SGSM3 Inhibitors
Chemical inhibitors of SGSM3 include a range of compounds that disrupt the protein's function by targeting various elements of the cellular pathways it's involved in, particularly endocytic trafficking and related signaling. Wortmannin and LY294002 inhibit SGSM3 by impairing the PI3K signaling pathway, which is fundamental for endocytic processes that SGSM3 is part of. These inhibitors prevent PI3K from fulfilling its role in the generation of phosphatidylinositol (3,4,5)-trisphosphate (PIP3), a lipid second messenger crucial for the initiation of endosomal formation and trafficking, leading to a disruption of SGSM3's functional role in these processes. Dynasore and MiTMAB target the GTPase dynamin, which is essential for the scission of clathrin-coated vesicles from the plasma membrane, a step in which SGSM3 is implicated. The inhibition of dynamin by these chemicals results in the impairment of endocytic vesicle recycling, thereby functionally inhibiting SGSM3.
Furthermore, Pitstop 2 acts by selectively inhibiting clathrin, a protein that forms a polyhedral lattice around vesicles during endocytosis, thereby preventing the formation of endocytic vesicles where SGSM3 operates. Endosidin 2 disrupts endosomal trafficking by targeting ARF-GEF proteins, which are regulators of vesicle formation and trafficking; this disruption leads to an inhibition of SGSM3 by impairing the protein's ability to mediate endosome dynamics. Bafilomycin A1 and Concanamycin A inhibit the vacuolar-type H+-ATPase (V-ATPase), essential for endosomal acidification, a process that SGSM3 relies on for sorting cargo within endosomes. Monensin, an ionophore, disrupts ion gradients critical for SGSM3's function in endosomal sorting, while Ionomycin alters intracellular calcium levels, therefore disturbing calcium-dependent signaling pathways crucial for SGSM3's role. Finally, Tyrphostin AG 879 and Genistein inhibit tyrosine kinases that regulate endocytic pathways, leading to the functional inhibition of SGSM3 through the impairment of tyrosine kinase-dependent signaling pathways that control endosomal sorting and trafficking.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Wortmannin | 19545-26-7 | sc-3505 sc-3505A sc-3505B | 1 mg 5 mg 20 mg | $66.00 $219.00 $417.00 | 97 | |
Wortmannin is a specific inhibitor of phosphoinositide 3-kinases (PI3Ks). Since SGSM3 is involved in the endosomal trafficking pathways, which are regulated by PI3K signaling, wortmannin can inhibit SGSM3 by impeding the PI3K-dependent trafficking routes necessary for SGSM3's function. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is another inhibitor of PI3K. By inhibiting PI3K, LY294002 impairs the endosomal trafficking, which is essential for SGSM3 activity, leading to functional inhibition of SGSM3 through disruption of its cellular context. | ||||||
Dynamin Inhibitor I, Dynasore | 304448-55-3 | sc-202592 | 10 mg | $87.00 | 44 | |
Dynasore is a non-competitive inhibitor of dynamin, a GTPase that SGSM3 interacts with during clathrin-mediated endocytosis. Inhibition of dynamin by dynasore will disrupt the recycling of endosomes, thereby inhibiting the function of SGSM3 in endosomal sorting. | ||||||
Pitstop 2 | 1419093-54-1 | sc-507418 | 10 mg | $360.00 | ||
Pitstop 2 is a selective clathrin inhibitor. Since SGSM3 operates in the clathrin-mediated endocytic pathway, inhibition of clathrin by Pitstop 2 results in the functional inhibition of SGSM3 by disrupting endocytic vesicle formation. | ||||||
Bafilomycin A1 | 88899-55-2 | sc-201550 sc-201550A sc-201550B sc-201550C | 100 µg 1 mg 5 mg 10 mg | $96.00 $250.00 $750.00 $1428.00 | 280 | |
Bafilomycin A1 is a specific inhibitor of the vacuolar-type H+-ATPase (V-ATPase). As SGSM3 is implicated in endosomal acidification processes, inhibition of V-ATPase by Bafilomycin A1 can inhibit SGSM3 by preventing the acidification required for its function in endosomal sorting. | ||||||
Monensin A | 17090-79-8 | sc-362032 sc-362032A | 5 mg 25 mg | $152.00 $515.00 | ||
Monensin is an ionophore that disrupts intracellular ion gradients. SGSM3's role in endosomal sorting is dependent on proper ion homeostasis, and thus disruption by Monensin leads to inhibition of SGSM3 function. | ||||||
Concanamycin A | 80890-47-7 | sc-202111 sc-202111A sc-202111B sc-202111C | 50 µg 200 µg 1 mg 5 mg | $65.00 $162.00 $650.00 $2550.00 | 109 | |
Concanamycin A, similar to Bafilomycin A1, is a V-ATPase inhibitor. It inhibits SGSM3 by hindering endosomal acidification, which is critical for SGSM3's role in trafficking. | ||||||
Ionomycin, free acid | 56092-81-0 | sc-263405 sc-263405A | 1 mg 5 mg | $94.00 $259.00 | 2 | |
Ionomycin is a calcium ionophore that alters intracellular calcium levels. As calcium signaling is vital for endocytic pathways, Ionomycin's alteration of calcium homeostasis can inhibit SGSM3 by disrupting calcium-dependent sorting within endosomes. | ||||||
Tyrphostin AG 879 | 148741-30-4 | sc-3557 sc-3557A | 5 mg 25 mg | $83.00 $328.00 | 4 | |
Tyrphostin AG 879 is an inhibitor of tyrosine kinases, which can regulate endocytic pathways. By inhibiting these kinases, Tyrphostin AG 879 indirectly inhibits SGSM3 by disrupting downstream signaling required for SGSM3's endosomal sorting function. | ||||||
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 | $26.00 $92.00 $120.00 $310.00 $500.00 $908.00 $1821.00 | 46 | |
Genistein is a tyrosine kinase inhibitor that can also affect endocytic pathways. Inhibition of tyrosine kinases by Genistein leads to functional inhibition of SGSM3 by impairing the signaling pathways that control endosomal sorting where SGSM3 is involved. | ||||||