These results, in concert with previous studies, strengthen the rationale to further investigate: (a) KCZ and other azole compounds as candidate cancer therapeutics; (b) the non-canonical pathways leading to GLI1 and tGLI1 activation; (c) the structure–activity relationship between azole compounds and tGLI1 antagonism; and (d) additional mechanisms by which KCZ and related compounds inhibit tGLI1-positive breast cancer. Here, GLI1 is linked to breast cancer.