KIBRA Activators
Chemical activators of the KIBRA protein (also known as WWC1) largely operate through distinct biochemical pathways, many of which revolve around the modulation of protein phosphorylation. Some, such as Calyculin A and Okadaic Acid, inhibit protein phosphatases like PP1 and PP2A, maintaining higher phosphorylation levels of proteins, including KIBRA, and thereby indirectly increasing its activation.
A significant number of activators, including Forskolin, Isoproterenol, 8-bromo-cAMP, Epinephrine, IBMX, and Rolipram, function through the cAMP-dependent PKA pathway. These compounds increase cAMP levels, leading to PKA activation, which can then phosphorylate and activate KIBRA. Additionally, Ionomycin and A23187 are calcium ionophores that increase intracellular calcium levels. This elevation can activate calmodulin-dependent kinases which have been shown to phosphorylate and activate KIBRA. Lastly, PMA and Bisindolylmaleimide I act on the Protein Kinase C pathway which has also been implicated in KIBRA phosphorylation and activation. These chemicals illustrate the various pathways that can modulate KIBRA activity, underscoring the protein's involvement in diverse cellular events.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $160.00 $750.00 | 59 | |
Calyculin A inhibits protein phosphatases like PP1 and PP2A, thus maintaining higher phosphorylation levels of proteins. Since KIBRA is regulated by phosphorylation, the inhibition of phosphatases can indirectly lead to KIBRA 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 is a potent inhibitor of protein phosphatases such as PP2A. By inhibiting these phosphatases, Okadaic Acid can indirectly increase the phosphorylation and activation of KIBRA. | ||||||
Forskolin | 66575-29-9 | sc-3562 sc-3562A sc-3562B sc-3562C sc-3562D | 5 mg 50 mg 1 g 2 g 5 g | $76.00 $150.00 $725.00 $1385.00 $2050.00 | 73 | |
Forskolin can activate the PKA pathway by stimulating adenylyl cyclase, which increases cAMP levels. The PKA pathway can phosphorylate KIBRA leading to its activation. | ||||||
Isoproterenol Hydrochloride | 51-30-9 | sc-202188 sc-202188A | 100 mg 500 mg | $27.00 $37.00 | 5 | |
Isoproterenol is an agonist of β-adrenergic receptors, increasing cAMP levels which can activate PKA. PKA, in turn, can lead to the phosphorylation and activation of KIBRA. | ||||||
8-Bromo-cAMP | 76939-46-3 | sc-201564 sc-201564A | 10 mg 50 mg | $97.00 $224.00 | 30 | |
This cAMP analog can increase cAMP concentrations, leading to the activation of PKA. PKA can then phosphorylate and activate KIBRA. | ||||||
(−)-Epinephrine | 51-43-4 | sc-205674 sc-205674A sc-205674B sc-205674C sc-205674D | 1 g 5 g 10 g 100 g 1 kg | $40.00 $102.00 $197.00 $1739.00 $16325.00 | ||
By binding to adrenergic receptors, Epinephrine can lead to an increase in cAMP levels, which activates PKA. PKA can phosphorylate and activate KIBRA. | ||||||
IBMX | 28822-58-4 | sc-201188 sc-201188B sc-201188A | 200 mg 500 mg 1 g | $159.00 $315.00 $598.00 | 34 | |
IBMX is a non-selective phosphodiesterase inhibitor. By increasing intracellular cAMP, it activates PKA which can phosphorylate and activate KIBRA. | ||||||
Rolipram | 61413-54-5 | sc-3563 sc-3563A | 5 mg 50 mg | $75.00 $212.00 | 18 | |
Rolipram inhibits PDE4, leading to increased cAMP levels. This activates PKA, which can phosphorylate and activate KIBRA. | ||||||
Ionomycin, free acid | 56092-81-0 | sc-263405 sc-263405A | 1 mg 5 mg | $94.00 $259.00 | 2 | |
Ionomycin increases intracellular calcium levels. This can activate calmodulin-dependent kinase, which can phosphorylate and activate KIBRA. | ||||||
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 | |
A23187 is a calcium ionophore that can increase intracellular calcium levels. Elevated calcium levels can activate calmodulin-dependent kinase, leading to KIBRA phosphorylation and activation. | ||||||