| Bioactivity | 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)[1]. | ||||||||||||
| Invitro | 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[1]. T3Inh-1 exhibits no toxicity and did not affect HEK cell proliferation[1].T3Inh-1 (HEK cells; 6 hours)increases cleavage of FGF23[1]. | ||||||||||||
| In Vivo | T3Inh-1 (25 or 50 mg/kg; i.p.) blocks ppGalNAc-T3-mediated glycan-masking of FGF23 thereby increasing its cleavage[1]. Animal Model: | ||||||||||||
| Name | T3Inh-1 | ||||||||||||
| CAS | 50440-30-7 | ||||||||||||
| Formula | C27H20N6O3 | ||||||||||||
| Molar Mass | 476.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Song L, et al. Inhibitor of ppGalNAc-T3-mediated O-glycosylation blocks cancer cell invasiveness and lowers FGF23 levels. Elife. 2017;6:e24051. Published 2017 Mar 31. |