Description
Endosidin-2 (1839524-44-5) binds to the EXO70 subunit of the exocyst complex which results in inhibition of exocytosis and endosomal recycling in both plant and human cells and enhancement of plant vacuolar trafficking. EXO70 is a component of the octameric exocyst complex which tethers post-Golgi vesicles to the plasma membrane before SNARE- mediated membrane fusion.2?Endosidin-2 was previously identified as a plant endomembrane trafficking disruptor.3?Inhibits intracellular glucose transporter, GLUT4 trafficking to the membrane and impairs glucose uptake in response to insulin.4?It is a valuable new tool for the study of exocytosis.
Uses
Endosidin 2 binds to the EXO70 (exocyst component of 70 kDa) subunit of the exocyst complex, resulting in inhibition of exocytosis and endosomal recycling in both plant and human cells and enhancement of plant vacuolar trafficking. A valuable tool for exocytosis studies.
Biochem/physiol Actions
Endosidin2 is a cell-permeable benzylidene-benzohydrazide based compound that binds to the exocyst component of 70 kDa (EXO70) subunit of exocyst complex (Kd?= 253 μM for interaction with EXO70A1) and reduces exocytosis and endosomal recycling in plant and mammalian cells. Displays good aqueous stability. Endosidin2 has shown to disrupt the trafficking of proteins between the plasma membrane and endosome, which leads to enhanced trafficking to the vacuole for degradation. It is reported to inhibit the recycling of endocytosed transferrin to plasma membrane in HeLa cells, and can target multiple isoforms of EXO70 in mammals, resulting in misregulation of exocytosis.
References
1) Zhang?et al. (2016),?Endosidin2 targets conserved exocyst complex subunit EXO70 to inhibit exocytosis;? Proc. Natl. Acad. Sci. USA,?113?E41
2) Novick?et al. (1980),?Identification of 23 complementation groups required for post-translational events in the yeast secretory pathway;? Cell,?21?205
3) Drakakaki?et al. (2011),?Clusters of bioactive compounds target dynamic endomembrane networks in vivo;? Proc. Natl. Acad. Sci. USA,?108?17850
4) Fujimoto?et al.?(2019),?The Exocyst Complex Regulates Insulin-Stimulated Glucose Uptake of Skeletal Muscle Cells; Am. J. Physiol. Endocrinol. Metab.?317(6)?E957
