2. Stem Cell/Wnt
  3. Smo
  4. MRT-81

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.

For research use only. We do not sell to patients.

MRT-81 Chemical Structure

MRT-81 Chemical Structure

CAS No. : 1263132-08-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 244 In-stock
Solution
10 mM * 1 mL in DMSO USD 244 In-stock
Solid
5 mg USD 200 In-stock
10 mg USD 300 In-stock
25 mg USD 540 In-stock
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Based on 1 publication(s) in Google Scholar

MRT-81 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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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[1].

IC50 & Target

IC50: 41 nM (Shh-light2 cells Smo receptors)[1]
Cellular Effect
Cell Line Type Value Description References
C3H 10T1/2 IC50
0.06 μM
Compound: 61
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
63 nM
Compound: 61
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]
Shh Light II IC50
0.041 μM
Compound: 61
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]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MRT-81 Related Antibodies
Molecular Weight

555.64

Formula

C31H29N3O5S
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=C(C2=CC=CC=C2)C=C1)NC3=CC(NC(NC(C4=CC(OC)=C(C(OC)=C4)OC)=O)=S)=CC=C3C
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
In Vitro: 

DMSO : 100 mg/mL (179.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7997 mL 8.9986 mL 17.9973 mL
5 mM 0.3599 mL 1.7997 mL 3.5995 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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 1.7997 mL 8.9986 mL 17.9973 mL 44.9932 mL
5 mM 0.3599 mL 1.7997 mL 3.5995 mL 8.9986 mL
10 mM 0.1800 mL 0.8999 mL 1.7997 mL 4.4993 mL
15 mM 0.1200 mL 0.5999 mL 1.1998 mL 2.9995 mL
20 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2497 mL
25 mM 0.0720 mL 0.3599 mL 0.7199 mL 1.7997 mL
30 mM 0.0600 mL 0.3000 mL 0.5999 mL 1.4998 mL
40 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
50 mM 0.0360 mL 0.1800 mL 0.3599 mL 0.8999 mL
60 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7499 mL
80 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
100 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4499 mL
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MRT-81 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRT-811263132-08-6MRT81MRT 81SmoSmoothenedhumanrodentShh-light2 cellsC3H10T1/2 cellsrat granule cell precursorsBODIPY-cyclopamineInhibitorinhibitorinhibit

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