α-naphthoflavone

β-Naphthoflavone-CH2-Br is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br used to synthesize the PROTAC β-NF-JQ1.

β-Naphthoflavone-CH2-OH (β-NF-CH2-OH) serves as an AhR E3 ligase ligand, forming chimeric molecules when connected to a protein ligand through a linker, resulting in PROTACs or SNIPERs (e.g., β-naphthoflavone-JQ1). These chimeric molecules recruit the AhR E3 ligase complex by incorporating AhR ligands. By inducing ubiquitination-mediated degradation, PROTACs effectively target and degrade cancer-promoting proteins [1].

4'-Methyl-β-naphthoflavone, a metabolite of naphthoflavones (benzoflavones) in fungi, acts as an activator or inhibitor of CYP-450 [1].

5,6-Benzoflavone (β-Naphthoflavone) is an exogenous ligand for the aryl hydrocarbon receptor, which disrupts zinc homeostasis in human hepatocellular carcinoma HepG2 cells. 5,6-Benzoflavone (β-Naphthoflavone) possesses anti-inflammatory and antioxidant activities, inhibits LPS-induced inflammation through the AKT/Nrf-2/HO-1-NF-kappaB signaling axis, inhibits TNF-α-induced ICAM-1 and VCAM-1 expression, which can be used to study neurodegenerative diseases.

alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.

PROTAC CYP1B1 Degrader-1 (Compound 6C), an α-naphthoflavone chimera derivative, effectively targets and degrades cytochrome P450 (CYP) 1B1 to overcome agent resistance, displaying half-maximal inhibitory concentrations (IC50s) of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2. This compound is suitable for investigating prostate cancer characterized by overexpression of CYP1B1 [1].