PP2C Inhibitors
Chemical inhibitors of protein phosphatase 2C (PP2C) act through various mechanisms to inhibit the activity of this enzyme. Okadaic Acid, Calyculin A, and Tautomycin, for instance, are known to exert their inhibitory effects by binding competitively to the active site of PP2C, thereby preventing the access of natural substrates. Their action mimics that of PP2C's physiological substrates, which allows them to effectively block the catalytic activity necessary for the dephosphorylation process. Similarly, Cantharidin and its derivative, Norcantharidin, inhibit PP2C by occupying the active site, a key region for enzyme-substrate interactions. This binding prevents the enzyme from performing its dephosphorylation function, which is crucial for its biological role in cells.
Endothall and Fostriecin also inhibit PP2C, but they do so by mimicking the transition state of phosphate ester hydrolysis. This mimicry creates a steric hindrance at the active site, which disrupts the normal activity of PP2C. Microcystin-LR takes a different approach by binding irreversibly to the active site, leading to permanent inactivation of the enzyme. This binding is particularly effective because it not only prevents substrate access but also locks the enzyme in an inactive form. Other inhibitors, such as Phenothiazine, exert an indirect effect on PP2C by interfering with mitochondrial functions, which in turn affects the energy status of the cell and the availability of ATP, a molecule required for PP2C's activity. Sanguinarine affects PP2C indirectly by disrupting cellular signaling pathways through DNA intercalation, which can lead to downregulation of PP2C activity. Cerulenin alters lipid metabolism, which can affect membrane dynamics and signaling pathways involving PP2C. Lastly, Brefeldin A causes broad disruptions in cellular trafficking and signaling pathways by affecting the structure and function of the Golgi apparatus, which can lead to a decrease in PP2C function.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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, particularly PP1 and PP2A, and through competitive inhibition, it can inhibit PP2C activity due to the structural similarities and overlap in substrate specificities among these phosphatases. | ||||||
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 strong inhibitor of protein phosphatases PP1 and PP2A, and it is likely to inhibit PP2C by competing with natural substrates for the active site due to shared properties among these phosphatases. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin is a known inhibitor of serine/threonine protein phosphatases and can inhibit PP2C activity by binding to the active site, which prevents substrate access and dephosphorylation processes. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $49.00 $203.00 | 1 | |
Endothall displays inhibitory action against protein phosphatases by mimicking the transition state of phosphate ester hydrolysis, thereby inhibiting PP2C through steric hindrance and competition at the active site. | ||||||
Fostriecin | 87860-39-7 | sc-202160 | 50 µg | $265.00 | 9 | |
Fostriecin selectively inhibits PP2A and PP4, but it can also inhibit PP2C by binding to its active site, preventing the dephosphorylation process that is critical to the protein's function. | ||||||
Norcantharidin | 29745-04-8 | sc-280719 | 5 g | $113.00 | 2 | |
Norcantharidin, a demethylated analog of cantharidin, inhibits serine/threonine protein phosphatases and can inhibit PP2C by binding to the active site, thus blocking substrate access. | ||||||
Phenothiazine | 92-84-2 | sc-250686 sc-250686A | 50 g 250 g | $23.00 $44.00 | ||
Phenothiazine is known to inhibit PP2C indirectly by interfering with the electron transport chain in mitochondria, leading to altered cellular energy states and reducing the availability of ATP required for PP2C's phosphatase activity. | ||||||
Sanguinarium | 2447-54-3 | sc-473396 | 10 mg | $220.00 | ||
Sanguinarium is a benzophenanthridine alkaloid that can inhibit PP2C by intercalating into the DNA, leading to the disruption of cellular signaling pathways that ultimately reduce PP2C activity. | ||||||
Cerulenin (synthetic) | 17397-89-6 | sc-200827 sc-200827A sc-200827B | 5 mg 10 mg 50 mg | $161.00 $312.00 $1210.00 | 9 | |
Cerulenin, an inhibitor of fatty acid synthase, can inhibit PP2C indirectly by altering lipid metabolism, thereby affecting membrane composition and signaling pathways that involve PP2C. | ||||||
Brefeldin A | 20350-15-6 | sc-200861C sc-200861 sc-200861A sc-200861B | 1 mg 5 mg 25 mg 100 mg | $31.00 $53.00 $124.00 $374.00 | 25 | |
Brefeldin A disrupts the structure and function of the Golgi apparatus, leading to a broad disruption of cellular trafficking and signaling pathways that can result in the functional inhibition of PP2C. | ||||||