PP2A-B55-α Inhibitors
PP2A-B55-α inhibitors comprise a diverse group of compounds primarily recognized for their ability to inhibit protein phosphatase activity, with a secondary effect on the B55-α regulatory subunit of PP2A. These inhibitors, such as Okadaic Acid and Cantharidin, do not bind directly to the B55-α subunit but instead modulate PP2A's catalytic core, indirectly affecting the assembly and specificity of the B55-α containing PP2A holoenzymes. By doing so, they alter the phosphorylation status of a broad range of cellular proteins, thereby modifying the activity of PP2A-B55-α in the context of its regulatory role over cell cycle progression and other cellular processes. The complexity of PP2A regulation and the non-specificity of the available inhibitors necessitate a comprehensive understanding of cellular signaling networks to deduce the exact impact on PP2A-B55-α.
Moreover, chemicals like LB-100 and microcystin-LR serve as tools to investigate the biological roles of PP2A-B55-α by influencing the balance of phosphorylation within cells. Inhibition of PP2A by these compounds results in increased phosphorylation of downstream targets, which can elucidate the functional contributions of PP2A-B55-α under normal physiological conditions. The specificity of this class of inhibitors varies, with some like Tautomycetin and Calyculin A showing selectivity towards the PP2A enzyme. Their utilization in research provides insight into the signaling pathways and substrates under the purview of PP2A-B55-α, aiding in the delineation of its roles in cellular homeostasis and signaling. Through these chemical modulators, the activity and regulatory functions of PP2A-B55-α can be dissected, revealing its involvement in crucial cellular processes.
SEE ALSO...
| Product Name | CAS # | Catalog # | QUANTITY | Price | Citations | RATING |
|---|---|---|---|---|---|---|
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 PP1 and PP2A; by inhibiting PP2A, it can indirectly affect the substrate specificity and activity of PP2A-B55-α subunit by altering the phosphatase's overall composition. | ||||||
Cantharidin | 56-25-7 | sc-201321 sc-201321A | 25 mg 100 mg | $89.00 $279.00 | 6 | |
Cantharidin inhibits protein phosphatases PP1 and PP2A. Inhibition of PP2A by Cantharidin could alter the dephosphorylation state of substrates relevant to PP2A-B55-α, indirectly affecting its regulatory role. | ||||||
Endothall | 145-73-3 | sc-201325 sc-201325A | 20 mg 100 mg | $49.00 $203.00 | 1 | |
Endothall acts as a PP2A inhibitor, and while its primary mechanism is broad, it can disrupt the activity of PP2A complexes including PP2A-B55-α by preventing substrate dephosphorylation. | ||||||
Norcantharidin | 29745-04-8 | sc-280719 | 5 g | $113.00 | 2 | |
Norcantharidin is a demethylated analog of Cantharidin with similar phosphatase inhibition profiles, potentially modulating PP2A-B55-α activity through broader PP2A complex activity disruption. | ||||||
Calyculin A | 101932-71-2 | sc-24000 sc-24000A | 10 µg 100 µg | $163.00 $800.00 | 59 | |
As a toxin that inhibits PP1 and PP2A, Calyculin A could affect PP2A-B55-α function by stabilizing the phosphorylated state of its substrates, indirectly reducing the subunit's regulatory capacity. | ||||||
LB-100 | 1632032-53-1 | sc-507368 | 10 mg | $330.00 | ||
LB-100 is a small molecule inhibitor of PP2A, indirectly modulating the activity of PP2A-B55-α by changing the phosphorylation status of proteins that the B55-α subunit would typically regulate. | ||||||
Phenothiazine | 92-84-2 | sc-250686 sc-250686A | 50 g 250 g | $23.00 $44.00 | ||
Phenothiazines, though broadly acting, are known to inhibit PP2A activity. This can affect PP2A-B55-α indirectly by influencing the phosphoprotein networks that PP2A-B55-α oversees. | ||||||
Perphenazine | 58-39-9 | sc-208161 | 100 mg | $190.00 | ||
Perphenazine, as part of the phenothiazine class, has demonstrated inhibition of PP2A. This impacts PP2A-B55-α by modulating dephosphorylation dynamics within cells. | ||||||
Thiostrepton | 1393-48-2 | sc-203412 sc-203412A | 1 g 5 g | $117.00 $423.00 | 10 | |
Thiostrepton is known to interact with protein synthesis and potentially affect PP2A through indirect mechanisms, potentially modulating PP2A-B55-α activity by altering protein translation and stability. | ||||||
Sulfabenzamide | 127-71-9 | sc-251079 | 1 g | $43.00 | ||
Sulfabenzamide, while primarily an antimicrobial, has been observed to influence phosphatase activity. It could modulate PP2A-B55-α by affecting the broader PP2A holoenzyme function. | ||||||