mrt-92 hcl

MRT-92 is a potent and selective Smoothened (Smo) receptor inhibitor. MRT-92 displays subnanomolar antagonist activity against Smo in various Hh cell-based assays. MRT-92 inhibits rodent cerebellar granule cell proliferation induced by Hh pathway activation through pharmacologic (half maximal inhibitory concentration [IC50] = 0.4 nM) or genetic manipulation. Smo is the target of anticancer drugs that bind to a long and narrow cavity in the 7-transmembrane (7TM) domain.

MRT-92 是一种针对Smoothened(Smo)的拮抗剂，具备抗癌特性 (Ki=0.7 nM)。其作用机理主要是通过阻断Smoothened受体跨膜域的重叠结合位点，抑制Hedgehog信号通路，进而影响啮齿动物小脑颗粒细胞的增殖 (IC50=0.4 nM)。该化合物广泛应用于小脑神经胶质瘤的科研领域。