TMEM165 Inhibitors
Chemical inhibitors of TMEM165 can disrupt its function in various ways, mainly by interfering with the environment of the Golgi apparatus where TMEM165 operates. Benzyl isothiocyanate, for instance, can inactivate TMEM165 through the modification of its cysteine residues, which are pivotal for the protein's functionality in glycosylation. E64d, although typically an inhibitor of cysteine proteases, can irreversibly modify the essential cysteine residues within TMEM165, thus compromising its role in maintaining the Golgi pH critical for glycosylation. Other chemicals, like Swainsonine and Tunicamycin, can indirectly affect TMEM165 by inhibiting enzymes involved in glycosylation processes. Swainsonine inhibits mannosidase II, affecting the maturation of glycoproteins, while Tunicamycin prevents the first step in N-linked glycosylation, potentially causing a buildup of glycoproteins that TMEM165 would normally help process.
Further disrupting the Golgi's microenvironment essential for TMEM165's function are chemicals that affect ionic gradients and pH levels. Brefeldin A disrupts the Golgi structure by inhibiting vesicle trafficking, indirectly impacting TMEM165. Monensin, an ionophore, and Concanamycin A, a V-ATPase inhibitor, can alter the pH and ionic gradients, which TMEM165 is known to help regulate. Calcium homeostasis is another critical factor for TMEM165's function, and chemicals such as Niflumic acid, Niguldipine, KB-R7943, Thapsigargin, Ruthenium Red, 2-Aminoethoxydiphenyl borate, Verapamil, Diltiazem, Cyclopiazonic acid, Nifedipine, and SKF-96365 can disrupt this balance. For example, Niflumic acid inhibits chloride channels, potentially affecting TMEM165's ability to maintain Golgi pH, while Niguldipine and KB-R7943 block calcium channels or alter calcium exchange, respectively, which could disturb the calcium-dependent processes TMEM165 is involved in regulating. Thapsigargin, by inhibiting SERCA pumps, and other calcium channel blockers like Verapamil and Diltiazem can indirectly inhibit TMEM165 by disrupting the Ca2+ homeostasis, essential for its role in glycosylation within the Golgi apparatus.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $94.00 $349.00 | 114 | |
Thapsigargin is an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca2+-ATPase (SERCA). By disrupting Ca2+ homeostasis, thapsigargin may cause indirect inhibition of TMEM165, as TMEM165 is involved in regulating Ca2+ levels critical for its function in the Golgi. | ||||||
Ruthenium red | 11103-72-3 | sc-202328 sc-202328A | 500 mg 1 g | $184.00 $245.00 | 13 | |
Ruthenium Red is a polycationic dye that can inhibit calcium channels and calcium-dependent processes. It could indirectly inhibit TMEM165 by disrupting intracellular calcium levels, which are essential for TMEM165's role in glycosylation within the Golgi. | ||||||
2-APB | 524-95-8 | sc-201487 sc-201487A | 20 mg 100 mg | $27.00 $52.00 | 37 | |
2-Aminoethoxydiphenyl borate (2-APB) is a modulator of inositol 1,4,5-trisphosphate receptors and store-operated channels. By interfering with Ca2+ signaling, 2-APB may indirectly inhibit TMEM165's function in regulating Golgi Ca2+ levels for proper glycosylation. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $367.00 | ||
Verapamil is a calcium channel blocker that may indirectly inhibit TMEM165 by altering Ca2+ homeostasis in the Golgi, potentially disrupting the environment that TMEM165 is involved in maintaining for proper glycosylation. | ||||||
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 V-ATPases. Since V-ATPases are involved in acidifying organelles like the Golgi, inhibition of these enzymes could indirectly inhibit TMEM165 by disrupting the pH gradient, affecting its function in glycosylation. | ||||||
Diltiazem | 42399-41-7 | sc-204726 sc-204726A | 1 g 5 g | $209.00 $464.00 | 4 | |
Diltiazem, another calcium channel blocker, could indirectly inhibit TMEM165 by impacting Ca2+ homeostasis within the Golgi, thereby potentially disrupting the Ca2+-dependent processes that TMEM165 regulates. | ||||||
Cyclopiazonic Acid | 18172-33-3 | sc-201510 sc-201510A | 10 mg 50 mg | $173.00 $612.00 | 3 | |
Cyclopiazonic acid is an inhibitor of SERCA pumps. By disturbing Ca2+ storage and signaling, this compound could indirectly inhibit TMEM165 by altering the Ca2+ balance within the Golgi that TMEM165 is known to regulate. | ||||||
Nifedipine | 21829-25-4 | sc-3589 sc-3589A | 1 g 5 g | $58.00 $170.00 | 15 | |
Nifedipine is a blocker of L-type calcium channels. Its role in reducing Ca2+ influx could indirectly inhibit TMEM165's function by altering the Ca2+ homeostasis within the Golgi, which is crucial for TMEM165's role in glycosylation. | ||||||
SK&F 96365 | 130495-35-1 | sc-201475 sc-201475B sc-201475A sc-201475C | 5 mg 10 mg 25 mg 50 mg | $101.00 $155.00 $389.00 $643.00 | 2 | |
SKF-96365 is an inhibitor of receptor-mediated calcium entry and store-operated calcium entry. By inhibiting these calcium channels, SKF-96365 may indirectly inhibit TMEM165 by disrupting the Ca2+ homeostasis in the Golgi, thus affecting TMEM165's glycosylation role. | ||||||