PP2B-Aγ Activators
The class of PP2B-Aγ activators encompasses a diverse spectrum of chemicals that intricately modulate the activity of the PP2B-Aγ phosphatase. PP2B-Aγ, also known as calcineurin, plays a pivotal role in cellular signaling by dephosphorylating key substrates involved in various physiological processes. One notable direct activator within this class is the Calcineurin Autoinhibitory Peptide (CAIP), which acts as a competitive inhibitor of calcineurin's autoinhibitory domain, promoting sustained phosphatase activity. Indirect activators such as Cyclosporin A and FK506, often used in immunosuppressive therapy, disrupt calcineurin function by forming complexes with cyclophilin and FKBP12, respectively. This inhibition leads to sustained phosphorylation levels of PP2B-Aγ substrates, indirectly promoting its activity. A23187, by inducing calcium influx, initiates the calcium-dependent pathway, ultimately influencing PP2B-Aγ activity through calcineurin activation. Okadaic Acid, a PP2A inhibitor, indirectly activates PP2B-Aγ by preventing the dephosphorylation and inactivation of PP2B-Aγ substrates. Dihydroxycalcitriol, a vitamin D receptor agonist, indirectly influences PP2B-Aγ by enhancing calcineurin expression, emphasizing the intricate relationship between vitamin D signaling and phosphatase activity.
Among the indirect activators, Endosulfine-α stands out as an endogenous inhibitor that directly binds to the autoinhibitory domain of PP2B-Aγ, preventing autoinhibition and promoting sustained phosphatase activity. This highlights the significance of endogenous modulators in fine-tuning the activation of PP2B-Aγ. Metal ions such as Manganese (II) Chloride serve as cofactors for calcineurin, indirectly enhancing PP2B-Aγ activity through their impact on calcineurin activation. Amlodipine, a calcium channel blocker, indirectly influences PP2B-Aγ by modulating calcium channels, altering calcium signaling dynamics and, consequently, phosphatase activity. In summary, the diverse mechanisms employed by PP2B-Aγ activators, whether direct or indirect, underscore the intricate regulatory networks governing this phosphatase's activation. The class of PP2B-Aγ activators provides valuable insights into the nuanced control of cellular signaling pathways and highlights the potential for targeted modulation of phosphatase activity in various physiological contexts.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Ionomycin, free acid | 56092-81-0 | sc-263405 sc-263405A | 1 mg 5 mg | $94.00 $259.00 | 2 | |
Increases intracellular calcium levels by facilitating calcium ion transport across the plasma membrane, leading to pp2b-aγ activation. | ||||||
FK-506 | 104987-11-3 | sc-24649 sc-24649A | 5 mg 10 mg | $76.00 $148.00 | 9 | |
FK506, similar to Cyclosporin A, indirectly activates PP2B-Aγ by forming a complex with FKBP12 and inhibiting calcineurin. The FK506-FKBP12 complex disrupts calcineurin function, leading to sustained phosphorylation levels of PP2B-Aγ substrates, indirectly promoting its activity. This highlights the role of calcineurin inhibition in the indirect activation of PP2B-Aγ by FK506. | ||||||
A23187 | 52665-69-7 | sc-3591 sc-3591B sc-3591A sc-3591C | 1 mg 5 mg 10 mg 25 mg | $54.00 $128.00 $199.00 $311.00 | 23 | |
Similar to ionomycin, elevates intracellular calcium levels, promoting pp2b-aγ activation. | ||||||
Okadaic Acid | 78111-17-8 | sc-3513 sc-3513A sc-3513B | 25 µg 100 µg 1 mg | $285.00 $520.00 $1300.00 | 78 | |
Okadaic Acid indirectly activates PP2B-Aγ by inhibiting PP2A, a phosphatase that dephosphorylates and inactivates PP2B-Aγ. Inhibition of PP2A by Okadaic Acid leads to sustained phosphorylation and activation of PP2B-Aγ substrates. This indirect activation underscores the interplay between phosphatases and highlights how Okadaic Acid influences PP2B-Aγ activity through modulation of its upstream regulators. | ||||||
Dibutyryl-cAMP | 16980-89-5 | sc-201567 sc-201567A sc-201567B sc-201567C | 20 mg 100 mg 500 mg 10 g | $45.00 $130.00 $480.00 $4450.00 | 74 | |
A cell-permeable analog of cAMP that directly activates pp2b-aγ by elevating cAMP levels in cells. | ||||||
Amlodipine | 88150-42-9 | sc-200195 sc-200195A | 100 mg 1 g | $73.00 $163.00 | 2 | |
Amlodipine indirectly activates PP2B-Aγ by modulating calcium channels. By blocking L-type calcium channels, Amlodipine reduces calcium influx, which negatively impacts calcineurin activation. The diminished calcineurin activity results in sustained phosphorylation and activation of PP2B-Aγ substrates, presenting an indirect route through which Amlodipine influences PP2B-Aγ activity by altering calcium signaling dynamics. | ||||||
Ryanodine | 15662-33-6 | sc-201523 sc-201523A | 1 mg 5 mg | $219.00 $765.00 | 19 | |
Modulates ryanodine receptors, leading to increased release of calcium from intracellular stores, which activates pp2b-aγ. | ||||||
(±)-Bay K 8644 | 71145-03-4 | sc-203324 sc-203324A sc-203324B | 1 mg 5 mg 50 mg | $82.00 $192.00 $801.00 | ||
Bay K8644 indirectly activates PP2B-Aγ by enhancing calcium influx through L-type calcium channels. Increased intracellular calcium levels activate calcineurin, leading to dephosphorylation and activation of PP2B-Aγ. Bay K8644's action on calcium channels provides an indirect mechanism for modulating PP2B-Aγ activity, illustrating the impact of calcium signaling dynamics on phosphatase regulation. | ||||||
Manganese(II) chloride beads | 7773-01-5 | sc-252989 sc-252989A | 100 g 500 g | $19.00 $30.00 | ||
Manganese (II) Chloride indirectly activates PP2B-Aγ by enhancing calcineurin activity. Manganese serves as a cofactor for calcineurin, promoting its activation and subsequent dephosphorylation and activation of PP2B-Aγ. The increased calcineurin activity provides an indirect mechanism for modulating PP2B-Aγ activity, illustrating the impact of metal ions on the activation of phosphatases in cellular signaling pathways. | ||||||
BAY 11-7085 | 196309-76-9 | sc-202490 sc-202490A | 10 mg 50 mg | $122.00 $516.00 | 55 | |
Bay 11-7082 indirectly activates PP2B-Aγ by inhibiting NF-κB signaling. NF-κB activation suppresses calcineurin expression, and by inhibiting NF-κB, Bay 11-7082 enhances calcineurin levels, leading to increased PP2B-Aγ activity. The modulation of NF-κB signaling by Bay 11-7082 provides an indirect mechanism for influencing PP2B-Aγ activity, emphasizing the crosstalk between signaling pathways and the consequential impact on phosphatase activity. | ||||||