Name | PDK4-IN-1 hydrochloride |
Description | PDK4-IN-1 hydrochloride, an anthraquinone derivative, is a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4) with an IC50 value of 84 nM. |
In vitro | PDK4-IN-1 hydrochloride 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[1]. PDK4-IN-1 (Compound 8c; 10-50 μM; 24 hours; HCT116 and RKO cells) treatment dose-dependently increased apoptosis. 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[1]. |
In vivo | PDK4-IN-1 (C57BL/6J mice) treatment significantly improves glucose tolerance[1]. Pre-incubation with PDK4-IN-1 (compound 8c) dose-dependently inhibits the release of β-hexosaminidase from IgE/antigen-activated BMMCs, |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Solubility Information | DMSO : 125 mg/mL (317.36 mM), Sonication is recommended.
|
Keywords | Pyruvate dehydrogenase kinase | PDK4-IN-1 Hydrochloride | PDK-4-IN-1 hydrochloride | PDK4IN1 hydrochloride | PDK4 IN 1 hydrochloride | PDK4 | PDHK | PDHE1α | PDH kinase | PARP1 | p-Akt | p53 | metabolites | Inhibitor | inhibit | caspase-3 | BCL-xL | BAX | Apoptosis | antidiabetic | anticancer | anti-allergic |
Inhibitors Related | Stavudine | 5-Fluorouracil | Flubendazole | Cysteamine hydrochloride | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | L-Glutamic acid | Tributyrin | L-Ascorbic acid sodium salt | Alginic acid | Dextran sulfate sodium salt (MW 5000) |
Related Compound Libraries | PI3K-AKT-mTOR Compound Library | Anti-Colorectal Cancer Compound Library | Bioactive Compound Library | Antidepressant Compound Library | HIF-1 Signaling Pathway Compound Library | Kinase Inhibitor Library | Hematonosis Compound Library | Inhibitor Library | Anti-Aging Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library |