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

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

MCE 顾客使用本产品发表的 1 篇科研文献

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

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
10.56 μM
Compound: 4Bb
Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
A549/CDDP IC50
2.65 μM
Compound: 4Bb
Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human A549/DDP cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
MCF7 IC50
6.54 μM
Compound: 4Bb
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
MGC-803 IC50
3.2 μM
Compound: 4Bb
Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
NCI-H460 IC50
2.31 μM
Compound: 4Bb
Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
SK-OV-3 IC50
2.84 μM
Compound: 4Bb
Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human SK-OV-3 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
T-24 IC50
2.9 μM
Compound: 4Bb
Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
Anticancer activity against human T24 cells assessed as inhibition of cell growth incubated for 48 hrs by crystal violet staining based analysis
[PMID: 38657480]
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
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

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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:

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

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