| Cas No.: | 1263132-08-6 |
| Chemical Name: | MRT-81 |
| Synonyms: | 3,4,5-trimethoxy-N-[[4-methyl-3-[(4-phenylbenzoyl)amino]phenyl]carbamothioyl]benzamide;MRT-81 |
| SMILES: | C1(C2=CC=CC=C2)=CC=C(C(NC2=CC(NC(=S)NC(=O)C3=CC(OC)=C(OC)C(OC)=C3)=CC=C2C)=O)C=C1 |
| Formula: | C31H29N3O5S |
| M.Wt: | 555.64 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | MRT-81 is a potent antagonist of human and rodent smoothened Smo receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer. |
| Target: | IC50: 41 nM (Shh-light2 cells Smo receptors)[1] |
| In Vitro: | MRT-81 inbihits the differentiation of the mesenchymal pluripotent C3H10T1/2 cells into alkaline phosphatasepositive osteoblasts induced by the Smo agonist SAG (0.1 μM), with an IC50 value of 64 nM[1]. MRT-81 (1-1000 nM) is a potent antagonist of SAG (0.01 μM)-induced proliferation of rat granule cell precursors (GCPs) with an IC50 less than 10 nM[1]. MRT-81 (0, 0.1, 1, 10, 30, 100, 300, 1000 nM, 2 h, 37 °C) blocks BODIPY-cyclopamine (5 nM) binding to hSmo in a dose-dependent manner with an IC50 of 63 nM in HEK-hSmo cells[1]. |
| References: | [1]. Solinas A, et al. Acylthiourea, acylurea, and acylguanidine derivatives with potent hedgehog inhibiting activity. J Med Chem. 2012 Feb 23;55(4):1559-71. |
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| 2018-0101 |
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