Name | PDK4-IN-1 hydrochloride |
Synonyms | PDK4-IN-1 hydrochloride PDK4-IN-1 HYDROCHLORIDE 1-(1-(Piperidin-4-yl)-1H-pyrazol-4-yl)anthracene-9,10-dione hydrochloride |
CAS | 2310262-11-2 |
Molecular Formula | C22H20ClN3O2 |
Molar Mass | 393.87 |
Storage Condition | Inert atmosphere,Room Temperature |
biological activity | PDK4-IN-1 hydrochloride is an anthraquinone derivative and also a potent, an orally active Pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride effectively inhibits cell transformation and cell proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has anti-diabetic, anti-cancer and anti-allergic effects. |
Target | IC50: 84 nM (Pyruvate dehydrogenase kinase 4 (PDK4)) |
Cell Line: | HCT116 and RKO cells HCT116 and RKO cells HEK293T human embryonic kidney cells |
Concentration: | 50 μM 10 μM, 25 μM, 50 μM 10 μM |
Incubation Time: | 0 hour, 24 hours, 48 hours, 72hours 24 hours 24 hours |
Result: | Significantly impeded the proliferation of human colon cancer cell lines, HCT116 and RKO. Dose-dependently increased apoptosis. Inhibited phosphorylation of Ser 232 , Ser 293 , and Ser 300 of PDHE1α. Significantly improved glucose tolerance. |
Animal Model: | C57BL/6J mice (8-week old) fed with high-fat diet |
Dosage: | 100 mg/kg |
Administration: | Oral administration; daily; for 1 week |