1. Cytoskeleton Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  2. Myosin PDGFR Reactive Oxygen Species (ROS) Ferroptosis Akt mTOR ERK
  3. MT-125 free base

MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma.

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

MT-125 free base

MT-125 free base Chemical Structure

CAS No. : 2404652-80-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
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10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

MT-125 free base is a specific and well-tolerated inhibitor of non-muscle myosin IIA (Ki,NMIIA = 2.7 μM) and IIB (EC50 = 1.7 μM). MT-125 free base can pass through the blood-brain barrier. MT-125 free base induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 free base can enhance the PDGFR signaling pathway. MT-125 free base can be used for research on glioblastoma[1].

IC50 & Target[1]

PDGFRα

 

In Vitro

MT-125 free base (5 μM, 8 h) significantly inhibits the invasive ability of one murine (MES1861) and three human (187, 190, and L1) Glioblastoma (GBM) cell lines[1].
MT-125 free base (5 μM, 48 h) leads to 12 %-25 % cell multinucleation in 10 human GBM cells[1].
MT-125 free base (0.1-10 μM; 96 h) produces over 90 % cytotoxicity in various mouse and human GBM cell lines[1].
MT-125 increase reactive oxygen species (ROS) and lipid peroxidation levels in L1 cells[1].
MT-125 free base (4 μM) can induce ferroptosis and ferroptosis inhibitors can reverse its cytotoxicity in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) significantly increase PDGFRα expression and activation of downstream signaling pathways in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) regulates the MAPK signaling pathway by inhibiting NMIIA in Trp53(-/-) cells[1].
MT-125 free base (5 μM, 48 h) exhibits synergistic effects with carcinogenic kinase inhibitors in Trp53(-/-) cells[1].

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

Cell Viability Assay[1]

Cell Line: murine (TRP53(-/-), Pten(-/-), TRP53/Pten(-/-)) and human (L1, L0, GBM1A, 612, QNS120, QNS166, QNS315) GBM cell lines
Concentration: 3.3-7.3 μM
Incubation Time: 96 h
Result: Significantly inhibited the GBM cell lines.

Western Blot Analysis[1]

Cell Line: Trp53(‒/‒) cells
Concentration: 5 μM
Incubation Time: 48 h
Result: Effectively enhanced activation of PDGFRα, AKT, mTOR, ERK1/2, and SRC.
In Vivo

MT-125 free base (10 mg/kg; s.c.; once daily; for 2 weeks) demonstrates low toxicity in vivo for the C57BL/6 mice[1].
MT-125 free base (20 mg/kg, s.c.; once daily; for 7 days) does not cause any adverse effects related to medication and does not affect age-related weight changes in the C57BL/6 mice[1].
MT-125 free base (7.5, 15, or 30 mg/kg; s.c.; once daily; for 28 days) maintain good tolerability in repeated dose toxicology studies in the female rats[1].
MT-125 free base (10 mg/kg; i.p.; once daily; for 4 weeks) synergizes with oncogenic kinase inhibitors and can significantly inhibit the growth of tumor cells in the C57BL/6 mice with Trp53(?/?) tumors[1].

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

Animal Model: C57BL/6 mice (8-10 weeks; 25-35 g)[1]
Dosage: 10 mg/kg
Administration: Subcutaneous injection (s.c.); once daily for 2 weeks
Result: Had good tolerance and the weight and hematological indicators of mice were within normal range.
Animal Model: C57BL/6 mice (8-10 weeks; 25-35 g)[1]
Dosage: 20 mg/kg
Administration: Subcutaneous injection (s.c.); once daily for 7 days
Result: Maintained normal body weight and hematological parameters within the normal range in mice.
Animal Model: Female rats (8-10 weeks; 25-35 g)[1]
Dosage: 7.5, 15, or 30 mg/kg
Administration: Subcutaneous injection (s.c.); once daily for 28 days
Result: Did not cause any obvious or lasting adverse health effects.
Animal Model: C57BL/6 mice with Trp53(‒/‒) tumors (8-10 weeks; 25-35 g)[1]
Dosage: 10 mg/kg, co-incubation with Paxalisib (HY-19962)
Administration: Intraperitoneal injection (i.p.); once daily for 4 weeks
Result: Markedly reduced tumor size to an isolated nest of HA-positive cells and prolonged survival rate.
Clinical Trial
Molecular Weight

357.41

Formula

C22H19N3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC2=C(N=C(N(C3=CC4=C(N=C(C)C=C4)C=C3)CC5)[C@]5(O)C2=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (93.25 mM; ultrasonic and warming and heat to 60°C; 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 2.7979 mL 13.9895 mL 27.9791 mL
5 mM 0.5596 mL 2.7979 mL 5.5958 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 (sealed storage, away from moisture). 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3.33 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (33.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 3.33 mg/mL (9.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.33 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 (33.3 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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mg/kg

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g

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(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 +
+
%
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%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

Purity: 98.67% ee.: 98.08%

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 (sealed storage, away from moisture). 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 2.7979 mL 13.9895 mL 27.9791 mL 69.9477 mL
5 mM 0.5596 mL 2.7979 mL 5.5958 mL 13.9895 mL
10 mM 0.2798 mL 1.3990 mL 2.7979 mL 6.9948 mL
15 mM 0.1865 mL 0.9326 mL 1.8653 mL 4.6632 mL
20 mM 0.1399 mL 0.6995 mL 1.3990 mL 3.4974 mL
25 mM 0.1119 mL 0.5596 mL 1.1192 mL 2.7979 mL
30 mM 0.0933 mL 0.4663 mL 0.9326 mL 2.3316 mL
40 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7487 mL
50 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3990 mL
60 mM 0.0466 mL 0.2332 mL 0.4663 mL 1.1658 mL
80 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
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  • 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.

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MT-125 free base
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