T3Inh-1 is a potent and selective inhibitor of ppGalNAc-T3 (IC50=7 μM). T3Inh-1 reduces FGF23 hormone levels in both tissue cells and mice, without causing any toxic side effects. T3Inh-1 also prevents breast cancer cells. The enzyme ppGalNAc-T3 is implicated in at least two medically important pathways: cancer metastasis and stabilization of FGF23 (regulates phosphate levels in the bloodstream).In Vitro:T3Inh-1 (5 μM; 24-48 hours; 5 μM; MDA-MB231 cells) is strikingly effective, inhibiting migration by >80% and invasion by 98% while causing no discernable effect on cell proliferation.
T3Inh-1 exhibits no toxicity and did not affect HEK cell proliferation.
T3Inh-1 (HEK cells; 6 hours)increases cleavage of FGF23.In Vivo:T3Inh-1 (25 or 50 mg/kg; i.p.) blocks ppGalNAc-T3-mediated glycan-masking of FGF23 thereby increasing its cleavage.