Antagonis increases inhibition of angiogenesis and tumour growth in melanoma, lung adenocarcinoma and ovarian cancer models.

PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC₅₀ of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease.