TM6SF1 Inhibitors
TM6SF1 inhibitors encompass a range of chemical compounds that interfere with the functional activity of TM6SF1 by targeting the pathways and processes it is involved in. Bafilomycin A1 and U18666A directly impact the intracellular trafficking and cholesterol distribution, respectively, both critical to TM6SF1's role in cholesterol homeostasis. By disrupting endosomal acidification and causing intracellular cholesterol accumulation, these inhibitors hinder the regulation and transport functions of TM6SF1. Similarly, GW4869 and Filipin III alter the composition of lipid rafts by affecting sphingomyelin-ceramide conversion and cholesterol binding, impeding the TM6SF1-mediated signaling crucial forcholesterol efflux. PD98059 and LY294002, on the other hand, exert their inhibitory effects by interfering with upstream signaling pathways. The MEK inhibitor PD98059 diminishes ERK/MAPK signaling, which is modulated by TM6SF1, while LY294002, as a PI3K inhibitor, disrupts the PI3K/Akt pathway, affecting TM6SF1-associated cellular survival and cholesterol metabolism processes.
Furthermore, compounds like MβCD, Progesterone, Simvastatin, Chlorpromazine, Nystatin, and Genistein indirectly inhibit TM6SF1 through modulation of cholesterol levels and membrane integrity or by inhibiting key kinases. MβCD depletes membrane cholesterol, vital for TM6SF1 activity, while Progesterone and Simvastatin modify cholesterol synthesis and bioavailability, crucial for TM6SF1's function in cholesterol metabolism. Chlorpromazine and Nystatin disrupt membrane composition, influencing the cholesterol-dependent activity of TM6SF1, and Genistein suppresses tyrosine kinase-mediated signaling pathways that could be essential for TM6SF1's regulatory functions. Collectively, these inhibitors elucidate the multifaceted approach required to attenuate the functional activity of TM6SF1, highlighting the protein's intricate involvement in cholesterol regulation and cell signaling.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Bafilomycin A1 | 88899-55-2 | sc-201550 sc-201550A sc-201550B sc-201550C | 100 µg 1 mg 5 mg 10 mg | $98.00 $255.00 $765.00 $1457.00 | 280 | |
Bafilomycin A1 is a specific inhibitor of the vacuolar-type H+-ATPase. By inhibiting this ATPase, the compound disrupts endosomal acidification, which is crucial for the intracellular trafficking and function of TM6SF1, as TM6SF1 is implicated in the regulation of cholesterol homeostasis and trafficking to the plasma membrane. | ||||||
U 18666A | 3039-71-2 | sc-203306 sc-203306A | 10 mg 50 mg | $143.00 $510.00 | 2 | |
U18666A is a cholesterol transport inhibitor that can cause intracellular accumulation of cholesterol in the late endosomes and lysosomes. This effect can indirectly inhibit the functional activity of TM6SF1 by disrupting the cholesterol distribution and homeostasis that TM6SF1 regulates. | ||||||
GW4869 | 6823-69-4 | sc-218578 sc-218578A | 5 mg 25 mg | $203.00 $611.00 | 24 | |
GW4869 is a neutral sphingomyelinase inhibitor. It prevents the conversion of sphingomyelin to ceramide, thus affecting lipid raft composition and potentially the lipid microenvironments where TM6SF1 is active, leading to an inhibition of TM6SF1-mediated signaling involved in cholesterol efflux. | ||||||
Filipin III | 480-49-9 | sc-205323 sc-205323A | 500 µg 1 mg | $118.00 $148.00 | 26 | |
Filipin III is a polyene macrolide that binds to cholesterol, disrupting lipid rafts in cell membranes. This binding can inhibit the function of TM6SF1 by altering the cholesterol-rich domains necessary for its proper localization and function. | ||||||
PD 98059 | 167869-21-8 | sc-3532 sc-3532A | 1 mg 5 mg | $40.00 $92.00 | 212 | |
PD98059 is a MEK inhibitor that indirectly affects the ERK/MAPK signaling pathway. Since TM6SF1 has been shown to modulate MAPK activation, inhibition of this pathway can lead to a decrease in TM6SF1-mediated signaling and functional activity. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor that impedes the PI3K/Akt signaling pathway. The inhibition of this pathway can decrease the functional activity of TM6SF1, given that TM6SF1-associated processes are interlinked with the PI3K/Akt pathway through its involvement in cholesterol metabolism and cell survival. | ||||||
Methyl-β-cyclodextrin | 128446-36-6 | sc-215379A sc-215379 sc-215379C sc-215379B | 100 mg 1 g 10 g 5 g | $20.00 $48.00 $160.00 $82.00 | 19 | |
MβCD is a cholesterol-depleting agent that extracts cholesterol from the plasma membrane. This can inhibit TM6SF1 function by depleting the cholesterol necessary for its activity, as TM6SF1 is involved in cholesterol regulation and efflux. | ||||||
Progesterone | 57-83-0 | sc-296138A sc-296138 sc-296138B | 1 g 5 g 50 g | $20.00 $52.00 $298.00 | 3 | |
Progesterone is known to regulate cholesterol synthesis. By altering cholesterol synthesis and potentially the intracellular cholesterol pool, progesterone can indirectly inhibit TM6SF1 through disruption of the cholesterol homeostasis that TM6SF1 is involved in maintaining. | ||||||
Simvastatin | 79902-63-9 | sc-200829 sc-200829A sc-200829B sc-200829C | 50 mg 250 mg 1 g 5 g | $31.00 $89.00 $135.00 $443.00 | 13 | |
Simvastatin is an HMG-CoA reductase inhibitor that reduces cholesterol biosynthesis. This reduction can inhibit TM6SF1 function by decreasing the availability of cholesterol, which is essential for TM6SF1's role in cholesterol metabolism and transport. | ||||||
Chlorpromazine | 50-53-3 | sc-357313 sc-357313A | 5 g 25 g | $61.00 $110.00 | 21 | |
Chlorpromazine is known to affect the distribution and function of cholesterol. Its action can lead to an alteration in the plasma membrane composition, potentially inhibiting the function of TM6SF1 due to its dependency on cholesterol-rich microdomains. | ||||||