Name | 4-[(6-nitroquinolin-4-yl)amino]-N-[4-(pyridin-4-ylamino)phenyl]benzamide |
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Synonyms | hms2860i06 |
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)[1]. |
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Related Catalog | |
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]. |
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: Wild-type C57BL/6 six to eight week old mice[1] Dosage: 25 or 50 mg/kg Administration: Intraperitoneal injection (Dissolved in DMSO at 25 and 50 mg/ml then further diluted with PEG400 to create 5 and 10 mg/ml stocks for injection) Result: Caused a robust and statistically significant increase the ratio of cleaved/intact FGF23 at the tested 25 and 50 mg/kg concentrations. |
References |
Density | 1.431g/cm3 |
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Boiling Point | 662.7ºC at 760mmHg |
Molecular Formula | C27H20N6O3 |
Molecular Weight | 476.48600 |
Flash Point | 354.6ºC |
Exact Mass | 476.16000 |
PSA | 124.76000 |
LogP | 7.01970 |
Index of Refraction | 1.783 |