2. Cell Cycle/DNA Damage
  3. Polo-like Kinase (PLK)
  4. PLK1-IN-10

PLK1-IN-10 (Compound 4Bb) 是一种口服有效的 PLK1 PBD (polo-box 域) 抑制剂。PLK1-IN-10 阻断了 PLK1 与细胞分裂调节蛋白 1 (PRC1) 的相互作用，调低 CDK1-Cyclin B1 复合物的蛋白表达。PLK1-IN-10 与谷胱甘肽 (GSH) 发生反应，增加细胞氧化应激，最终导致细胞死亡。

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PLK1-IN-10 Chemical Structure

PLK1-IN-10 Chemical Structure

CAS No. : 2991469-21-5

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PLK1-IN-10 相关抗体

Top Publications Citing Use of Products

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型
PLK1 PLK2 PLK3 PLK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PLK1-IN-10 (Compound 4Bb) is an orally active PLK1 PBD (polo-box domain) inhibitor. PLK1-IN-10 blocks the interaction of PLK1 with the cell division regulator protein 1 (PRC1) and decreases the protein expression of the CDK1-Cyclin B1 complex. PLK1-IN-10 reacts with glutathione (GSH) to increase cellular oxidative stress, ultimately leading to cell death[1].

IC50 & Target

PLK1 PBD

 

体外研究
(In Vitro)

PLK1-IN-10 (0-6 μM; 48 h) 诱导 A549 和 A549/DDP 的细胞周期停滞在 G2/M 期，抑制细胞增殖[1]。
PLK1-IN-10 (20 μM) 能够在不同温度范围内稳定 A549/DDP 的 PLK1 蛋白[1]。
PLK1-IN-10 (5 μM; 24 h) 与 GSH 反应，产生剂量和时间依赖性的荧光响应，A549/DDP 细胞内荧光强度更高[1]。
PLK1-IN-10 (0-9 μM; 48 h) 增加 A549/DDP 胞内 ROS 水平[1]。
PLK1-IN-10 (10 μM; 48 h) 抑制 PLK1 与 PRC1 的相互作用，出现多核现象[1]。
PLK1-IN-10 对 NCI–H1975 细胞的抗癌活性为 IC50=7.83 μM[1]。

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

PLK1-IN-10 相关抗体:

Western Blot Analysis[1]

Cell Line: A549, A549/DDP
Concentration: 0, 1.5, 3, 6 μM
Incubation Time: 48 h
Result: Downregulated the expression of PLK1, CDK1, Cyclin B1, as well as significantly downregulated the expression of the CDK1-Cyclin B1 complex and Cdc25 protein.

Cell Cycle Analysis[1]

Cell Line: A549, A549/DDP
Concentration: 0, 1.5, 3, 6 μM
Incubation Time: 48 h
Result: Significantly increased the number of A549 and A549/DDP cells in the G2/M phase, inducing mitotic catastrophe.
体内研究
(In Vivo)

PLK1-IN-10 (30, 50 mg/kg; i.p.; 每两天一次,持续 32 天) 显著抑制 A549/DDP 耐药异种移植老鼠的肿瘤生长，50 mg/kg 组甚至导致肿瘤回归[1]。
PLK1-IN-10 (30 mg/kg; p.o.; 每两天一次,持续 20 天) 有效抑制 NCI–H1975 耐药异种移植老鼠的肿瘤生长[1]。

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

Animal Model: A549/DDP drug-resistant xenograft mice[1]
Dosage: 30, 50 mg/kg
Administration: i.p.; once every two days for 32 days
Result: TGI reached 42% for the 30 mg/kg group and 62% for the 50 mg/kg group.
Extended the median survival time from 38 days in the control group to 53 days in the 30 mg/kg group and 62 days in the 50 mg/kg group.
Had no significant impact on the body weight and major organs of the mice, except for a slight difference in heart index observed in the 30 mg/kg group.
Significantly reduced the number of Ki-67 positive cells in the tumor tissue.
Showed no significant differences in H&E staining of major organs, further confirming its good biosafety.
Animal Model: NCI-H1975 drug-resistant xenograft mice[1]
Dosage: 30 mg/kg
Administration: p.o.; once every two days for 20 days
Result: TGI reached 44%. Caused no harm to the body weight and major organs of the mice.
分子量

455.50

Formula

C23H22FN3O4S
CAS 号
非同位 CAS

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

PLK1-IN-10 相关分类

  • 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)

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

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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.

Keywords:

PLK1-IN-102991469-21-5Polo-like Kinase (PLK)Drug resistanceMitotic catastropheCell redox homeostasiscancerCell Cycle ArrestGSH DepletionOxidative Stress InducerMitotic CatastropheInhibitorinhibitorinhibit

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