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LLS30 is a potent, allosteric Galectin-1 (Gal-1) inhibitor, inhibits AR negative cells PC3, DU145, and AR positive cells, 22RV1 and CWR-R1 cells with IC50 of 10.4 μM, 5.3 μM, 3.3 μM and 5.9 μM, respectively; decreases Gal-1 binding affinity to its binding partners; showes in vivo efficacy in both AR positive and AR negative xenograft models; not only can potentiate the anti-tumor effect of docetaxel to cause complete regression of tumors, but also effectively inhibit the invasion and metastasis of PCa cells in vivo.




OTX008 (Calixarene 0118, PTX-008) is a calixarene derivative designed to bind the Galectin-1 (Gal1) amphipathic β-sheet conformation; inhibits Gal1 expression and ERK1/2 and AKT-dependent survival pathways, and induces G2/M cell cycle arrest through CDK1; inhibits proliferation and invasion at micromolar concentrations in cancer cells; inhibits growth of A2780-1A9 xenografts in vivo.

Solid Tumors

Phase 1 Clinical




TD-139 (TD139) is a highly potent, selecitve inhibitor of Galectin-3 (Gal-3) carbohydrate binding domain with Ki of 14 nM; reduces TGF-β1-induced β-catenin translocation to the nucleus, blocks β-catenin phosphorylation in vitro and in vivo; attenuates the late-stage progression of lung fibrosis in murine models; attenuates liver injury and milder infiltration of IFNγ- and IL-17- and -4-producing CD4(+) T cells, increases IL-10-producing CD4(+) T cells and F4/80(+) CD206(+) alternatively activated macrophages and prevents the apoptosis of liver-infiltrating MNCs in WT C57BL/6 mice.

Cystic Fibrosis

Phase 2 Clinical



1978336-61-6 GB1107 (GB-1107, GB 1107) is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with Kd of 37 nM (human Galectin-3); displays >100-fold lower affinity for most of the tested human galectins, and 20 and 4-fold lower affinity for galectin-2 and the C-terminal CRD of galectin-4, respectively; prevents human lung adenocarcinoma growth in vivo, increases tumor M1 macrophage polarization and CD8+ T cell infiltration; GB1107 also can potentiate the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules.


2138366-93-3 LLS2 is a novel potent Galectin-1 (Gal1) inhibitor that decreases membrane-associated H-Ras and K-Ras and contributed to the suppression of pErk pathway; kills SKOV3, HT29, PC3, XPA3, MCF7, and A549 with an IC50 of 11.7, 24.5, 28.2, 20.9, 23.2 and 34.3 uM respectively; exhibits synergistic activity against several human cancer cell lines, significantly inhibits the growth of ovarian cancer xenografts in athymic mice combined with paclitaxel.

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