MRT-10
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 98.99%
- CAS No.: 330829-30-6
- Formula: C24H23N3O5S
- Molecular Weight:465.52
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Cancer Stem Cells Compound Library
HY-L135
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Bioactive Compound Library
HY-L001
-
Protein Kinase Compound Library
HY-L196
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| C3H 10T1/2 | IC50 |
0.868 μM
Compound: 2; MRT-10
|
Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
Inhibition of hedgehog signalling in mouse C3H10T1/2 cells assessed as reduction in Smo agonist SAG induced cell differentiation into alkaline phosphatase-positive osteoblasts using pNp substrate incubated for 72 hrs
|
10.1039/C5MD00092K |
| C3H 10T1/2 | IC50 |
0.9 μM
Compound: 1a
|
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs
|
[PMID: 22268551] |
| HEK293 | IC50 |
0.281 μM
Compound: 2; MRT-10
|
Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
Displacement of boron-dipyrromethene-cyclopamine from human smoothened receptor expressed in HEK293 cells incubated for 4 hrs by hSMO-BC binding assay
|
10.1039/C5MD00092K |
| HEK293 | IC50 |
300 nM
Compound: 1a
|
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy
|
[PMID: 22268551] |
| HT-29 | IC50 |
6.61 μM
Compound: 2; MRT-10
|
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition after 48 hrs by MTT assay
|
10.1039/C5MD00092K |
| MGC-803 | IC50 |
8.62 μM
Compound: 2; MRT-10
|
Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human MGC803 cells assessed as cell growth inhibition after 48 hrs by MTT assay
|
10.1039/C5MD00092K |
| Shh Light II | IC50 |
0.65 μM
Compound: 1a
|
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay
|
[PMID: 22268551] |
| SW-620 | IC50 |
21.23 μM
Compound: 2; MRT-10
|
Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
Antiproliferative activity against human SW620 cells assessed as cell growth inhibition after 48 hrs by MTT assay
|
10.1039/C5MD00092K |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 330829-30-6
-
Appearance Solid
-
Molecular Weight 465.52
-
Formula C24H23N3O5S
-
Color White to light yellow
-
SMILES
O=C(NC(NC1=CC=CC(NC(C2=CC=CC=C2)=O)=C1)=S)C3=CC(OC)=C(OC)C(OC)=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (214.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (271 KB)
-
SDS (560 KB)
- English - EN (560 KB)
- Français - FR (560 KB)
- Deutsch - DE (560 KB)
- Norwegian - NO (560 KB)
- Español - ES (560 KB)
- Swedish - SV (560 KB)
- Italian - IT (560 KB)
- Korean - KR (560 KB)
- Portuguese - PT (560 KB)
-
Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1481 mL | 10.7407 mL | 21.4814 mL | 53.7034 mL |
| 5 mM | 0.4296 mL | 2.1481 mL | 4.2963 mL | 10.7407 mL | |
| 10 mM | 0.2148 mL | 1.0741 mL | 2.1481 mL | 5.3703 mL | |
| 15 mM | 0.1432 mL | 0.7160 mL | 1.4321 mL | 3.5802 mL | |
| 20 mM | 0.1074 mL | 0.5370 mL | 1.0741 mL | 2.6852 mL | |
| 25 mM | 0.0859 mL | 0.4296 mL | 0.8593 mL | 2.1481 mL | |
| 30 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7901 mL | |
| 40 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3426 mL | |
| 50 mM | 0.0430 mL | 0.2148 mL | 0.4296 mL | 1.0741 mL | |
| 60 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8951 mL | |
| 80 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL | |
| 100 mM | 0.0215 mL | 0.1074 mL | 0.2148 mL | 0.5370 mL |
MRT-10 Related Classifications
HY-108507 Related Classifications
Powered by Bioz