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Discovery and Development of LX7101
ClH/c22-6-7-29-8-9-30-10-11-31-12-13-32-16-3-1-2-14-18(16)21(28)24(20(14)27)15-4-5-17(25)23-19(15)26
InChi: InChI=1S/C18H14N2O3S/c1-11-19-20-18(23-11)13-5-8-17-15(9-13)16(10-22-17)12-3-6-14(7-4-12)24(2)21/h3-10H
43 μM for BRD4(1)
814:178-186
PS10 aptomycin Discovery and Development of LX7101PS10 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