vismodegib

Vismodegib (GDC-0449) 是一种刺猬抑制剂，IC50值为 3 nM。它还可抑制 P-gp 和ABCG2的活性，IC50值分别为 3.0 μM 和 1.4 μM。

Vismodegib-d7 是 Vismodegib 的氘代化合物。Vismodegib 的 CAS 号为 879085-55-9。Vismodegib 是一种刺猬抑制剂，IC50值为 3 nM。它还可抑制P-gp和ABCG2的活性，IC50值分别为 3.0 μM 和 1.4 μM。

Vismodegib-d4 是 Vismodegib 的氘代化合物。Vismodegib 的 CAS 号为 879085-55-9。Vismodegib 是一种刺猬抑制剂，IC50值为 3 nM。它还可抑制P-gp和ABCG2的活性，IC50值分别为 3.0 μM 和 1.4 μM。

NL-103 is a novel dual-targeted inhibitor of histone deacetylases and hedgehog pathway, effectively overcomes vismodegib resistance conferred by Smo mutations. NL-103 comprises structural elements of Hh pathway inhibitor vismodegib, and histone deacetylase (HDAC) inhibitor vorinostat. NL-103 simultaneously and significantly inhibited both HDACs and Hh pathway. Importantly, NL-103 effectively overcame vismodegib resistance induced by Smoothened point mutations. Moreover, NL-103 significantly downregulated the expression of Gli2 which plays an important role in Hh pathway. NL-103 may be a promising compound for clinical development as a more effective Hh pathway inhibitor.