MRT-10

Names

[ Name ]:
MRT-10

[Synonym ]:
N-[[[3-(benzoylamino)phenyl]amino]thioxomethyl]-3,4,5-methoxy-benzamide
Immethridine dihydrobromide
MRT-10
N-(3-benzamidophenylcarbamothioyl)-3,4,5-trimethoxybenzamide

Biological Activity

[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].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> Smo

Research Areas >> Cancer

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₃N₃O₅S

[ Molecular Weight ]:
465.52200

[ Exact Mass ]:
465.13600

[ PSA ]:
144.03000

[ LogP ]:
5.27080

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS05, GHS09

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H318-H410

[ Precautionary Statements ]:
P273-P280-P305 + P351 + P338-P501

[ RIDADR ]:
UN 3077 9 / PGIII

Synthetic Route

Click to get detail synthetic route

Related Compounds

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