SANT 2

SANT 2 is a potent Hh-signaling pathway antagonist. SANT 2 interferes with the expression of Gli1. SANT 2 causes developmental delay in medaka embryos. SANT 2 has the potential for the research of several malignancies including Gorlin syndrome (a disorder predisposing to basal cell carcinoma, medulloblastoma and rhabdomyosarcoma), prostate, pancreatic and breast cancers^[1][2]. In Vitro:SANT-2 (48 h) interferes with the expression of the Hh target gene Gli1 in Shh-Light II cells (IC₅₀ of 97.9 nM)^[1].
SANT 2 (0.01-100 μM; from 4-5 h post-fertilization until 5 days post-fertilization) does not induce the cyclopia phenotype in medaka embryos, but causes developmental delays at concentrations close to lethality^[1].
SANT 2 (5 h for radioligand binding assay, 40-48 h for β-lactamase reporter gene assay) shows allosteric inhibition of [³H]SAG-1.3 binding to Smo receptors in radioligand binding assays and fully inhibits SAG-1.5-induced Hh pathway activation in a β-lactamase reporter gene assay^[2].