| Cas No.: | 50440-30-7 |
| Chemical Name: | Benzamide,4-[(6-nitro-4-quinolinyl)amino]-N-[4-(4-pyridinylamino)phenyl]- |
| Synonyms: | Benzamide,4-[(6-nitro-4-quinolinyl)amino]-N-[4-(4-pyridinylamino)phenyl]-;4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide;HMS2860I06 |
| SMILES: | [N+](C1=CC=C2C(C(NC3C=CC(C(NC4C=CC(NC5C=CN=CC=5)=CC=4)=O)=CC=3)=CC=N2)=C1)([O-])=O |
| Formula: | C27H20N6O3 |
| M.Wt: | 476.4861 |
| Purity: | >98% |
| Sotrage: | 0°C (short term), -20°C (long term), desiccated |
| Description: | 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 Vivo: | T3Inh-1 (25 or 50 mg/kg; i.p.) blocks ppGalNAc-T3-mediated glycan-masking of FGF23 thereby increasing its cleavage[1]. |
| 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[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]. |
| References: | [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. |

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