Galectin-3 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.

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.

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.

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.

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.

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.

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.

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.

(2S)-Selvigaltin is the S-enantiomer of Selvigaltin (HY-147041). Selvigaltin is an orally active galectin-3 (Gal-3) inhibitor.

GB1490 is an orally active galectin inhibitor with K_d values of 0.4 μM and 2.7 μM for galectin-1 and galectin-3, respectively.

Galectin-4-IN-3 (Compound 11) is a Galectin 4C inhibitor, with a K_d of 160 μM.

Dual Galectin-3/EGFR-IN-1 (Compound 29) is the dual inhibitor for Galectin-3 and EGFR with the K_D of 52.29 μM and 3.31 μM. Dual Galectin-3/EGFR-IN-1 inhibits TGF-β-induced hepatic stellate cell (HSCs) activation, induces apoptosis in LX-2 cell, and exhibits anti-liver fibrotic efficacy.

Galectin-3-IN-7 is a selective Galectin-3 inhibitor with a K_d of 5.7 nM and shows 390-fold selectivity over Gal-1. Galectin-3-IN-7 can downregulate profibrotic signaling such as ACTA2, COL1A2, and FN1 in TGFβ-stimulated LX2 hepatic stellate cells. Galectin-3-IN-7 can be used for the research of fibrosis.

Galectin-3-IN-4 (compound 5) is a carboxamide analog. Galectin-3-IN-4 is a potent, selective, and orally bioavailable inhibitor of human and mouse galectin-3, with IC₅₀ values of 21 and 167 nM for hGal-3 and mGal-3, respectively. Galectin-3-IN-4 has IC₅₀ values of 1580 and 2750 nM for hGal-1 and hGal-9, respectively.

Galectin-3-IN-2 (Compound 9) is a potent multivalent inhibitor of galectin-3 (Gal-3; IC₅₀=8.3 μM). Galectin-3 participates in many cancer-related metabolic processes.

Galectin-3-IN-6 is a human and murine galectin-3 (Gal-3) inhibitor, with an IC₅₀ of 12 nM against human galectin-3, an IC₅₀ of 12.6 nM against mutant murine galectin-3 (V160A), and a K_d of 13 nM for human galectin-3, as well as oral bioavailability. Galectin-3-IN-6 reduces the levels of liver fibrosis markers type I collagen and α-smooth muscle actin in mouse models of acute liver injury and fibrosis. Galectin-3-IN-6 can be used for the research of acute liver injury and fibrosis.

CHI3L1-IN-6 (Compound 9e) is a CHI3L1 inhibitor with a K_d of 19.11 μM for hCHI3L1. CHI3L1-IN-6 blocks CHI3L1-Galectin-3 interaction. CHI3L1-IN-6 reduces STAT3 signaling. CHI3L1-IN-6 exhibits anti-cancer activity against glioblastoma.