Glabrescione B is a novel compound that specifically binds to Gli1, an important modulator of the Hedgehog (Hh) signaling pathway. By disrupting the Gli1-DNA interaction, Glabrescione B effectively impairs the activity of Gli1. Moreover, Glabrescione B demonstrates potent inhibitory effects on the growth of tumor cells that rely on Hedgehog signaling, as well as on the self-renewal capacity and clonogenicity of tumor-derived stem cells.

Glabrescione B (5 μM; 24-72 hours) inhibits the growth of Gli-dependent basal cell carcinoma[2]. Glabrescione B (1-10 μM; 24-48 hours) decreases Gli1 mRNA expression levels[2]. Cell Proliferation Assay[1]Cell Line: ASZ001 BCC cells Concentration: 5 μM Incubation Time: 24-72 hours Result: Basal cell carcinoma cell proliferation was impaired. Western Blot Analysis[1]Cell Line: ASZ001 BCC cells Concentration: 1-10 μM Incubation Time: 24-48 hours Result: Gli1 mRNA expression levels was decreased.

Animal Model: Female NOD/SCID mice (ASZ001 BCC allografts)[2]Dosage: 100 μmol/kg Administration: I.p.; every second day for 18 days Result: A significant reduction of tumor growth as well as Gli1 mRNA levels was observed.