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Merck
CN

SML2418

Sigma-Aldrich

PS10

≥98% (HPLC)

别名:

2-[(2,4-Dihydroxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindole-4,6-diol

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About This Item

经验公式(希尔记法):
C14H13NO6S
分子量:
323.32
UNSPSC代码:
12352200
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

O=S(C1=C(O)C=C(O)C=C1)(N2CC(C(O)=CC(O)=C3)=C3C2)=O

InChI

1S/C14H13NO6S/c16-9-1-2-14(13(19)4-9)22(20,21)15-6-8-3-10(17)5-12(18)11(8)7-15/h1-5,16-19H,6-7H2

InChI key

SVUZJWAAXPEMKJ-UHFFFAOYSA-N

生化/生理作用

2-[(2,4-dihydroxyphenyl) sulfonyl]isoindoline-4,6-diol (PS10) can be considered as a therapeutic method to preserve glucose and lipid homeostasis in obesity and type 2 diabetes (T2D). It can induce pyruvate dehydrogenase complex (PDC) activity in liver and kidney. It is also considered as an effective PDK inhibitor to treat diabetic cardiomyopathy. In the normal myocardium, PS10 helps to enhance fractional carbohydrate oxidation.
PS10 is a potent and selective PDK (Pyruvate dehydrogenase kinase) inhibitor that improves glucose tolerance and lessens hepatic steatosis in diet-induced obese mice. PS10 binds to the ATP-binding pocket of PDKs.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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访问文档库

Shih-Chia Tso et al.
Journal of medicinal chemistry, 60(3), 1142-1150 (2017-01-14)
Pyruvate dehydrogenase kinases 1-4 (PDK1-4) negatively control activity of the pyruvate dehydrogenase complex (PDC) and are up-regulated in obesity, diabetes, heart failure, and cancer. We reported earlier two novel pan-PDK inhibitors PS8 [4-((5-hydroxyisoindolin-2-yl)sulfonyl)benzene-1,3-diol] (1) and PS10 [2-((2,4-dihydroxyphenyl)sulfonyl)isoindoline-4,6-diol] (2) that targeted
Shih-Chia Tso et al.
The Journal of biological chemistry, 289(7), 4432-4443 (2013-12-21)
Pyruvate dehydrogenase kinase isoforms (PDKs 1-4) negatively regulate activity of the mitochondrial pyruvate dehydrogenase complex by reversible phosphorylation. PDK isoforms are up-regulated in obesity, diabetes, heart failure, and cancer and are potential therapeutic targets for these important human diseases. Here
Targeting hepatic pyruvate dehydrogenase kinases restores insulin signaling and mitigates ChREBP-mediated lipogenesis in diet-induced obese mice
Wu CY, et al.
Molecular Metabolism, 12, 12-24 (2018)
A novel inhibitor of pyruvate dehydrogenase kinase stimulates myocardial carbohydrate oxidation in diet-induced obesity
Wu CY, et al.
Test, 293(25), 9604-9613 (2018)
Cheng-Yang Wu et al.
The Journal of biological chemistry, 293(25), 9604-9613 (2018-05-10)
The pyruvate dehydrogenase complex (PDC) is a key control point of energy metabolism and is subject to regulation by multiple mechanisms, including posttranslational phosphorylation by pyruvate dehydrogenase kinase (PDK). Pharmacological modulation of PDC activity could provide a new treatment for

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