VPS8 inhibitors encompass a range of chemical compounds that impede the functional activity of VPS8 through distinct mechanisms involving key cellular pathways and processes. Bafilomycin A1 and Chloroquine both target the acidification of vesicles, specifically disrupting VPS8's role in endosomal-lysosomal trafficking by altering the pH within these organelles, essential for their maturation and function. Similarly, Monensin, as an ionophore, compromises VPS8 activity by disturbing the proton gradient and pH of lysosomes. Dynasore and Pitstop 2 hinder clathrin-mediated endocytosis, thereby reducing the substrate availability for lysosomal delivery and indirectly limiting VPS8's function within the HOPS complex. Wortmannin and YM201636 disrupt the generation of phosphoinositide pools and inhibit PI3K activity, respectively, leading to impaired endosome formation and maturation, which are crucial for VPS8's role in endosomal-lysosomal fusion processes.
Furthermore, U 18666A's interference with cholesterol transport perturbs the trafficking and fusion functionality of lysosomes, indirectly curtailing VPS8's activity. Genistein's inhibition of tyrosine kinase signaling pathways has repercussions on endosomal trafficking, consequently diminishing VPS8's involvement in lysosomal fusion. Microtubule destabilization by Nocodazole affects intracellular transport, thus indirectly inhibiting VPS8 by impeding vesicular trafficking to lysosomes. 5-(N-Ethyl-N-isopropyl)-Amiloride affects endosomal pH regulation and macropinocytosis, processes that are foundational to VPS8's role in endocytic trafficking. Lastly, Latrunculin A's disruption of actin polymerization hampers cytoskeletal dynamics, which are essential for the vesicular trafficking pathways that VPS8 facilitates. Collectively, these inhibitors exert their effects through modulation of various biochemical pathways, ultimately leading to the decreased functional activity of VPS8.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bafilomycin A1 | 88899-55-2 | sc-201550 sc-201550A sc-201550B sc-201550C | 100 µg 1 mg 5 mg 10 mg | $98.00 $255.00 $765.00 $1457.00 | 280 | |
Bafilomycin A1 is a specific inhibitor of the V0 subunit of V-ATPases, which are critical for vesicle acidification. By inhibiting V-ATPase activity, it disrupts endosomal-lysosomal trafficking, a process that VPS8 is known to be involved in, thereby diminishing VPS8 function by preventing the proper acidification of endosomal compartments. | ||||||
Dynamin Inhibitor I, Dynasore | 304448-55-3 | sc-202592 | 10 mg | $89.00 | 44 | |
Dynasore is a small molecule inhibitor of the GTPase activity of dynamin, which is essential for clathrin-mediated endocytosis. Since VPS8 is part of the HOPS complex involved in trafficking to the lysosome, inhibition of endocytosis by Dynasore indirectly inhibits VPS8 function by reducing the substrate availability for lysosomal delivery. | ||||||
Monensin A | 17090-79-8 | sc-362032 sc-362032A | 5 mg 25 mg | $155.00 $525.00 | ||
Monensin is an ionophore that disrupts the proton gradient across lysosomal membranes. By altering lysosomal pH, Monensin affects the trafficking and fusion processes of lysosomes, where VPS8 is functionally important, leading to a diminished role of VPS8 in these processes. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $69.00 | 2 | |
Chloroquine is known to impair the acidification of endosomes and lysosomes, which is a critical step in the maturation of these organelles. This impairment would indirectly inhibit VPS8 function by disrupting the endosomal-lysosomal pathway that VPS8 is involved in. | ||||||
YM201636 | 371942-69-7 | sc-204193 | 5 mg | $217.00 | 6 | |
YM201636 is an inhibitor of phosphatidylinositol 4-kinase IIIβ (PI4KB), which affects the generation of phosphatidylinositol 4-phosphate (PI4P) on Golgi and endosomal membranes. Since VPS8 is implicated in endosomal membrane trafficking, the reduction of PI4P pools by YM201636 indirectly diminishes VPS8’s role in these trafficking events. | ||||||
Pitstop 2 | 1419320-73-2 | sc-507418 | 10 mg | $360.00 | ||
Pitstop 2 is an inhibitor of clathrin-mediated endocytosis by blocking the interaction between clathrin and adaptor proteins. As VPS8 is involved in the subsequent trafficking of endocytosed materials to lysosomes, Pitstop 2 indirectly inhibits VPS8 function by reducing the endocytic flow of cargo to the lysosome. | ||||||
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $67.00 $223.00 $425.00 | 97 | |
Wortmannin is an irreversible inhibitor of phosphoinositide 3-kinases (PI3K), which are involved in early endosome formation. Inhibiting PI3K activity leads to reduced endosome maturation and trafficking, indirectly diminishing VPS8 function since it is part of the HOPS complex responsible for endosomal-lysosomal fusion. | ||||||
U 18666A | 3039-71-2 | sc-203306 sc-203306A | 10 mg 50 mg | $143.00 $510.00 | 2 | |
U 18666A is a cholesterol transport inhibitor that can induce the accumulation of cholesterol in late endosomes and lysosomes, disrupting their function and trafficking. This would indirectly inhibit VPS8 function by altering the trafficking and fusion processes of lysosomes, where VPS8 plays a role. | ||||||
Genistein | 446-72-0 | sc-3515 sc-3515A sc-3515B sc-3515C sc-3515D sc-3515E sc-3515F | 100 mg 500 mg 1 g 5 g 10 g 25 g 100 g | $45.00 $164.00 $200.00 $402.00 $575.00 $981.00 $2031.00 | 46 | |
Genistein is a tyrosine kinase inhibitor that can indirectly affect endosomal trafficking by modulating signaling pathways involved in this process. By doing so, Genistein may diminish VPS8 function as it is involved in the trafficking and fusion of endosomes with lysosomes. | ||||||
Nocodazole | 31430-18-9 | sc-3518B sc-3518 sc-3518C sc-3518A | 5 mg 10 mg 25 mg 50 mg | $59.00 $85.00 $143.00 $247.00 | 38 | |
Nocodazole is a microtubule destabilizer that affects intracellular transport mechanisms, including the trafficking of vesicles to the lysosome. By disrupting microtubule dynamics, Nocodazole can indirectly inhibit VPS8 function as VPS8 is involved in lysosomal trafficking. | ||||||