Exo-1, Vesicular trafficking inhibitor
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(2 Publications)
MW 273.26 Da, Purity >99%. Cell-permeable, reversible inhibitor of vesicular trafficking between endoplasmic reticulum and the Golgi apparatus. Inhibits exocytosis with an IC50 of approx. 20 μM. Rapidly releases Arf1 from Golgi membranes. Has similar mechanism of action to brefeldin A (ab120299).
View Alternative Names
CP2D6_HUMAN, CPD6, CYP2D, CYP2D7AP, CYP2D7BP, CYP2D7P2, CYP2D8P2, CYP2DL1, CYPIID6, Cholesterol 25-hydroxylase, Cytochrome P450 2D6, Cytochrome P450 family 2 subfamily D member 6, Cytochrome P450 family 2 subfamily D polypeptide 6, Cytochrome P450-DB1, Debrisoquine 4-hydroxylase, Microsomal monooxygenase, P450 DB1, P450C2D, Xenobiotic monooxygenase, flavoprotein-linked monooxygenase
- ICC/IF
Unknown
Immunocytochemistry/ Immunofluorescence - Exo-1, Vesicular trafficking inhibitor (AB120292)
ab86071 staining GBF1 in HeLa cells treated with Exo-1 (ab120292), by ICC/IF. Increase in GBF1 expression correlates with increased concentration of Exo-1 as described in literature.
The cells were incubated at 37°C for 5 minutes in media containing different concentrations of ab120292 ( Exo-1) in DMSO, fixed with 4% formaldehyde for 10 minutes at room temperature and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab86071 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
- Chemical Structure
Lab
Chemical Structure - Exo-1, Vesicular trafficking inhibitor (AB120292)
2D chemical structure image of ab120292, Exo-1, Vesicular trafficking inhibitor
Properties and storage information
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Storage information
Supplementary information
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Biological function summary
Enzymes related to drug metabolism perform essential roles in the detoxification of foreign chemicals. CYP2D6 is notably part of the microsomal enzyme complex in the liver. It facilitates the transformation of lipophilic compounds into more water-soluble metabolites rendering them easier for the body to excrete. This enzyme affects the bioavailability and efficacy of many medications such as antidepressants antipsychotics and beta-blockers. Its role is integral in the activation of certain prodrugs converting them into their active pharmacological forms.
Pathways
CYP2D6 functions significantly in drug metabolism and clearance pathways. It takes part in the Phase I metabolism pathway where it initiates the oxidation of drugs setting the stage for further modifications. It interacts closely with other CYP enzymes like CYP3A4 which sometimes share substrates and inhibitors affecting their metabolic activities. CYP2D6's interaction with these pathways emphasizes its involvement in the intricate network of enzyme-mediated drug handling in the body.
Publications (2)
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Nature communications 9:4126 PubMed30297691
2018
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Unspecified reactive species
The Journal of neuroscience : the official journal 38:5399-5414 PubMed29760175
2018
Applications
Unspecified application
Species
Unspecified reactive species
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