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.
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.
Phase 2 Clinical
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