3,4,5-trimethoxy-N-[[4-methyl-3-[(4-phenylbenzoyl)amino]phenyl]carbamothioyl]benzamide

Biological Activity

MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer[1]. MRT-81 inbihits the differentiation of the mesenchymal pluripotent C3H10T1/2 cells into alkaline phosphatasepositive osteoblasts induced by the Smo agonist SAG (0.1 μM), with an IC50 value of 64 nM[1].MRT-81 (1-1000 nM) is a potent antagonist of SAG (0.01 μM)-induced proliferation of rat granule cell precursors (GCPs) with an IC50 less than 10 nM[1].MRT-81 (0, 0.1, 1, 10, 30, 100, 300, 1000 nM; 2 h; 37 °C) blocks BODIPY-cyclopamine (5 nM) binding to hSmo in a dose-dependent manner with an IC50 of 63 nM in HEK-hSmo cells[1].

References

[1]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71.