2. Cell Cycle/DNA Damage Epigenetics
  3. CDK Aurora Kinase
  4. CDK1-IN-9

CDK1-IN-9 是一种具有口服活性的 CDK1 选择性抑制剂，其 IC50 值为 5.5 nM。CDK1-IN-9 具有广泛的抗增殖活性，尤其对 HCT116 结肠癌细胞有效。CDK1-IN-9 可诱导 G2/M 期阻滞，并下调 CDK1、cyclin B1 和复制起始因子 CDC45 的表达。CDK1-IN-9 可诱导严重的 DNA 复制应激，进而激活 p53 信号通路，最终触发细胞凋亡 (apoptosis)。CDK1-IN-9 可用于结肠癌、肝癌和胃癌的研究。

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CDK1-IN-9

CDK1-IN-9 Chemical Structure

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CDK1-IN-9 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK1-IN-9 is an orally active and selective CDK1 inhibitor with an IC50 of 5.5 nM. CDK1-IN-9 exhibits broad antiproliferative activity, particularly against HCT116 colon cancer cells. CDK1-IN-9 induces G2/M phase arrest and downregulates CDK1, cyclin B1, and the replication initiation factor CDC45. CDK1-IN-9 induces severe DNA replication stress, subsequently activating the p53 signaling pathway to trigger apoptosis. CDK1-IN-9 can be used for research on colon cancer, liver cancer and gastric cancer[1].

IC50 & Target[1]

CDK1/cyclinB1

5.5 nM (IC50)

CDK2/cyclinE

25.9 nM (IC50)

CDK4/cyclin D

402.8 nM (IC50)

Aurora A

77.8 nM (IC50)

体外研究
(In Vitro)

CDK1-IN-9 (compound 11I) (0.1-5 μM；24-72 小时) 在 HCT116 细胞系、HepG2 细胞系、SGC7901 细胞系和正常角质形成细胞系 HaCaT 中分别表现出 0.023 μM、0.292 μM、0.360 μM 和 0.566 μM 的 IC50 值[1]。
CDK1-IN-9 (0.1-0.5 μM；3 天) 可显著抑制 HCT116 细胞系、HepG2 细胞系和 SGC7901 细胞系的克隆形成能力[1]。
CDK1-IN-9 (0.5 μM；24-48 小时) 可显著抑制 HCT116 细胞的迁移能力[1]。
CDK1-IN-9 (0.01-0.1 μM；72 小时) 可诱导 HCT116 细胞系发生 G2/M 期阻滞[1]。
CDK1-IN-9 (0.1-0.5 μM；72 小时) 可诱导 HepG2 和 SGC7901 细胞系发生 G2/M 期阻滞[1]。
CDK1-IN-9 (0.1-1 μM；72 小时) 通过非经典途径抑制 CDK1/cyclin B1 激酶活性[1]。
CDK1-IN-9 (1 μM；72 小时) 在 HCT116 细胞系中抑制细胞周期蛋白 45 (CDC45) 的活性，导致 DNA 损伤，并通过 p53 介导的线粒体途径触发细胞凋亡，敲低 HCT116 细胞系中的 CDC45 可重现该途径[1]。

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

CDK1-IN-9 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT116 cell line, HepG2 cell line, SGC7901 cell line
Concentration: 0.1 μM; 0.25 μM; 0.5 μM; 1 μM; 2.5 μM; 5 μM
Incubation Time: 24 h; 48 h; 72 h
Result: Decreased the viability of HCT116, HepG2, and SGC7901 cells in a dose- and time-dependent manner.

Cell Migration Assay [1]

Cell Line: HCT116 cell line
Concentration: 0.5 μM
Incubation Time: 24 h; 48 h
Result: Significantly impaired the migratory ability.

Cell Cycle Analysis[1]

Cell Line: HepG2 cell line, SGC7901 cell line
Concentration: 0.1 μM; 0.5 μM
Incubation Time: 72 h
Result: Induced G2/M arrest in a concentration-dependent manner.

Cell Cycle Analysis[1]

Cell Line: HCT116 cell line
Concentration: 0.01 μM; 0.1 μM
Incubation Time: 72 h
Result: Induced G2/M arrest in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: HCT116 cell line, HepG2 cell line, SGC7901 cell line
Concentration: 0.01 μM; 0.1 μM; 0.5 μM
Incubation Time: 72 h
Result: Induced apoptosis in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: HCT116 cell line
Concentration: 0.1 μM; 0.5 μM; 1 μM
Incubation Time: 72 h
Result: Reduced the protein levels of CDK1 and cyclin B1 in a concentration-dependent fashion.
Significantly reduced CDC45 expression.
Increased γH2AX accumulation.
Elevated both total and phosphorylated levels of p53.
Decreased the ratio of the anti-apoptotic protein Bcl-xL to the pro-apoptotic protein BAX.
Increased Cytochrome c release.

Real Time qPCR[1]

Cell Line: HCT116 cell line
Concentration: 0.5 μM; 1 μM
Incubation Time: 24 h; 48 h; 72 h
Result: Downregulated the transcriptional levels of CDK1 and cyclin B1.
体内研究
(In Vivo)

CDK1-IN-9 (3.3-30 mg/kg；灌胃；每天；持续 14 天) 显著抑制了雄性 BALB/c 裸鼠的异种移植肿瘤生长，而未引起明显的体重减轻或可观察到的器官毒性[1]。

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

Animal Model: Male BALB/c nude mice (4-6 weeks old; 16-20 g) received a subcutaneous injection of 1 × 107 HCT116 cells to establish a xenograft tumor model[1].
Dosage: 3.3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: i.g.; every day; for 14 days
Result: Significantly lower tumor volume compared with the control group.
Reduced tumor weight by 56.4% in 30 mg/kg group.
Did not have significant changes in mouse body weight or in the weights of major organs (heart, liver, spleen, lung, and kidney).
Showed no obvious pathological injury or toxicity in these tissues through histological examination.
Did not have significantly effect on serum biochemistry parameters (including ALT and AST).
分子量

419.48

Formula

C16H17N7O3S2
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

CDK1-IN-9 相关分类

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  • 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:

CDK1-IN-9CDKAurora KinaseCyclin dependent kinaseselective CDK1 inhibitorbroad antiproliferative activityHCT116 colon cancer cellsG2/M phase arrestcyclin B1CDC45DNA replication stressp53 signaling pathwayapoptosiscolon cancerliver cancergastric cancerInhibitorinhibitorinhibit

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