PS10 aptomycin (2012) Proc Natl Acad Sci

(2012) Proc Natl Acad Sci U S A

ML 145 acts as a competitive antagonist for a number of agonists at human GPR35 and has an IC50 value against EC80 concentrations of various GPR35 agonists in the region of 20 nM

Discovery and Development of LX7101

58 μM) and norepinephrine transporter (NET) (IC50=0

PS10 aptomycin (2012) Proc Natl Acad SciPS10 is a novel, potent and ATP competitive pan PDK inhibitor, inhibits all PDK isoforms with IC50 of 0. 8 M, 0. 76 M, 2. 1 M and 21. 3 M for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 M). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy. PDK: pyruvate