| Identification | Back Directory | [Name]
Benzamide,4-[(6-nitro-4-quinolinyl)amino]-N-[4-(4-pyridinylamino)phenyl]- | [CAS]
50440-30-7 | [Synonyms]
T3Inh-1
Benzamide,4-[(6-nitro-4-quinolinyl)amino]-N-[4-(4-pyridinylamino)phenyl]-
50440-30-7 Benzamide,4-[(6-nitro-4-quinolinyl)amino]-N-[4-(4-pyridinylamino)phenyl]-
T3Inh1,T3Inh 1,inhibit,O-glycosylation,Inhibitor,T-3Inh-1,ppGalNAc-T3,breast cancer cells,FGF23,T3Inh-1,invasion | [Molecular Formula]
C27H20N6O3 | [MOL File]
50440-30-7.mol | [Molecular Weight]
476.49 |
| Chemical Properties | Back Directory | [Boiling point ]
662.7±55.0 °C(Predicted) | [density ]
1.431±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 31.25 mg/mL (65.58 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
13.21±0.70(Predicted) | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Uses]
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]. | [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.
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| [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. DOI:10.7554/eLife.24051 |
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