Potent and selective pyruvate dehydrogenase kinase (PDK) 1/2/3 inhibitor (IC50 values are 49, 101 and 313 nM for PDK1, PDK2 and PDK3, respectively). Exhibits selectivity for PDK1/2/3 over PDK4 and a panel of 323 other kinases. Suppresses A549 lung cancer cell proliferation in vitro. Reduces tumor volume of A549 xenografts in mice.
Sun et al (2015) JX06 selectively inhibits pyruvate dehydrogenase kinase PDK1 by a covalent cysteine modification. Cancer Res. 75 4923 PMID:26483203