PS10

PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) [1]. PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy[2].PDK: pyruvate dehydrogenase kinase

Product Specifications

CAS Number

1564265-82-2

UNSPSC

12352005

Target

PDHK

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/ps10.html

Purity

98.51

Solubility

DMSO : 62.5 mg/mL (ultrasonic)

Smiles

OC1=CC(O)=CC2=C1CN(S(=O)(C3=CC=C(O)C=C3O)=O)C2

Molecular Formula

C14H13NO6S

Molecular Weight

323.32

References & Citations

[1]Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket.J Biol Chem. 2014 Feb 14;289 (7) :4432-43.|[2]Wu CY, et al. A novel inhibitor of pyruvate dehydrogenase kinase stimulates myocardial carbohydrate oxidation in diet-induced obesity.J Biol Chem. 2018 Jun 22;293 (25) :9604-9613.