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, at concentrations ranging from 1 to 10 μM and incubation periods of 24 to 72 hours, significantly suppresses the proliferation of basal cell carcinoma cells dependent on Gli signaling, evidenced by its ability to inhibit cell growth and decrease Gli1 mRNA expression levels. Specifically, at a concentration of 5 μM over 24 to 72 hours, it hindered the proliferation of ASZ001 BCC cells, as demonstrated by a Cell Proliferation Assay. Additionally, Western Blot Analysis revealed that Glabrescione B, within a concentration range of 1-10 μM and over 24 to 48 hours, effectively reduced Gli1 mRNA expression in the same cell line.

In an animal model utilizing female NOD/SCID mice with ASZ001 BCC allografts [2], the administration of the chemical compound at a dosage of 100 μmol/kg through intraperitoneal (i.p.) injection every other day for a duration of 18 days resulted in a significant decrease in tumor growth and Gli1 mRNA levels.