TMEM206 Inhibitors
Chemical inhibitors of TMEM206 can exert their effects through various mechanisms that influence the channel's ability to conduct chloride ions across cellular membranes. Tetrodotoxin, for instance, is known for its ability to bind to and block voltage-gated sodium channels. This blockage can reduce cellular excitability, which in turn can decrease the activity of chloride channels due to a reduced overall cellular activity, thus influencing TMEM206. Zinc ions utilize a different approach; they act as non-selective inhibitors of ion channels, including chloride channels. The binding of zinc to TMEM206 or its vicinity can lead to a conformational change that interferes with the ion flow, thereby inhibiting the channel's activity. Similarly, chloroquine exerts its effect by raising endosomal pH, which can affect TMEM206 by altering the intracellular pH and thereby inhibiting the channel's proton-activated chloride conduction.
Other chemicals interact with TMEM206 more directly. DCPIB, which is primarily an inhibitor of volume-regulated anion channels, may inhibit TMEM206 by altering chloride ion flux in a manner analogous to its action on VRACs. Niflumic acid and flufenamic acid, both known blockers of chloride channels, could inhibit TMEM206 by binding to the channel or altering its gating mechanism, thus preventing chloride ion flow. DIDS, a covalent inhibitor of anion transport, can inhibit TMEM206 by binding to lysine residues near the channel pore, blocking the transport of chloride ions. Mefloquine, while primarily used for other purposes, can also block various ion channels, suggesting that it may inhibit TMEM206 by altering the channel conformation or the electrochemical gradient. Verapamil, although a calcium channel blocker, may influence TMEM206 indirectly by modifying intracellular calcium levels, which could affect calcium-sensitive chloride channels. Cadmium chloride could inhibit TMEM206 by interacting with the protein or by modifying the calcium signaling pathways. Ethacrynic acid, a diuretic affecting sodium, potassium, and chloride cotransport, could inhibit TMEM206 by interfering with the chloride transport mechanism or altering the chloride ion concentration gradient. Lastly, tolfenamic acid, which is known to block chloride channels, could inhibit TMEM206 by interfering with channel gating or ion transport mechanisms.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Zinc | 7440-66-6 | sc-213177 | 100 g | $47.00 | ||
Zinc ions can act as non-selective inhibitors of various ion channels. Given that TMEM206 is an ion channel, zinc can bind to the protein or its vicinity, leading to a conformational change or interference with the ion flow, resulting in inhibition of its chloride channel activity. | ||||||
Chloroquine | 54-05-7 | sc-507304 | 250 mg | $68.00 | 2 | |
Chloroquine is known to raise endosomal pH and, by altering the intracellular pH, can inhibit the activity of pH-sensitive ion channels like TMEM206. | ||||||
Niflumic acid | 4394-00-7 | sc-204820 | 5 g | $31.00 | 3 | |
Niflumic acid is a known blocker of several members of the chloride channel family. It could potentially inhibit TMEM206 by binding to the channel or modulating its gating mechanism, thus preventing the flow of chloride ions. | ||||||
Flufenamic acid | 530-78-9 | sc-205699 sc-205699A sc-205699B sc-205699C | 10 g 50 g 100 g 250 g | $26.00 $77.00 $151.00 $303.00 | 1 | |
Flufenamic acid is a member of the fenamate group of nonsteroidal anti-inflammatory drugs, and it is known to block chloride channels. It could inhibit TMEM206 by altering its conformation, thereby preventing chloride ion transport through the channel. | ||||||
Mefloquine Hydrochloride | 51773-92-3 | sc-211784 | 100 mg | $116.00 | 4 | |
Mefloquine is an antimalarial drug that can block gap junctions and has been shown to inhibit various ion channels. It could inhibit TMEM206 by a similar mechanism of ion channel blockage, possibly by altering channel conformation or the electrochemical gradient necessary for channel function. | ||||||
Verapamil | 52-53-9 | sc-507373 | 1 g | $367.00 | ||
Verapamil, a calcium channel blocker, may inhibit TMEM206 indirectly by altering the intracellular calcium concentration, which in turn can affect calcium-sensitive chloride channels and potentially inhibit TMEM206 activity by changing the cellular conditions required for its activation. | ||||||
Cadmium chloride, anhydrous | 10108-64-2 | sc-252533 sc-252533A sc-252533B | 10 g 50 g 500 g | $55.00 $179.00 $345.00 | 1 | |
Cadmium ions can inhibit various calcium-permeable channels. Even though TMEM206 is a chloride channel, cadmium could inhibit it by binding to the protein or indirectly by modifying the calcium signaling that could be essential for the regulation of TMEM206 activity. | ||||||
Ethacrynic acid | 58-54-8 | sc-257424 sc-257424A | 1 g 5 g | $49.00 $229.00 | 5 | |
Ethacrynic acid is a loop diuretic that inhibits the cotransport of sodium, potassium, and chloride ions. As a chloride channel inhibitor, it could potentially inhibit TMEM206 by interacting with the chloride transport mechanism or altering the chloride ion concentration gradient across the cell membrane, which is necessary for TMEM206 function. | ||||||
Tolfenamic Acid | 13710-19-5 | sc-204918 sc-204918A | 5 g 25 g | $69.00 $312.00 | ||
Fenamates are a class of nonsteroidal anti-inflammatory drugs that block chloride channels. Although the CAS number provided is for tolfenamic acid, which is a specific member of the fenamate class, fenamates in general can inhibit TMEM206 by a similar mechanism of chloride channel blockage, potentially by interfering with the channel gating or ion transport mechanism. | ||||||