MRT-83 (C09-1152-193)

MRT-83 is a potent antagonist of Smo , with an IC 50 in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.In VitroMRT-83 displays full antagonist properties with an IC 50 (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC 50 ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC 50 of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC 50 of 14 nM, which is in good correlation with its IC 50 in the Shh-light2 and alkaline phosphatase assays. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAnimals 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:Smo. Specifications and Purity: 99%. Molecular Formula: C31H30N4O5. Molecular Weight: 538.59. PubChem CID: 136210511. Isomeric SMILES: CC1=C(C=C(C=C1)N=C(N)NC(=O)C2=CC(=C(C(=C2)OC)OC)OC)NC(=O)C3=CC=C(C=C3)C4=CC=CC=C4.