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

MT-125 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 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma[1].

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

MT-125 Chemical Structure

MT-125 Chemical Structure

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Description

MT-125 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 can pass through the blood-brain barrier. MT-125 induces ferroptosis and DNA damage by increasing the levels of reactive oxygen species (ROS) within tumor cells. MT-125 can enhance the PDGFR signaling pathway. MT-125 can be used for research on glioblastoma[1].

IC50 & Target

PDGFRα

 

In Vitro

MT-125 (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 (5 μM, 48 h) leads to 12 %-25 % cell multinucleation in 10 human GBM cells[1].
MT-125 (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 (4 μM) can induce ferroptosis and ferroptosis inhibitors can reverse its cytotoxicity in Trp53(‒/‒) cells[1].
MT-125 (5 μM, 48 h) significantly increase PDGFRα expression and activation of downstream signaling pathways in Trp53(‒/‒) cells[1].
MT-125 (5 μM, 48 h) regulates the MAPK signaling pathway by inhibiting NMIIA in Trp53(‒/‒) cells[1].
MT-125 (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 (10 mg/kg; s.c.; once daily; for 2 weeks) demonstrates low toxicity in vivo for the C57BL/6 mice[1].
MT-125 (20 or 40 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 (7.5, 15, or 30 mg/kg; s.c.; once daily; for 28 days) maintain good tolerability in repeated dose toxicology studies in the C57BL/6 mice[1].
MT-125 (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 or 40 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: C57BL/6 mice (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.
Molecular Weight

393.87

Formula

C22H20ClN3O2

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.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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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Product Name:
MT-125
Cat. No.:
HY-174406
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