KPLH1130是一种特异性的丙酮酸脱氢酶激酶（PDK）抑制剂，能够有效阻断巨噬细胞的极化并减轻促炎反应。该化合物在高脂饮食小鼠模型中显示出改善葡萄糖耐受性的潜力，适用于研究代谢疾病和炎症相关疾病。

AZD7545是一种选择性PDHK2（丙酮酸脱氢酶激酶2）抑制剂，对PDHK1和PDHK2的IC50分别为36.8 nM和6.4 nM。

VER-246608 是一种 ATP 竞争性的丙酮酸脱氢酶激酶抑制剂，对 PDK-1、PDK-3、PDK-2 和 PDK-4 的 IC50 分别为 35 nM、40 nM、84 nM 和 91 nM。

PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity[1].

SU11652 is a sunitinib analog with anti-tyrosine-kinase activity, also is identified as a potential inhibitor for Leishmania major (Lm) nucleoside diphosphate kinases NDK and structural studies indicated that this molecule binds to the active site of LmNDK in a similar conformation to nucleotides, mimicking natural substrates.