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MRT-10

  Cat. No.:  DC43413   Featured
Chemical Structure
330829-30-6
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Field of application
MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 330829-30-6
Chemical Name: N-[(3-benzamidophenyl)carbamothioyl]-3,4,5-trimethoxybenzamide
Synonyms: N-[(3-benzamidophenyl)carbamothioyl]-3,4,5-trimethoxybenzamide;N-(3-benzamidophenylcarbamothioyl)-3,4,5-trimethoxybenzamide;STK099293;MRT-10;Oprea1_307096;ARONIS27184;CHEMBL2031084;N-[[[3-(benzoylamino)phenyl]amino]thioxomethyl]-3,4,5-methoxy-benzamide;MRT 10;AG-690;N-[[[3-[(Benzoyl)amino]phenyl]amino](thioxo)methyl]-3,4,5-trimethoxybenzamide
SMILES: C(NC1=CC=CC(NC(NC(=O)C2C=C(OC)C(OC)=C(OC)C=2)=S)=C1)(=O)C1C=CC=CC=1
Formula: C24H23N3O5S
M.Wt: 465.52
Purity: >98%
Sotrage: 0°C (short term), -20°C (long term), desiccated
Description: MRT-10 is a seven-transmembrane receptor smoothened (Smo) antagonist with an IC50 of 0.65 μM in the micromolar range in various Hedgehog (Hh) assays. MRT-10 binds to the Smo receptor at the level of the Bodipycyclopamine binding site. MRT-10 can be used for the research of cancer[1][2].
In Vitro: MRT-10 inhibits the Smo-induced IP accumulation in a dosedependent manner (IC50=2.5 μM) in HEK293 cells[1]. MRT-10 (10-9-10-5 M; 2 h) blocks Bodipy-cyclopamine (5 nM; 2 h) binding to cells expressing mouse Smo in a dosedependent manner with an IC50=0.5 μM[1]. MRT-10 (10-9-10-5 M; 40 h) inhibits ShhN signaling in Shh-light2 cells in a dose-dependent manner with an IC50=0.64 μM[1]. MRT-10 (10-9-10-5 M; 6 days) inhibits the SAG-induced (0.1 μM) alkaline phosphatase (AP) activity with an IC50=0.90 μM ) in C3H10T1/2 cells[1].
References: [1]. Manetti F, et al. Virtual screening-based discovery and mechanistic characterization of the acylthiourea MRT-10 family as smoothened antagonists. Mol Pharmacol. 2010 Oct;78(4):658-65. [2]. 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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