MRT-81

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].

Signaling Pathways >> Stem Cell/Wnt >> Smo

Research Areas >> Cancer

IC50: 41 nM (Shh-light2 cells Smo receptors)[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].

[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.