产品
编 号:F103070
分子式:C31H30N4O5
分子量:538.59
产品类型
结构图
CAS No: 1263131-92-5
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产品详情
生物活性:
MRT-83 is a potent antagonist of Smo, with an IC50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.
体内研究:
Animals treated with ShhN in the presence of MRT-83 are as healthy as those of the other groups but up-regulation of Ptc transcription in the SVZ of these animals is no longer observed in agreement with a complete inhibition of ShhN-mediated effects (8.7±2.4 Ptc+ cells/section, n=9) and is not different from vehicle-mediated effects. MRT-83 but not MRT-36 antagonizes the up-regulation of Ptc transcription induced by ShhN in vivo in the SVZ of the LV.
体外研究:
MRT-83 displays full antagonist properties with an IC50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC50 of 14 nM, which is in good correlation with its IC50 in the Shh-light2 and alkaline phosphatase assays.