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oroxylin A
- Development stage
- Unknown
- Lead developer
- China Pharmaceutical University
- Modality
- Small Molecules
- Administration
- Oral, Intravenous
01
Overview
Oroxylin A is a natural O-methylated flavone originally isolated from *Scutellaria baicalensis* (Baikal skullcap) and *Oroxylum indicum*. It is a bioactive small molecule with diverse pharmacological properties, notably in oncology and neurology. In cancer research, it has been identified as a cyclin-dependent kinase 9 (CDK9) inhibitor that suppresses PINK1-PRKN-mediated mitophagy by modulating the SIRT1-FOXO3-BNIP3 axis, which helps overcome drug resistance in hepatocellular carcinoma. It also binds to and inhibits the transforming growth factor beta (TGFβ) signaling pathway, effectively suppressing the epithelial–mesenchymal transition (EMT) and reducing metastasis in colorectal cancer cells. Beyond its antineoplastic activity, oroxylin A acts as a negative allosteric modulator of the GABA-A receptor, contributing to its explored roles in enhancing cognitive function and treating attention deficit hyperactivity disorder (ADHD).
- Other names
- 5,7-dihydroxy-6-methoxyflavone5,7-dihydroxy-6-methoxy-2-phenyl-4H-chromen-4-oneOroxylin-A
02
Targets
CDK9 (Cyclin-dependent kinase 9)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)
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