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MRT-83

CAS No. : 1263131-92-5

MCE 站：MRT-83

产品活性：MRT-83 是有效的 Smo 拮抗剂，其 IC₅₀ 值在纳摩尔级别。MRT-83 也抑制 Hedgehog (Hh) 信号通路。

研究领域：Stem Cell/Wnt

作用靶点：Smo

In Vitro: 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.

In Vivo: 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.

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