GSA-10 is a Smoothened (Smo) receptor agonist (EC50 = 1.2 μM). GSA-10 fits to the agonist pharmacophoric model with two hydrogen bond acceptor groups and four hydrophobic regions. GSA-10 acts at Smo to promote the differentiation of multipotent mesenchymal progenitor cells into osteoblasts. GSA-10 does not recognize the classic bodipy-cyclopamine binding site. GSA-10 allows the pharmacological characterization of a novel Smo active site, which is notably not targeted to the primary cilium and strongly potentiated by forskolin and cholera toxin. GSA-10 belongs to a new class of Smo agonists and will be helpful for dissecting Hh mechanism of action, with important implications in physiology and in therapy. (Mol Pharmacol. 2013 May;83(5):1020-9) References: Gorojankina T, Hoch L, Faure H, Roudaut H, Traiffort E, Schoenfelder A, Girard N, Mann A, Manetti F, Solinas A, Petricci E, Taddei M, Ruat M. Discovery, molecular and pharmacological characterization of GSA-10, a novel small-molecule positive modulator of Smoothened. Mol Pharmacol. 2013 May;83(5):1020-9. doi: 10.1124/mol.112.084590. Epub 2013 Feb 28. Erratum in: Mol Pharmacol. 2013 Aug;84(2):303. PubMed PMID: 23448715.

纯度：≥98%

CAS：300833-95-8