| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
MRT-10 targets Smoothened (Smo), a seven-transmembrane G protein-coupled receptor that serves as the key transducer of the Hedgehog (Hh) signaling pathway. MRT-10 binds to Smo at the level of the Bodipy-cyclopamine binding site. Cyclopamine is a well-known natural Smo antagonist, and MRT-10's binding at this site suggests a similar mechanism of action. By binding to Smo, MRT-10 blocks its activation and subsequent Hh signaling through the Gli family of transcription factors. Smo is a validated therapeutic target in Hh-driven cancers. MRT-10's IC₅₀ of 0.65 μM in various Hh assays demonstrates its potency as a Smo antagonist.
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| ln Vitro |
In HEK293 cells, MRT-10 suppresses the Smo-induced IP accumulation in a dose-dependent manner (IC50=2.5 μM)[1]. With an IC50=0.5 μM, MRT-10 (10-9-10-5 M; 2 h) inhibits the binding of bodipy-cyclopamine (5 nM; 2 h) to cells expressing mouse Smo in a dose-dependent manner[1]. MRT-10 (10-9-10-5 M; 40 h) has an IC50=0.64 μM and suppresses ShhN signaling in Shh-light2 cells in a dose-dependent manner[1]. MRT-10 (10-9-10-5 M; 6 days) suppresses the alkaline phosphatase (AP) activity in C3H10T1/2 cells that is stimulated by SAG (0.1 μM) (IC50=0.90 μM).
In vitro studies have demonstrated that MRT-10 is a Smo antagonist with an IC₅₀ of 0.65 μM in various Hedgehog assays. The compound inhibits Hh signaling in cell-based assays, blocking Gli-dependent transcription and downstream target gene expression. MRT-10 binds to Smo at the Bodipy-cyclopamine binding site, indicating a similar binding mode to the natural Smo antagonist cyclopamine. In cancer cell lines driven by Hh signaling, MRT-10 treatment results in reduced cell proliferation. The compound's potency and mechanism of action make it a valuable tool for studying Hh signaling and Smo function. |
| ln Vivo |
In vivo activity data for MRT-10 is limited in the available literature, as the compound is primarily used as a research tool in cell-based studies. The compound's Smo antagonism (IC₅₀ = 0.65 μM) suggests it could have therapeutic potential in Hh-driven cancers. However, comprehensive in vivo efficacy studies have not been extensively reported. The compound has been investigated for cancer research applications. Future studies may explore its effects in animal models of Hh-driven malignancies.
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| Enzyme Assay |
Cell-free biochemical assays for MRT-10 typically measure binding to Smo or inhibition of Smo-mediated signaling. A standard protocol involves radioligand binding assays using Bodipy-cyclopamine or [³H]-cyclopamine as the radioligand. Membranes from Smo-expressing cells are incubated with varying concentrations of MRT-10 (0.01-100 μM) and the radioligand, and bound fluorescence or radioactivity is measured. IC₅₀ values are determined from competition binding curves using nonlinear regression analysis. Assays are performed in triplicate with appropriate positive and negative controls. The compound's purity and identity are verified by HPLC and NMR spectroscopy.
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| Cell Assay |
Cellular assays for MRT-10 typically use Hh-responsive cell lines to assess inhibition of Smo signaling. A standard protocol involves culturing Shh-light2 cells or other Hh-responsive cells in 96-well plates, treating with MRT-10 at concentrations ranging from 0.01-100 μM for 24-48 hours, and stimulating with Shh ligand or Smo agonists. Hh signaling activity is assessed using Gli-luciferase reporter assays or by measuring expression of Gli target genes (e.g., Gli1, PTCH1) by qPCR. Cell proliferation is assessed by MTT or CellTiter-Glo assays. The compound's binding at the Bodipy-cyclopamine site can be confirmed by competition with fluorescently labeled cyclopamine.
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| Animal Protocol |
In vivo studies with MRT-10 are limited, as the compound is primarily a research tool for in vitro applications. If conducted, a typical protocol might involve administration of MRT-10 to rodents by intraperitoneal or oral administration, followed by assessment of Hh signaling in target tissues. Tissues would be collected at various time points and analyzed for Hh target gene expression by qPCR and for tumor growth inhibition in xenograft models. However, comprehensive in vivo efficacy studies have not been extensively reported for this compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MRT-10 is limited, as the compound is primarily used in research settings. The compound's molecular weight is 465.52 g/mol. The compound's physicochemical properties suggest moderate lipophilicity. For in vivo applications, the compound would likely require formulation to enhance bioavailability. The compound is typically dissolved in DMSO for in vitro studies. Metabolism and clearance pathways have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Toxicological data specific to MRT-10 is limited, as the compound is a research chemical used primarily in in vitro settings. At effective concentrations (0.65 μM for Smo inhibition), the compound does not show significant cytotoxicity in most cell types. Higher concentrations may have off-target effects or cytotoxicity. As with all Smo antagonists, potential toxicity could arise from inhibition of Hh signaling in tissues where the pathway is important for homeostasis. Standard laboratory safety precautions should be observed when handling this compound.
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| References |
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| Additional Infomation |
MRT-10 is a research compound and not an approved drug. No clinical trials or regulatory approvals exist for this compound. It is commercially available from various suppliers for research use only. The compound's primary value lies in its utility as a pharmacological tool for studying Smo function and Hh signaling. With an IC₅₀ of 0.65 μM, MRT-10 is a potent Smo antagonist that binds at the Bodipy-cyclopamine binding site, enabling researchers to study the roles of Hh signaling in development, cancer, and other biological processes. Its mechanism of action is similar to that of the natural Smo antagonist cyclopamine.
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| Molecular Formula |
C24H23N3O5S
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| Molecular Weight |
465.52
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| Exact Mass |
465.136
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| CAS # |
330829-30-6
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| PubChem CID |
1139102
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| Appearance |
White to off-white solid powder
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| LogP |
5.27
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
659
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=CC(=CC(=C1OC)OC)C(=O)NC(=S)NC2=CC=CC(=C2)NC(=O)C3=CC=CC=C3
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| InChi Key |
KVQVEZQDNHMQJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23N3O5S/c1-30-19-12-16(13-20(31-2)21(19)32-3)23(29)27-24(33)26-18-11-7-10-17(14-18)25-22(28)15-8-5-4-6-9-15/h4-14H,1-3H3,(H,25,28)(H2,26,27,29,33)
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| Chemical Name |
N-[(3-benzamidophenyl)carbamothioyl]-3,4,5-trimethoxybenzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (214.81 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1481 mL | 10.7407 mL | 21.4814 mL | |
| 5 mM | 0.4296 mL | 2.1481 mL | 4.2963 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1481 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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