PAR-6 Activators
PAR-6 Activators are a diverse set of chemical compounds that indirectly enhance the activity of PAR-6, a pivotal protein in the regulation of cell polarity. Among these, Phorbol 12-myristate 13-acetate (PMA) serves as a potent PKC activator, which subsequently phosphorylates and activates PAR-6, bolstering its role in the formation of polarity complexes. Similarly, Forskolin, by escalating intracellular cAMP levels, activates PKA which may phosphorylate proteins that interact with PAR-6, thereby facilitating PAR-6's engagement in cell polarity. The GSK-3β inhibitor, 1-Azakenpaullone, may enhance PAR-6 signaling by preventing the phosphorylation of PAR-6's negative regulators. Y-27632, a ROCK inhibitor, and LY294002, a PI3K inhibitor, both function to dampen competing pathways, thereby indirectly potentiating PAR-6's involvement in cell adhesion and polarity. NSC 23766 curtails Rac1 activation, potentially stabilizing the PAR-6 complex, crucial for cell polarity maintenance. Sphingosine-1-phosphate and Thapsigargin, through lipid signaling and calcium mobilization, respectively, enhance the pathways that necessitate PAR-6's role in cell morphology and cytoskeletal organization.
Furthermore, the MEK inhibitor U0126 may indirectly facilitate PAR-6 function by altering the balance of intracellular signaling in favor of pathways that activate PAR-6. Go 6983, while generally inhibiting PKC, may preferentially support PAR-6 activity by selectively targeting specific PKC isoforms that negatively regulate cell polarity. Staurosporine, known for its broad kinase inhibition, can, at precise dosages, selectively inhibit kinases that otherwise suppress PAR-6 function, thereby indirectly promoting PAR-6's role in polarity. Finally, Bisindolylmaleimide I, by inhibiting negative regulatory PKC isoforms, may result in an upsurge in PAR-6 activity, underscoring the complexity and specificity of how these activators can converge on the pivotal cell polarity regulator PAR-6. Collectively, these compounds provide a framework for understanding the diverse mechanisms that can be leveraged to enhance PAR-6 activity without necessarily increasing its expression or direct activation.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
PMA | 16561-29-8 | sc-3576 sc-3576A sc-3576B sc-3576C sc-3576D | 1 mg 5 mg 10 mg 25 mg 100 mg | $41.00 $132.00 $214.00 $500.00 $948.00 | 119 | |
PMA is a diester of phorbol and is known to activate protein kinase C (PKC) which interacts with PAR-6 in establishing cell polarity. Activation of PKC can lead to the phosphorylation of PAR-6, enhancing its ability to participate in polarity complexes. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $78.00 $153.00 $740.00 $1413.00 $2091.00 | 73 | |
Forskolin activates adenylyl cyclase, increasing cAMP levels, which in turn activates PKA. PKA can phosphorylate various proteins including those that may interact with PAR-6, thus indirectly enhancing the function of PAR-6 in the regulation of cell polarity. | ||||||
SRPIN 340 | 218156-96-8 | sc-394310 | 10 mg | $226.00 | 1 | |
1-Azakenpaullone is a known GSK-3β inhibitor. Inhibition of GSK-3β can prevent the phosphorylation of proteins that compete or negatively interact with PAR-6, thus potentially enhancing PAR-6 mediated signaling related to cell polarity. | ||||||
Y-27632, free base | 146986-50-7 | sc-3536 sc-3536A | 5 mg 50 mg | $186.00 $707.00 | 88 | |
Y-27632 is a ROCK inhibitor that can increase cell-cell adhesion by decreasing phosphorylation levels of myosin light chain. Since PAR-6 is involved in cell adhesion and polarity, inhibition of ROCK can enhance the function of PAR-6 indirectly. | ||||||
LY 294002 | 154447-36-6 | sc-201426 sc-201426A | 5 mg 25 mg | $123.00 $400.00 | 148 | |
LY294002 is a PI3K inhibitor. By inhibiting PI3K, it may reduce the competitive pathways that negatively regulate PAR-6, thus indirectly enhancing the function of PAR-6 in cell polarity and junction formation. | ||||||
NSC 23766 | 733767-34-5 | sc-204823 sc-204823A | 10 mg 50 mg | $151.00 $609.00 | 75 | |
NSC 23766 inhibits Rac1-GEF interaction, which can lead to a decrease in active Rac1. Since PAR-6 forms a complex with Rac1, inhibition of its activation could enhance the stability and function of the PAR-6 complex in cell polarity. | ||||||
D-erythro-Sphingosine-1-phosphate | 26993-30-6 | sc-201383 sc-201383D sc-201383A sc-201383B sc-201383C | 1 mg 2 mg 5 mg 10 mg 25 mg | $165.00 $322.00 $570.00 $907.00 $1727.00 | 7 | |
Sphingosine-1-phosphate is a lipid signaling molecule that activates G-protein coupled receptors and can lead to actin cytoskeletal rearrangements, which is a process where PAR-6 is involved. This can enhance the function of PAR-6 in cell morphology. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin is a SERCA pump inhibitor leading to increased intracellular calcium levels. Elevated calcium can activate signaling pathways that involve PAR-6, thereby potentially enhancing PAR-6's role in cell polarity and cytoskeletal organization. | ||||||
U-0126 | 109511-58-2 | sc-222395 sc-222395A | 1 mg 5 mg | $64.00 $246.00 | 136 | |
U0126 is a MEK inhibitor, and by inhibiting MEK, it may shift the equilibrium of intracellular signaling pathways to favor those that activate PAR-6, thereby indirectly enhancing PAR-6's function in cell polarity. | ||||||
Gö 6983 | 133053-19-7 | sc-203432 sc-203432A sc-203432B | 1 mg 5 mg 10 mg | $105.00 $299.00 $474.00 | 15 | |
Go 6983 is a PKC inhibitor but has been shown to have selective effects on different PKC isoforms. By selectively inhibiting certain PKC isoforms, it could potentially enhance the activity of PAR-6 in its role in establishing cell polarity. | ||||||