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

MT-125 是一种特异性和耐受性良好的非肌肉肌球蛋白 myosin IIA (Ki,NMIIA = 2.7 μM) 和 IIB (EC50 = 1.7 μM) 抑制剂。MT-125 可以穿过血脑屏障。MT-125 通过增加肿瘤细胞内的活性氧 (ROS) 水平诱导铁死亡 ferroptosis 和 DNA 损伤。MT-125 可以增强 PDGFR 信号通路。MT-125 可用于胶质母细胞瘤的研究[1]。

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MT-125 Chemical Structure

MT-125 Chemical Structure

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MT-125 相关抗体

Top Publications Citing Use of Products

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PDGFR PDGFRβ PDGFRα

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Akt Akt1 Akt2 Akt3

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mTOR mTORC1 mTORC2

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

MT-125 (5 μM，8 小时) 显著抑制了一种小鼠 (MES1861) 和三种人类 (187、190和L1) GBM 细胞系的侵袭能力[1]。
MT-125 (5 μM，48 小时) 在 10 种人 GBM 细胞中导致 12 %-25 % 的细胞多核化[1]。
MT-125 (0.1-10 μM；96 小时) 在各种小鼠和人类 GBM 细胞系中产生 90 % 以上的细胞毒性[1]。
MT-125 增加 L1 细胞中的活性氧 (ROS) 和脂质过氧化水平[1]。
MT-125 (4 μM) 可诱导 Trp53(‒/‒) 细胞的铁死亡，铁死亡抑制剂可逆转其细胞毒性[1] 。
MT-125 (5 μM，48 小时) 显著增加 Trp53(‒/‒) 细胞的 PDGFRα 的表达和下游信号通路的激活[1]。
MT-125 (5 μM，48 小时) 在 Trp53(‒/‒) 细胞中通过抑制 NMIIA 调节 MAPK 信号通路[1]。
MT-125 (5 μM，48 小时) 与 Trp53(‒/‒) 细胞中的致癌激酶抑制剂显示出协同作用[1]。

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

MT-125 相关抗体:

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.
体内研究
(In Vivo)

MT-125 (10 mg/kg；皮下注射；每日一次；持续 2 周) 在 C57BL/6 小鼠体内表现出低毒性[1]。
MT-125 (20 或 40 mg/kg，皮下注射；每天一次；持续 7 天) 在 C57BL/6 小鼠体内不会引起任何与药物有关的不良反应，也不会影响与年龄相关的体重变化[1]。
MT-125 (7.5，15 或 30 mg/kg；皮下注射；每日一次；持续 28 天) 对 C57BL/6 小鼠在重复剂量毒理学研究中保持良好的耐受性[1]。
MT-125 (10 mg/kg；腹腔注射；每天一次；持续 4 周) 在胶质母细胞瘤 C57BL/6 小鼠体内与致癌激酶抑制剂协同作用，可以显著抑制肿瘤细胞的生长[1]。

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.
分子量

393.87

Formula

C22H20ClN3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MT-125 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

MT-125MT125MT 125PDGFRReactive Oxygen Species (ROS)FerroptosisMyosinAktmTORERKPlatelet-derived growth factor receptorPKBProtein kinase BMammalian target of RapamycinExtracellular signal regulated kinasesferroptosisROSanticancerglioblastomaMAPKPI3KInhibitorinhibitorinhibit

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