TMEM216 Inhibitors
Chemical inhibitors of TMEM216 can act through various mechanisms to disrupt its function, primarily revolving around the role of TMEM216 in ciliogenesis and the maintenance of primary cilia. Cyclopamine and Jervine are steroidal alkaloids that inhibit the Hedgehog signaling pathway, which is essential for the formation and function of primary cilia, thereby indirectly inhibiting TMEM216. Similarly, SANT-1 also targets the Hedgehog signaling pathway by directly inhibiting Smoothened, a critical component of this pathway, leading to a downstream effect on the proper functioning of TMEM216. Purmorphamine, although typically an activator of the Hedgehog pathway, can indirectly lead to TMEM216 inhibition when downstream elements of the pathway are blocked, resulting in an accumulation of intermediates that interfere with primary cilia formation involving TMEM216.
Other chemicals interfere with cellular processes that are crucial for the proper localization and function of TMEM216 within cilia. For instance, Forskolin raises cAMP levels, which can lead to alterations in ciliary assembly or function, thus indirectly affecting TMEM216. Ciliobrevin D specifically targets dynein, a motor protein necessary for ciliary function, and its inhibition can compromise the role of TMEM216 in ciliary transport. In a similar manner, Brefeldin A disrupts vesicular trafficking and Golgi apparatus function, pivotal for the trafficking of TMEM216 to cilia. Microtubule integrity, crucial for ciliogenesis, is targeted by Mebendazole and Nocodazole, which destabilize or depolymerize microtubules, respectively, thereby indirectly inhibiting the function of TMEM216. Azadirachtin also affects microtubule dynamics, thus indirectly inhibiting TMEM216 by impacting the cellular infrastructure required for its role in cilia. Lastly, cell cycle inhibitors like Roscovitine and Alsterpaullone disrupt the timing and formation of primary cilia, which are processes that TMEM216 is involved in, leading to an indirect inhibition of its ciliary function.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Cyclopamine | 4449-51-8 | sc-200929 sc-200929A | 1 mg 5 mg | $92.00 $204.00 | 19 | |
Cyclopamine is a steroidal alkaloid inhibitor of the Hedgehog (Hh) signaling pathway, which indirectly inhibits TMEM216 by blocking the pathway required for ciliogenesis, a process that TMEM216 is involved in. Disruption of the Hh pathway leads to the functional inhibition of TMEM216 by preventing its role in the formation and function of primary cilia. | ||||||
Purmorphamine | 483367-10-8 | sc-202785 sc-202785A | 1 mg 5 mg | $56.00 $180.00 | 18 | |
Purmorphamine is a small molecule that activates the Hedgehog signaling pathway, but when used in a specific context where downstream effectors are blocked, it can lead to the accumulation of pathway intermediates that indirectly inhibit primary cilia formation involving TMEM216. | ||||||
Jervine | 469-59-0 | sc-200934 sc-200934A | 1 mg 5 mg | $66.00 $240.00 | 1 | |
Jervine is an inhibitor of the Hedgehog signaling pathway, which can lead to a decrease in primary cilia formation, a cellular process that TMEM216 is directly involved in. By specifically inhibiting this pathway, Jervine leads to functional inhibition of TMEM216's role in ciliogenesis. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin activates adenylate cyclase, increasing cAMP levels. Elevated cAMP can alter the assembly and function of primary cilia where TMEM216 is localized, indirectly leading to its functional inhibition by disrupting the ciliary processes that TMEM216 is known to be involved in. | ||||||
Ciliobrevin D | 1370554-01-0 | sc-507482 | 10 mg | $413.00 | ||
Ciliobrevin D is a specific inhibitor of dynein, which is crucial for cilia formation and function. By inhibiting dynein, Ciliobrevin D indirectly inhibits TMEM216 by disrupting its role in ciliary transport, a key process for the normal function of primary cilia where TMEM216 is localized. | ||||||
Roscovitine | 186692-46-6 | sc-24002 sc-24002A | 1 mg 5 mg | $92.00 $260.00 | 42 | |
Roscovitine is a cyclin-dependent kinase inhibitor that can disrupt the cell cycle. Since TMEM216 is involved in ciliogenesis, which is closely tied to the cell cycle, Roscovitine indirectly inhibits the function of TMEM216 by affecting the timing and formation of primary cilia. | ||||||
SANT-1 | 304909-07-7 | sc-203253 | 5 mg | $132.00 | 5 | |
SANT-1 directly inhibits Smoothened, a component of the Hedgehog signaling pathway. By inhibiting Smoothened, SANT-1 indirectly inhibits TMEM216 by preventing the signaling required for the formation of primary cilia, thus impacting the functional role of TMEM216 in ciliogenesis. | ||||||
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 disrupts Golgi apparatus function and vesicular trafficking, which is essential for the trafficking and localization of proteins to primary cilia. TMEM216, being involved in ciliary function, is indirectly inhibited by Brefeldin A due to the disruption of its correct localization to the cilia. | ||||||
Mebendazole | 31431-39-7 | sc-204798 sc-204798A | 5 g 25 g | $45.00 $87.00 | 2 | |
Mebendazole, a microtubule-disrupting agent, can indirectly inhibit TMEM216 by destabilizing microtubules, which form the structural backbone of cilia. Since TMEM216 is associated with the ciliary structure, its function is indirectly inhibited when microtubule integrity is compromised. | ||||||
Azadirachtin | 11141-17-6 | sc-257105 sc-257105A sc-257105B sc-257105C sc-257105D | 1 mg 5 mg 10 mg 25 mg 50 mg | $174.00 $367.00 $614.00 $979.00 $1693.00 | ||
Azadirachtin impacts the cell cycle and can disrupt microtubule organization. Given that TMEM216 is essential for ciliogenesis, which relies on proper microtubule assembly, Azadirachtin can indirectly inhibit TMEM216 by affecting the microtubule dynamics required for its function in ciliary maintenance and assembly. | ||||||