B430203M17Rik Activators
Chemical activators of PTEN function in various ways to modulate the activity of this crucial phosphatase. Perifosine, for instance, integrates into the plasma membrane and alters the composition of membrane lipids, which in turn positively influences PTEN activity by promoting its lipid phosphatase function. Similarly, VO-OHpic trihydrate acts as a robust inhibitor of protein tyrosine phosphatases, resulting in an upsurge of protein phosphorylation levels. This upregulation stabilizes PTEN and enhances its activity. Zinc Chloride, being a necessary cofactor for many enzymes, can bind directly to PTEN, aiding in its proper folding and thus catalytic function. Sodium Orthovanadate and Ammonium Vanadate, despite being general phosphatase inhibitors, at lower concentrations can activate PTEN through allosteric effects that induce a beneficial conformational shift in the protein structure, enhancing its phosphatase activity.
Further, Phenylarsine Oxide, which inhibits tyrosine phosphatases, and Calyculin A, a protein phosphatase inhibitor, both contribute to the activation of PTEN by preventing the dephosphorylation of regulatory sites on the protein. This maintenance of phosphorylation keeps PTEN in an active state. Cantharidin and Okadaic Acid, inhibitors of serine/threonine phosphatases, similarly lead to a rise in the phosphorylated state of proteins, which indirectly activates PTEN. Endothall's inhibition of protein phosphatases may trigger compensatory mechanisms that upregulate PTEN activity. Lastly, Sanguinarine can influence PTEN through modifications in the cellular redox state, which affects the oxidation-sensitive regulatory controls of PTEN, thereby activating the protein. Collectively, these chemicals engage with PTEN at various regulatory points and through different mechanisms, culminating in the activation of its phosphatase activity.
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| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
Perifosine | 157716-52-4 | sc-364571 sc-364571A | 5 mg 10 mg | $188.00 $327.00 | 1 | |
Perifosine activates phosphatase and tensin homolog (PTEN) by accumulating in the plasma membrane, where it modulates membrane lipid composition and affects membrane-associated signaling pathways, leading to the activation of PTEN's lipid phosphatase activity. | ||||||
Zinc | 7440-66-6 | sc-213177 | 100 g | $48.00 | ||
Zinc is known to be a cofactor necessary for the proper function of many enzymes, including phosphatases. Zinc Chloride can activate PTEN by binding to the protein, thus promoting its correct folding and catalytic activity. | ||||||
Sodium Orthovanadate | 13721-39-6 | sc-3540 sc-3540B sc-3540A | 5 g 10 g 50 g | $49.00 $57.00 $187.00 | 142 | |
Sodium Orthovanadate acts as a non-specific phosphatase inhibitor, but at sub-inhibitory concentrations, it can paradoxically increase the phosphatase activity of some proteins, including PTEN, by inducing a conformational change that results in activation. | ||||||
Phenylarsine oxide | 637-03-6 | sc-3521 | 250 mg | $41.00 | 4 | |
Phenylarsine Oxide is an inhibitor of tyrosine phosphatases, which indirectly can lead to the activation of PTEN by preventing dephosphorylation of PTEN's regulatory sites, maintaining PTEN in an active state. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
Calyculin A, a protein phosphatase inhibitor, can increase phosphorylation levels within the cell. It indirectly activates PTEN by preventing dephosphorylation at the regulatory sites that are important for PTEN's activity. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin inhibits serine/threonine phosphatases, which may result in the accumulation of phosphorylated proteins, indirectly leading to the activation of PTEN by enhanced phosphorylation at its regulation sites. | ||||||
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 serine/threonine phosphatases. By inhibiting these phosphatases, it can indirectly result in the activation of PTEN through increased phosphorylation levels of the regulatory sites on PTEN. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $49.00 $203.00 | 1 | |
Endothall is an inhibitor of protein phosphatases and may activate PTEN by enhancing the phosphorylation state of proteins in the PI3K/AKT pathway, which upregulates PTEN activity as a compensatory mechanism. | ||||||
Sanguinarium | 2447-54-3 | sc-473396 | 10 mg | $220.00 | ||
Sanguinarium can activate PTEN by interacting with the cellular redox state and modifying the oxidation-sensitive regulatory mechanisms that control PTEN activity, leading to its functional activation. | ||||||