2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Mps1 Apoptosis
  4. Mps1-IN-5

Mps1-IN-5 是一种有效的，具有口服活性的 Mps1 抑制剂，IC50 值为 29 nM。Mps1-IN-5 诱导细胞凋亡 (Apoptosis) 和胞周期停滞在 G2/M 期。Mps1-IN-5 显示出抗增殖活性和抗肿瘤活性。Mps1-IN-5 抑制 Mps1 的磷酸化并诱导 DNA 损伤。

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Mps1-IN-5 Chemical Structure

Mps1-IN-5 Chemical Structure

CAS No. : 2890819-31-3

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Mps1-IN-5 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC50 value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage[1].

IC50 & Target

IC50: 29 nM (Mps1)[1]
体外研究
(In Vitro)

Mps1-IN-5 (compound 12) (0-10 µM,24, 48, 72 h) 以时间依赖性方式抑制 MCF-7 和 4T1 细胞的增殖[1].< br/> Mps1-IN-5 (0, 0.5, 1.0, 5.0 µM; 24, 48 h) 在 MCF-7 和 4T1 细胞中以剂量依赖性方式诱导细胞凋亡和胞周期停滞在 G2/M 期[1] .
Mps1-IN-5 (0, 0.03, 0.1, 1, 3 µM; 2 h) 抑制 Mps1 的磷酸化并诱导 DNA 损伤[1]。

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

Mps1-IN-5 相关抗体:

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells
Concentration: 0-3 µM
Incubation Time: 72 h
Result: Inhibited the cell growth with IC50s of 2.68, 0.37, 0.40, >3, >3, >3, 1.06, 2.03, >3 µM for MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF-7, 4T1 cells
Concentration: 0, 0.5, 1.0, 5.0 µM
Incubation Time: 24 h
Result: Induced cell cycle arrest of MCF-7 and 4T1 cells at the G2/M phase in a dose-dependent manner, decreased the protein expression levels of Cyclin B1 and CDK1.

Apoptosis Analysis[1]

Cell Line: MCF-7, 4T1 cells
Concentration: 0, 0.5, 1.0, 5.0 µM
Incubation Time: 48 h
Result: Induced apoptosis and significantly increased the expression level of an apoptosis-related protein, cleaved poly ADP-ribose polymerase (PARP).

Western Blot Analysis[1]

Cell Line: MCF-7, 4T1 cells
Concentration: 0, 0.03, 0.1, 1, 3 µM
Incubation Time: 2 h
Result: Increased the expression of level of γ-H2AX protein and decreased the protein expression of p-Mps1 in a dose-dependent manner.
体内研究
(In Vivo)

Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) 在乳腺癌模型中抑制肿瘤生长而无明显毒性[1]。

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

Animal Model: 6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)[1]
Dosage: 30, 60 mg/kg
Administration: P.o.; daily for 15 days
Result: Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys.
分子量

439.52

Formula

C24H25N9
CAS 号
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

Mps1-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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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:

Mps1-IN-52890819-31-3Mps1ApoptosisMonopolar spindle 1antiproliferativeanti-tumorMCF-74T1 cellsp-Mps1DNA damageapoptosisG2/M phasebreast cancerInhibitorinhibitorinhibit

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