| Identification | Back Directory | [Name]
PS10 | [CAS]
1564265-82-2 | [Synonyms]
PS10
PS10,PS-10
2-[(24-Dihydroxyphenyl)sulfonyl]-23-dihydro-1H-isoindole-46-diol
1H-Isoindole-4,6-diol, 2-[(2,4-dihydroxyphenyl)sulfonyl]-2,3-dihydro- | [Molecular Formula]
C14H13NO6S | [MDL Number]
MFCD31814433 | [MOL File]
1564265-82-2.mol | [Molecular Weight]
323.32 |
| Chemical Properties | Back Directory | [Boiling point ]
661.7±65.0 °C(Predicted) | [density ]
1.696±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
7.05±0.35(Predicted) | [color ]
Light yellow to khaki |
| Hazard Information | Back Directory | [Enzyme inhibitor]
This novel ATP binding pocket-directed inhibitor (FW = 323.32 g/mol), systematically named 2-[(2,4-dihydroxyphenyl)sulfonyl]isoindoline-4,6- diol, targets all four PDK isoforms, with an IC50 = 0.8 μM and Ki = 0.24 μM for PDK2. Its design is based on structure-guided design, converting a known Hsp90 inhibitor into a series of highly specific PDK inhibitors, substituting a sulfonyl group in place of a carbonyl in the parent compound. This modification results in weak binding to Hsp90 (Ki = 47 μM). PS10 administration (70 mg/kg) to diet-induced obese mice significantly augments PDC activity with reduced phosphorylation in different tissues. Prolonged treatment improves glucose tolerance, with notably lessened hepatic steatosis in a mouse model. Such findings suggest pharmacological targeting of PDK may be useful in controlling glucose and fat levels in obesity and type 2 diabetes. |
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