CUR-61414 is a smoothened receptor antagonist potentially for the treatment of basal cell carcinoma. CUR61414 significantly inhibited skin Hedgehog signaling, blocked the induction of hair follicle anagen, and shrank existing basal cell carcinomas. CUR61414 can suppress proliferation and induce apoptosis of basaloid nests in the basal cell carcinoma model systems, whereas having no effect on normal skin cells.