Galectin-1 Inhibitor

OTX008 is a selective inhibitor of galectin-1.

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.

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.

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.

Apoptosis inducer 8 (Compound 7c) is a galectin-1 (gal-1) mediated apoptosis-inducing agent against global major leading lung cancer burden. Apoptosis inducer 8 significantly reduced the gal-1 protein level. Apoptosis inducer 8 is also a PET imaging agent.

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.