Vismodegib
Sonic Hedgehog signaling pathway inhibitor / A potent and selective Hedgehog (Hh) pathway signaling inhibitor antagonizing SMO with a Ki of 1.3 nM).1 Alters intracellular Ca2+ homeostasis and inhibits growth of cisplatin-resistant lung cancer cells.2 Inhibits two ABC transporters, ABCG2/BCRP and ABCB1/Pgp, IC50s=1.4 and 3.0 μM respectively.3 Clinically useful for the treatment of basal cell carcinoma.4 Inhibits proliferation and induces apoptosis in colon cancer cell lines.
Biochemicals & reagents
879085-55-9
GDC-0449
1) Rominger et al. (2009), Evidence for allosteric interactions of antagonist binding to the smoothened receptor; J. Pharmacol. Exp. Therap., 329 995 2) Tian et al. (2012), the hedgehog pathway inhibitor GDC-0449 alters intracellular Ca2+ homeostasis and inhibits cell growth in cisplatin-resistant lung cancer cells; Anticancer Res., 32 89 3) Zhang et al. (2009), Hedgehog pathway inhibitor HhAntag691 is a potent inhibitor of ABCG2/BCRP and ABCB1/Pgp; Neoplasia, 11 96 4) Cirrone and Harris (2012), Vismodegib anf the hedgehog pathway: a new treatment for basal cell carcinoma; Clin. Ther., 34 2039 5) Wu et al. (2017), Smoothened antagonist GDC-0449 (Vismodegib) inhibits proliferation and triggers apoptosis in colon cancer cell lines; Exp. Ther. Med., 13 2529
-20°C
TARGET: GPCR -- PATHWAY: Hedgehog; Apoptosis inducer; Calcium signaling; Proliferation -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer