Table 2.
Phenolic class activators.
Name (proposed mode of action) | Chemical structure | Biochemical assay
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Cell-based assay
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Activity | Substrate | PP2A | Selectivities | Activity | Cell type | ||
Tetralone (direct in the presence of ceramide) |
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520% (20 μM; in the presence of C2-cer) | Phosphorylated myelin basic protein | Purified heterotrimer from Jurkat cells | Yes vs PP1 | Not reported | Not reported |
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Quinolone (direct in the presence of ceramide) |
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400% (20 μM; in the presence of C2-cer) | Phosphorylated myelin basic protein | Purified heterotrimer from Jurkat cells | Yes vs PP1 | Not reported | Not reported |
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(-)-epigallocatechin gallate (PP2A methylesterase) |
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129% (100 μM) Antogonistic to OA IC50~80 μM ABC | No effect (p-histoneH1) | AC | Not reported | Not reported | Not reported |
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Dihydroxyphenylethano (direct) |
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500% (400 μM) | Phosphopeptide | Recombinant C | Yes vs PP1 | 780% (400 μM) | HT-29 (synthetic phosphopeptide) |
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Methyl-3,5-diiodo-4-(4’-methoxyphenoxy) benzoate (direct) |
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250% (10 μM) | [32P]-histone H1 | Purified red cell PP2A | Substrate specific, but activates ALP | 300% (10 μM) | Eras 20 ([32P]-histone H1) |
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β-tocopherol (direct, synergistic with ceramide, PME) |
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190% (50 μM) | Phosphorylase a | Purified red cell PP2A | Yes vs PP1 | 500% (50 μM) | A7r5 ([32P]-PKC) |
PP: Phosphoprotein phosphatase.