Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T74830 | PDK-IN-1 | ||
PDK-IN-1(compound 7o)是一种针对丙酮酸脱氢酶激酶(PDK)的抑制剂,其对PDK1和HSP90的IC50值分别为0.03和0.1μM。通过靶向PDH/PDK轴,PDK-IN-1能有效降低肿瘤质量。 | |||
T12412L |
PDK4-IN-1 hydrochloride
|
Apoptosis; PDK | Apoptosis; PI3K/Akt/mTOR signaling |
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物,对丙酮酸脱氢酶激酶 4有抑制作用,IC50为 84 nM,具有口服活性。它抑制细胞转化和细胞增殖并诱导细胞凋亡。它具有抗过敏,抗糖尿病和抗癌作用。 | |||
T12412 |
PDK4-IN-1
|
Others | Others |
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4)(IC50 value of 84 nM). | |||
T16450 |
PDK1-IN-RS2
|
PDK | PI3K/Akt/mTOR signaling |
PDK1-IN-RS2 inhibits the activation of the downstream kinases S6K1 by PDK1. PDK1-IN-RS2 is a mimic of the peptide docking motif (PIFtide) and is a substrate-selective PDK1 inhibitor (Kd: 9 μM). | |||
T17224 |
VER-246608
|
Dehydrogenase; PDK | Metabolism; PI3K/Akt/mTOR signaling |
VER-246608 是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。 | |||
T79723 |
PDK-IN-2
|
||
PDK-IN-2(Compound 1F)是一种具有IC50为68 nM的PDK抑制剂。该化合物能够抑制PDK1和PDK4在细胞内的表达,增强线粒体生物能并降低糖酵解表型,同时诱导细胞走向线粒体途径的apoptosis。此外,PDK-IN-2在4T1同基因小鼠模型中能够有效抑制肿瘤生长。 |