1. Cell Cycle/DNA Damage Apoptosis
  2. Polo-like Kinase (PLK) Apoptosis
  3. YLT-11

YLT-11 是一种有效的选择性和具有口服活性的 PLK4 抑制剂,对 PLK1、PLK2、PLK3、PLK4的 Kd 值分别为 >10000、653、>10000、5.2 nM。YLT-11 显示出抗增殖活性。YLT-11 诱导细胞凋亡 (Apoptosis) 细胞周期停滞在 G2/M 期。YLT-11 具有抗癌活性。

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YLT-11 Chemical Structure

YLT-11 Chemical Structure

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查看 Polo-like Kinase (PLK) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YLT-11 is a potent, selective and orally active PLK4 inhibitor with Kd values of >10000, 653, >10000, 5.2 nM for PLK1, PLK2, PLK3, PLK4, respectively. YLT-11 shows antiproliferative activity. YLT-11 induces Apoptosis and cell cycle arrest at G2/M phase. YLT-11 show anticancer activity[1].

IC50 & Target[1]

PLK4

5.2 nM (Kd)

PLK2

653 nM (Kd)

PLK1

>10000 nM (Kd)

PLK3

>10000 nM (Kd)

体外研究
(In Vitro)

YLT-11 (0-1 µM; 48 h) 以剂量依赖性方式降低 p-PLK4 的表达[1]
YLT-11 (0-0.5 µM; 0-48 h) 诱导细胞凋亡和细胞周期停滞在 G2/M 期[1]

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468, BT549, MCF-7 cells
Concentration: 0-10 µM
Incubation Time: 24-96 h
Result: Showed antiproliferative activity in a time-dependent and concentration-dependent manner with IC50s of 120, 68, 73, 74 nM for MDA-MB-231, MDA-MB-468, BT549, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0, 0.25, 0.5, 1 µM
Incubation Time: 48 h
Result: Decreased the expression of p-PLK4 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0.25 µM
Incubation Time: 0-48 h
Result: Induced cell cycle arrest at G2/M phase.

Apoptosis Analysis[1]

Cell Line: MDA-MB-468, MDA-MB-231 cells
Concentration: 0, 0.125, 0.25, 0.5 µM
Incubation Time: 24, 48 h
Result: Induced apoptosis of cancer cells in a time-dependent and concentration-dependent manner with the expression of cleaved caspase-3 and cleaved PARP1 increased.
体内研究
(In Vivo)

YLT-11 (30、90 mg/kg;口服;每日一次,持续 20 天) 在小鼠体内显示出抗癌活性[1]

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

Animal Model: Six-week-old female BALB/c nude mice[1]
Dosage: 30, 90 mg/kg
Administration: P.o.; daily for 20 days
Result: Remarkably inhibited the growth of tumor xenografts in a dose-dependent manner.
分子量

412.49

Formula

C24H24N6O

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
YLT-11
目录号:
HY-115589
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