Smoothened (Smo) receptor antagonist (IC50
= 0.5 μ
M in HEK293 cells transiently expressing mouse Smo). Inhibits ShhN-induced Gli luciferase reporter activity in Shh-light 2 cells (IC50
= 2.5 μ
M); acts as an inverse agonist during nontranscriptional Hedgehog pathway activation (IC50
= 2.5 μ
M in HEK293 cells).
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All Tocris products are intended for laboratory research use only.
Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity.
Solinas et al.
Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists.
Manetti et al.