PP2A-δ Activators
PP2A-δ Activators are a diverse set of chemical compounds that enhance the activity of the protein phosphatase through various mechanisms. Fostriecin, for instance, augments PP2A-δ activity by preferentially inhibiting other phosphatases, thereby reducing substrate competition. Similarly, Cantharidin and NorcanthPP2A-δ Activators encompass a range of chemical compounds that specifically enhance the phosphatase function of PP2A-δ by modulating its activity and substrate availability. Starting with Fostriecin, which selectively inhibits other phosphatases, it increases PP2A-δ activity by reducing substrate competition. Cantharidin, at certain concentrations, preferentially binds to other phosphatases, which indirectly boosts the activity of PP2A-δ, and this mechanism is also observed with Norcantharidin, albeit with reduced toxicity. Okadaic Acid, in low concentrations, acts similarly by shifting the enzymatic activity balance in favor of PP2A-δ. The allosteric modulation by (-)-P-Bromolevamisole and the specific dose-dependent actions of Endothall and Calyculin A further enhance PP2A-δ activity either by altering subunit interactions or by preferentially inhibiting other phosphatases like PP1. Tautomycin's differential binding affinities also play a role in selectively enhancing PP2A-δ activity.
The activity of PP2A-δ is intricately linked to the phosphatase activity equilibrium within the cell, and the activators work by subtly shifting this balance. Microcystin-LR, in sub-inhibitory concentrations, indirectly up-regulates PP2A-δ by affecting this balance. Ceramide enhances PP2A-δ through its role in sphingolipid signaling pathways, which may alter the PP2A subunit composition favoring PP2A-δ. Forskolin elevates cAMP levels and through PKA-dependent phosphorylation reduces the inhibition of PP2A-δ by other proteins. Lastly, Arachidonic Acid, by integrating into cellular membranes, affects the regulatory subunits of PP2A, which can lead to increased PP2A-δ activity. Together, these compounds contribute to the fine-tuning of PP2A-δ activity, crucial for its role in cellular signaling and homeostasis.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Fostriecin | 87860-39-7 | sc-202160 | 50 µg | $265.00 | 9 | |
Fostriecin selectively inhibits Protein Phosphatase 2A (PP2A) over PP1, leading to the enhanced phosphatase activity of PP2A-δ by reducing competition for substrate phosphoproteins. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin acts as an inhibitor of PP1 and PP2A, but at specific concentrations, it can selectively activate PP2A-δ by preferential binding to other phosphatases, indirectly increasing the availability of PP2A-δ for dephosphorylation processes. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Okadaic Acid is a potent inhibitor of Protein Phosphatases 1 and 2A; however, at lower concentrations, it can serve as an activator for PP2A-δ by subtly shifting the balance of phosphatase activity in favor of PP2A-δ. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $49.00 $203.00 | 1 | |
Endothall disrupts PP1 and PP2A activity but has been shown to selectively enhance PP2A-δ activity at specific doses by preferential inhibition of PP1, thereby indirectly promoting PP2A-δ activity. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Calyculin A, like okadaic acid, is a potent inhibitor of PP1 and PP2A, but at low nanomolar concentrations, can preferentially activate PP2A-δ by differentially affecting its subunit interactions and substrate specificity. | ||||||
Tunicamycin | 11089-65-9 | sc-3506A sc-3506 | 5 mg 10 mg | $172.00 $305.00 | 66 | |
Tautomycin targets PP1 and PP2A, but differential binding affinities can lead to an increase in PP2A-δ activity under certain conditions by reducing competitive inhibition. | ||||||
Norcantharidin | 29745-04-8 | sc-280719 | 5 g | $113.00 | 2 | |
Norcantharidin is a demethylated analog of cantharidin with less toxicity. It can enhance PP2A-δ activity by selectively modulating the PP2A family of proteins, potentially through competitive binding interactions. | ||||||
C2 Ceramide | 3102-57-6 | sc-201375 sc-201375A | 5 mg 25 mg | $124.00 $460.00 | 12 | |
Ceramide can indirectly enhance PP2A-δ activity by participating in sphingolipid signaling pathways that lead to the alteration of PP2A subunit composition and increase in PP2A-δ activity. | ||||||
Arachidonic Acid (20:4, n-6) | 506-32-1 | sc-200770 sc-200770A sc-200770B | 100 mg 1 g 25 g | $92.00 $240.00 $4328.00 | 9 | |
Arachidonic Acid can modulate PP2A-δ activity by integrating into cellular membranes and affecting the membrane-associated regulatory subunits of PP2A, potentially increasing PP2A-δ activity. | ||||||