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 Vera (African Green Monkey Kidney epithelial) cultures reveal that selective blockage of GBF1 function by GCA (100 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.
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Product information
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Form
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Off-white solid
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Molar mass
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284.3
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Protect from Light
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Yes
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Packaged under inert gas
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Yes
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Purity
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≥95% by HPLC
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Solubility
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DMSO
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Chemical formula
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C17H14F2N2
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Store and ship information
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Storage
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+2°C to +8°C
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Ship
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Ambient Temperature Only
Standard Handling
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