MRT-92 is a potent selective Smoothened (Smo) receptor antagonist (Kd=0.3 nM), inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation with IC50 of 0.4 nM.
MRT-92 blocked both SAG (0.1 µM) and GSA-10 (1 µM) induced differentiation of C3H10T1/2 cells with IC50 of 0.006 and 1 uM, respectively.
MRT-92 displayed an IC50 of 5.6 nM for SAG induction of AP response, selectively blocks SmoSAG-induced AP response in C3H10T1/2 cells.
MRT-92 abrogated Smo ciliary translocation promoted by SAG in primary cilium of NIH3T3 cells.
MRT-92 did not block Wnt signaling.
MRT-92 inhibited rat GCPs and Shh medulloblastoma cell proliferation.
