PDK4-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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).

PDK4-IN-1 treatment significantly impedes the proliferation of human colon cancer cell lines, HCT116 and RKO. The colony formation efficiency in HCT116 and RKO cells Is significantly reduced after treatment of PDK4-IN-1. PDK4-IN-1 (Compound 8c; 10-50 ┢M; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. PDK4-IN-1 (compound 8c)-induced phosphorylation of p53 on serine 15 is a dose-dependent response in both HCT116 and RKO cells. PDK4-IN-1 decreases the expression of BCL-xL and increases the expression of BAX. Cleavage of PARP1 and caspase 3 are increased by PDK4-IN-1.

――

Others

Other Targets

Pyruvate dehydrogenase kinase 4 (PDK4),84 nM

――

――

2310262-10-1

357.41

C22H19N3O2

>98% (HPLC)

――

――

――

(-20℃)

With Ice Pack

≥ 2 years