ATP9B Inhibitors
ATP9B inhibitors can act by modulating calcium homeostasis, glycosylation, and protein transport within cells, and by disrupting lipid metabolism and transport. Thapsigargin, a SERCA pump inhibitor, disrupts calcium homeostasis in the endoplasmic reticulum, leading to an increase in cytosolic calcium levels which can impact ATP9B's phospholipid translocation activity. Tunicamycin, an inhibitor of N-linked glycosylation, and Brefeldin A, which inhibits protein transport from the endoplasmic reticulum to the Golgi apparatus, could alter ATP9B's glycosylation state and localization, respectively, thereby affecting its function. Ionophores like Monensin and Nigericin disrupt ion gradients across cell membranes, which could interfere with ATP9B's phospholipid-transporting activity.
In addition, ATP9B can be indirectly inhibited by chemicals that disrupt lipid metabolism and signaling. Wortmannin and LY294002, both inhibitors of phosphoinositide 3-kinases (PI3K), deplete PIP2 and PIP3 lipids which might be substrates for ATP9B. Consequently, the availability of these lipids could be a determining factor in ATP9B activity. U73122, a phospholipase C inhibitor, prevents the formation of IP3 and DAG from PIP2, which might alter the substrate availability for ATP9B, thereby inhibiting its function.
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| 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 a SERCA pump inhibitor. By inhibiting the SERCA pump, it disrupts the calcium homeostasis in the endoplasmic reticulum leading to an increase in cytosolic calcium levels. This could impact ATP9B as it is involved in phospholipid translocation that is sensitive to calcium levels. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $169.00 $299.00 | 66 | |
Tunicamycin inhibits N-linked glycosylation in the ER. This could affect ATP9B as it is a transmembrane protein and its function might be influenced by its glycosylation state. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $30.00 $52.00 $122.00 $367.00 | 25 | |
Brefeldin A inhibits protein transport from the endoplasmic reticulum to the Golgi apparatus. Given that ATP9B is a transmembrane protein, it could disrupt its proper localization and function. | ||||||
Monensin A | 17090-79-8 | sc-362032 sc-362032A | 5 mg 25 mg | $152.00 $515.00 | ||
Monensin is an ionophore that equalizes the concentration of sodium ions inside and outside of cells. This disrupts many cellular processes, including lipid metabolism and transport, which could interfere with ATP9B's phospholipid-transporting activity. | ||||||
Nigericin sodium salt | 28643-80-3 | sc-201518A sc-201518 sc-201518B sc-201518C sc-201518D | 1 mg 5 mg 25 mg 1 g 5 g | $45.00 $110.00 $235.00 $6940.00 $26879.00 | 9 | |
Nigericin is a potassium ionophore that disrupts proton and potassium gradients across membranes. This disruption could affect ATP9B's activity, as the protein's function in phospholipid transport may be dependent on maintaining these ion gradients. | ||||||
Cyclosporin A | 59865-13-3 | sc-3503 sc-3503-CW sc-3503A sc-3503B sc-3503C sc-3503D | 100 mg 100 mg 500 mg 10 g 25 g 100 g | $62.00 $90.00 $299.00 $475.00 $1015.00 $2099.00 | 69 | |
Cyclosporin A inhibits the function of the phosphatase calcineurin, which could disrupt calcium signaling pathways. This could indirectly affect ATP9B, as its phospholipid-transporting activity might be influenced by calcium levels. | ||||||
2-APB | 524-95-8 | sc-201487 sc-201487A | 20 mg 100 mg | $27.00 $52.00 | 37 | |
2-APB is a modulator of IP3 receptors and inhibits IP3-mediated calcium release. This could influence ATP9B's activity by altering calcium signaling, which may be involved in ATP9B's function. | ||||||
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 potent and irreversible inhibitor of phosphoinositide 3-kinases (PI3K). Given that PIP2 and PIP3 lipids might be substrates for ATP9B, the depletion of these lipids could inhibit ATP9B activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $121.00 $392.00 | 148 | |
LY294002 is a PI3K inhibitor. Similar to Wortmannin, the inhibition of PI3K and subsequent depletion of its lipid products could impact ATP9B's phospholipid-transporting activity. | ||||||
Progesterone | 57-83-0 | sc-296138A sc-296138 sc-296138B | 1 g 5 g 50 g | $20.00 $51.00 $292.00 | 3 | |
Progesterone at high concentrations can inhibit the scramblase activity, which might impact the function of ATP9B as it is thought to have scramblase activity. | ||||||