Biochem/physiol Actions
Potent, orally active PDK4 inhibitor with antidiabetic and anticancer efficacy.
PDK4-IN-1 (PDK4i-8c) is a cell-penetrating anthraquinone derivative that has been identified as an allosteric inhibitor of pyruvate dehydrogenase kinase 4 (PDK4), whis is binding to its lipoamide binding site with a high affinity (IC50 = 84 nM). PDK4-IN-1 is orally available, demonstrates excellent metabolic stability, and exhibits a promising pharmacokinetic profile in rat studies. Moreover, PDK4-IN-1 substantially enhances glucose tolerance in mice with diet-induced obesity and mitigates allergic reactions in a passive cutaneous anaphylaxis mouse model. The in vivo data support its effectiveness as a potential treatment for diabetes. Additionally, PDK4-IN shows notable anticancer properties by regulating cell proliferation, transformation, and apoptosis.
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Hygroscopic
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear (Warmed) |
| storage temp. | -10 to -25°C |
| SMILES string | Cl.[n]2(ncc(c2)c3c4c(ccc3)C(=O)c5c(cccc5)C4=O)C1CCNCC1 |
| InChI key | ZIMLKZKPNALXKK-UHFFFAOYSA-N |
