Hh Signaling Antagonist X, Itraconazole – CAS 84625-61-6 – Calbiochem

Descrição detalhada : A cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-alpha-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner., A cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-alpha-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~ 0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~ 0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner.
Sinónimos : Hh Signaling Antagonist X, Itraconazole - CAS 84625-61-6 - Calbiochem; 14LDM Inhibitor, Oriconazole, R51211, Smo Antagonist VII, Sporanox, 14-alpha-demethylase Inhibitor; 14LDM Inhibitor, Oriconazole, R51211, Smo Antagonist VII, Sporanox, 14-alpha-demethylase Inhibitor
Fórmula molecula r: C35H38Cl2N8O4
Armazenamento : 2-8C; 2-8C; 2-8C
Embalagem : 1X250MG