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6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
- русский язык имя
- английское имя6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
- CAS №1139889-93-2
- CBNumberCB12518793
- ФормулаC17H14F2N2
- мольный вес284.3
- файл Mol1139889-93-2.mol
химическое свойство
температура хранения | Store at RT |
растворимость | insoluble in H2O; ≥12.95 mg/mL in DMSO; ≥2.27 mg/mL in EtOH with ultrasonic |
форма | Off-white solid |
цвет | White to off-white |
Справочник по базе данных CAS | 1139889-93-2 |
6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline химические свойства, назначение, производство
Общее описание
A cell-permeable quinoline compound that selectively targets ArfGEF GBF1, but not BIG1/2, and attenuates GBF1-mediated cellular vesicle traffickings in a reversible manner. Phenotypic comparisons in Vero (African Green Monkey Kidney epithelial) cultures reveal that selective blockage of GBF1 function by GCA (10 μM) or by FGB1-E794K dominant-inactive expression affects medial- and cis-Golgi similarly to that seen with BFA (Cat. No. 203729), however, the non-GBF1-specific BFA (10 μg/ml or 35.6 μM) causes additional GBF1-independent morphologic effects on TGN, notably the rapid dispersal of Golgi-associated coat proteins AP-1 and GGA3, which are not seen with GCA treatment. Endocytic/retrograde transport studies using GCA establishes that GBF1 function is not required for the transport of bacterial toxins to the endosomes, however the retrograde transport of StxB (shiga toxin B subunit) from endosomes to TGN and Golgi is GBF1-dependent (100% inhibition of StxB sulfation at 10 μM), accounting for GCA′s (10 μM) ability to completely prevent Vera cells from Stx-induced (up to 100 ng/ml) inhibition of cellular protein synthesis.6,8-Difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline поставщик
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