PP2Cα Activators
PP2Cα activators are compounds that can enhance the enzymatic activity of the protein phosphatase 2C alpha (PP2Cα), which is a member of the PP2C family of Ser/Thr protein phosphatases. These activators can work by binding to the PP2Cα protein, thereby inducing conformational changes that promote its phosphatase activity. PP2Cα itself is a vital enzyme involved in various cellular processes, including the regulation of metabolic pathways, cell cycle progression, and stress responses. Activators of PP2Cα could increase the dephosphorylation rate of its substrate proteins, either by increasing the enzyme's affinity for its substrates or by enhancing its catalytic efficiency. The activation of PP2Cα could lead to the removal of phosphate groups from serine and threonine residues on target proteins, altering their activity, stability, or interaction with other proteins, and thereby having a profound impact on cellular signaling pathways.
The efficacy of PP2Cα activators can be determined by their ability to selectively interact with the PP2Cα enzyme. This specificity is crucial since indiscriminate activation of phosphatases could lead to widespread dephosphorylation and unintended cellular consequences. The design of PP2Cα activators may involve the optimization of molecular structures to fit into the active site of the enzyme or to interact with allosteric sites that can modulate the enzyme's activity. Furthermore, these activators can be fine-tuned to exhibit favorable pharmacokinetic properties, ensuring that they can reach their target within the cellular environment. By modulating the activity of PP2Cα, such activators can influence the phosphorylation status of a network of proteins, thus playing a key role in the regulation of cellular processes governed by reversible phosphorylation. Careful modulation of PP2Cα activity through these activators can thus serve as a tool for altering specific signaling pathways within cells.
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Magnesium sulfate anhydrous | 7487-88-9 | sc-211764 sc-211764A sc-211764B sc-211764C sc-211764D | 500 g 1 kg 2.5 kg 5 kg 10 kg | $46.00 $69.00 $163.00 $245.00 $418.00 | 3 | |
As a cofactor, Magnesium directly activates PP2Cα by binding to its metal-binding sites, which is essential for the catalytic activity of PP2Cα. Magnesium's presence is required for PP2Cα to adopt a conformation capable of dephosphorylation of its substrates. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $48.00 | ||
Zinc ions can bind to the metal-binding sites of PP2Cα, similar to magnesium, and are essential for its catalytic activity. Although zinc is a secondary cofactor, its presence can enhance the stability and function of PP2Cα. | ||||||
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 | |
By elevating cAMP levels, Forskolin activates PKA, which can phosphorylate various substrates, including those that may interact with PP2Cα. This can indirectly affect PP2Cα activity by altering the phosphorylation status of its regulatory proteins or substrates, thereby enhancing its functional activity. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $291.00 $530.00 $1800.00 | 78 | |
Although a potent inhibitor of PP1 and PP2A, at lower concentrations, Okadaic Acid can selectively inhibit these phosphatases without affecting PP2Cα. This differential effect can indirectly upregulate PP2Cα activity by reducing competitive dephosphorylation of shared substrates. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Similar to Okadaic Acid, Calyculin A inhibits PP1 and PP2A at nanomolar concentrations. This can lead to a relative increase in PP2Cα activity by decreasing the dephosphorylation of substrates by PP1 and PP2A, thereby indirectly enhancing the dephosphorylation activity of PP2Cα. | ||||||
Spermine | 71-44-3 | sc-212953A sc-212953 sc-212953B sc-212953C | 1 g 5 g 25 g 100 g | $61.00 $196.00 $277.00 $901.00 | 1 | |
Spermine has been shown to modulate various protein phosphatases. It can bind to PP2Cα and stabilize its conformation, enhancing its enzymatic activity. Spermine's polyamine nature allows it to interact with the negative charges on the surface of PP2Cα, potentially affecting the enzyme's substrate specificity and activity. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin is an inhibitor of PP2A and PP1. By selectively inhibiting these phosphatases, it may indirectly enhance the role of PP2Cα in dephosphorylation events by increasing the availability of substrates for PP2Cα, as the competitive inhibition of PP1 and PP2A is lifted. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $49.00 $203.00 | 1 | |
Endothall also acts as an inhibitor of PP1 and PP2A. This compound could lead to an indirect increase in PP2Cα activity due to reduced competition for substrates, thus enhancing the specific dephosphorylation functions of PP2Cα. | ||||||