PLP-Cβ Activators
Chemical activators of PLP-Cβ utilize various mechanisms to increase the protein's activity by influencing its phosphorylation state. Forskolin is known for its direct action on adenylate cyclase, which leads to a rise in cAMP levels within the cell. The subsequent activation of protein kinase A (PKA) results in PKA phosphorylating PLP-Cβ, thereby enhancing its activity. Similarly, dibutyryl cAMP (db-cAMP), a cAMP analog, activates PKA, which then targets PLP-Cβ for phosphorylation. Phorbol 12-myristate 13-acetate (PMA) and 1,2-Dioctanoyl-sn-glycerol (DiC8), on the other hand, directly stimulate protein kinase C (PKC). Once activated, PKC phosphorylates PLP-Cβ, leading to its activation. This PKC-mediated pathway is also implicated when the cell's cytoskeletal dynamics are altered by compounds like (−)-Blebbistatin, thereby indirectly affecting the phosphorylation and activity of PLP-Cβ.
Intracellular calcium levels play a pivotal role in the regulation of PLP-Cβ activity. Ionomycin, which is a calcium ionophore, elevates calcium levels inside the cell and can activate calcium-dependent protein kinases, such as calmodulin-dependent kinase (CaMK). These kinases can then phosphorylate PLP-Cβ, resulting in its activation. Thapsigargin and BAY K8644 both induce an increase in intracellular calcium, albeit through different mechanisms; thapsigargin interferes with the SERCA pump, while BAY K8644 acts as an agonist at L-type calcium channels. Both agents lead to the phosphorylation of PLP-Cβ via calcium-dependent kinases. Additionally, the use of okadaic acid and calyculin A inhibits protein phosphatases 1 and 2A, which normally act to dephosphorylate proteins. The inhibition of these phosphatases by okadaic acid and calyculin A thus keeps PLP-Cβ in a phosphorylated and active state. Finally, while H-89 is a PKA inhibitor, it can lead to the activation of PLP-Cβ through compensatory signaling pathways that may involve PKC or other kinases.
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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 | |
Phorbol 12-myristate 13-acetate (PMA) is a potent activator of protein kinase C (PKC). Upon activation, PKC phosphorylates a variety of target proteins. PKC-mediated phosphorylation of PLP-Cβ can lead to changes in its activity state, thereby functionally activating PLP-Cβ. | ||||||
Ionomycin | 56092-82-1 | sc-3592 sc-3592A | 1 mg 5 mg | $78.00 $270.00 | 80 | |
Ionomycin is a calcium ionophore that increases intracellular calcium levels. The rise in calcium can activate calcium-dependent protein kinases, such as calmodulin-dependent kinase (CaMK), which can phosphorylate and thus activate PLP-Cβ. | ||||||
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. By inhibiting these phosphatases, okadaic acid prevents the dephosphorylation of proteins, thus maintaining proteins like PLP-Cβ in a phosphorylated and active state. | ||||||
Anisomycin | 22862-76-6 | sc-3524 sc-3524A | 5 mg 50 mg | $99.00 $259.00 | 36 | |
Anisomycin is a protein synthesis inhibitor that also activates stress-activated protein kinases like JNK. The activation of these kinases can lead to the phosphorylation and activation of PLP-Cβ. | ||||||
Thapsigargin | 67526-95-8 | sc-24017 sc-24017A | 1 mg 5 mg | $136.00 $446.00 | 114 | |
Thapsigargin inhibits the SERCA pump, leading to an increase in cytosolic calcium levels. The elevation of intracellular calcium activates calcium-dependent kinases, which in turn can lead to the phosphorylation and activation of PLP-Cβ. | ||||||
(±)-Bay K 8644 | 71145-03-4 | sc-203324 sc-203324A sc-203324B | 1 mg 5 mg 50 mg | $84.00 $196.00 $817.00 | ||
BAY K8644 acts as an agonist at L-type calcium channels, causing increased calcium influx. The resulting increase in intracellular calcium concentration can activate calcium-dependent kinases that may phosphorylate and thus activate PLP-Cβ. | ||||||
Dibutyryl-cAMP | 16980-89-5 | sc-201567 sc-201567A sc-201567B sc-201567C | 20 mg 100 mg 500 mg 10 g | $47.00 $136.00 $492.00 $4552.00 | 74 | |
Dibutyryl cAMP is a membrane-permeable analogue of cAMP that activates PKA. PKA can phosphorylate and thereby activate PLP-Cβ. | ||||||
(S)-(−)-Blebbistatin | 856925-71-8 | sc-204253 sc-204253A sc-204253B sc-204253C | 1 mg 5 mg 10 mg 25 mg | $72.00 $265.00 $495.00 $968.00 | ||
(−)-Blebbistatin inhibits non-muscle myosin II ATPase activity, leading to alterations in cytoskeletal dynamics. Such changes can activate signaling pathways that influence the activity of kinases and phosphatases, which in turn can modulate the phosphorylation state and activity of PLP-Cβ. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Similar to okadaic acid, calyculin A is a potent inhibitor of protein phosphatase 1 and 2A, leading to increased phosphorylation levels of proteins. This inhibition can result in the sustained phosphorylation and activation of PLP-Cβ. | ||||||
1,2-Dioctanoyl-sn-glycerol | 60514-48-9 | sc-202397 sc-202397A | 10 mg 50 mg | $47.00 $254.00 | 2 | |
DiC8 is a synthetic analogue of diacylglycerol (DAG) and can directly activate PKC. Activation of PKC by DiC8 can lead to the phosphorylation and activation of PLP-Cβ. | ||||||