TMEM186 Inhibitors
Chemical inhibitors of TMEM186 can function through various molecular pathways to decrease its activity. For instance, PD 0332991 operates by impeding the function of CDK4/6, leading to a halt in the cell cycle at the G1 phase, which in turn can reduce the proliferation of cells where TMEM186 is active. Similarly, Omipalisib and LY294002 target the PI3K/mTOR signaling pathway; Omipalisib achieves this by simultaneously inhibiting PI3K and mTOR, while LY294002 specifically inhibits PI3K. This results in the diminution of AKT phosphorylation and activity, which can decrease TMEM186 activity if it relies on this pathway for cellular survival. U0126 intervenes by inhibiting MEK1/2, which is a precursor to ERK in the MAPK/ERK pathway, a pathway involved with cell cycle regulation and differentiation. Consequently, this can lead to a reduction in ERK activity, potentially diminishing TMEM186 activity associated with cell cycle control.
Additional compounds such as Rapamycin and AZD8055 also play a role in modulating TMEM186 activity by targeting mTOR, albeit through different mechanisms. Rapamycin specifically inhibits mTOR, which is central to the PI3K/AKT/mTOR pathway, while AZD8055 inhibits both mTORC1 and mTORC2 complexes within the same pathway. This inhibition can reduce cell growth and proliferation, which can affect TMEM186 activity. Sorafenib and Gefitinib take a different approach by targeting tyrosine protein kinases; Sorafenib inhibits the RAF/MEK/ERK pathway, and Gefitinib inhibits the EGFR tyrosine kinase. Erlotinib, similar to Gefitinib, inhibits the EGFR tyrosine kinase, leading to reduced downstream signaling. This can decrease the activity of pathways required for TMEM186's function. SP600125 and PD98059 focus on the MAPK signaling pathways, with SP600125 inhibiting JNK and PD98059 inhibiting MEK, which can lead to reduced TMEM186 activity if it interacts with these pathways. Lastly, Y-27632 inhibits ROCK, affecting cell motility and cytoskeletal arrangements, which can also influence TMEM186 activity if it is associated with these cellular processes.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Palbociclib | 571190-30-2 | sc-507366 | 50 mg | $321.00 | ||
Palbociclib inhibits CDK4/6, which are crucial for cell cycle progression. Inhibition of CDK4/6 leads to cell cycle arrest at G1 phase, which can inhibit TMEM186 activity by reducing the cellular proliferation where TMEM186 might play a role. | ||||||
GSK2126458 | 1086062-66-9 | sc-364503 sc-364503A | 2 mg 10 mg | $265.00 $1050.00 | ||
Omipalisib inhibits PI3K/mTOR signaling pathway. This pathway is involved in many cellular processes including growth and survival. By inhibiting PI3K/mTOR, Omipalisib can reduce the signaling that may be necessary for TMEM186's function in cell survival. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor. PI3K is part of the AKT/mTOR pathway which is implicated in cellular proliferation and survival. Inhibition of PI3K can decrease AKT phosphorylation and activity, which may be necessary for TMEM186's function. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $64.00 $246.00 | 136 | |
U0126 inhibits MEK1/2, which is upstream of ERK in the MAPK/ERK pathway. This pathway is involved in cell cycle regulation and differentiation. Inhibition of MEK1/2 can result in decreased ERK activity, possibly reducing TMEM186 activity related to cell cycle control. | ||||||
Rapamycin | 53123-88-9 | sc-3504 sc-3504A sc-3504B | 1 mg 5 mg 25 mg | $63.00 $158.00 $326.00 | 233 | |
Rapamycin inhibits mTOR, a central component of the PI3K/AKT/mTOR pathway. By inhibiting mTOR, Rapamycin can decrease cell growth and proliferation, which can inhibit the function of TMEM186 if its activity is linked to these processes. | ||||||
Sorafenib | 284461-73-0 | sc-220125 sc-220125A sc-220125B | 5 mg 50 mg 500 mg | $57.00 $100.00 $250.00 | 129 | |
Sorafenib targets multiple tyrosine protein kinases, and through this, it can inhibit the RAF/MEK/ERK pathway. Inhibition of this pathway can lead to reduced cell proliferation and angiogenesis, which can inhibit TMEM186 activity if it's associated with these pathways. | ||||||
Gefitinib | 184475-35-2 | sc-202166 sc-202166A sc-202166B sc-202166C | 100 mg 250 mg 1 g 5 g | $63.00 $114.00 $218.00 $349.00 | 74 | |
Gefitinib inhibits EGFR tyrosine kinase, which is part of the EGFR signaling pathway. This pathway is implicated in cell proliferation and survival. Inhibiting EGFR can result in reduced signaling required for TMEM186's associated functions. | ||||||
Erlotinib, Free Base | 183321-74-6 | sc-396113 sc-396113A sc-396113B sc-396113C sc-396113D | 500 mg 1 g 5 g 10 g 100 g | $87.00 $135.00 $293.00 $505.00 $3827.00 | 42 | |
Erlotinib is another EGFR tyrosine kinase inhibitor, leading to inhibition of the EGFR signaling pathway. This can decrease the activity of downstream signaling pathways that may be necessary for the function of TMEM186. | ||||||
SP600125 | 129-56-6 | sc-200635 sc-200635A | 10 mg 50 mg | $40.00 $150.00 | 257 | |
SP600125 inhibits JNK, which is part of the MAPK signaling pathways involved in apoptosis and cell proliferation. Inhibiting JNK can decrease TMEM186 activity if it interacts with this pathway for its function. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD98059 is a MEK inhibitor, which can inhibit the MAPK/ERK pathway. By inhibiting this pathway, PD98059 can reduce the activity of the downstream components that might be required for TMEM186's function in cell cycle regulation. | ||||||