2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis Bcl-2 Family Caspase
  4. CDK1/2/4-IN-1

CDK1/2/4-IN-1 (compound 3a) 是一种有效的 CDK 抑制剂， CDK1、CDK2 和 CDK4 的 IC50 值分别为 1.47、0.78 和 0.87 μM。CDK1/2/4-IN-1 在 G2/M 期阻滞细胞周期并诱导细胞凋亡 (apoptosis)。CDK1/2/4-IN-1 升高 Bax、caspase-3、P53 水平，降低 Bcl-2 水平。CDK1/2/4-IN-1 可用于癌症研究。

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CDK1/2/4-IN-1 Chemical Structure

CDK1/2/4-IN-1 Chemical Structure

CAS No. : 2414633-49-9

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CDK1/2/4-IN-1 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

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research[1].

IC50 & Target[1]

CDK1

1.47 (IC50)

CDK2

0.78 (IC50)

CDK4

0.87 (IC50)

Caspase 3

 

Bax

 

Bcl-2

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
1.39 μM
Compound: Cpd 58
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 33148490]
HepG2 IC50
1.56 μM
Compound: Cpd 58
Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
[PMID: 33148490]
MCF7 IC50
1.97 μM
Compound: Cpd 58
Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
[PMID: 33148490]
体外研究
(In Vitro)

CDK1/2/4-IN-1 (compound 3a) (0.01-100 µM; 24 hours) has antitumor activity in cancer cell lines[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 µM; 24 hours) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 µM; A549 cells) induces up-regulation of the expression of Bax, caspases-3 and p53, and increases the ratio of Bcl-2[1].

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

CDK1/2/4-IN-1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Liver cancer cell line (HepG-2), lung cancer cell line (A549) and breast cancer cell line (MCF-7)
Concentration: 0.01, 0.1, 1.0, 10, 100 µM
Incubation Time: 24 hours
Result: Displayed cytotoxic activity with IC50 values of 1.56, 1.39 and 1.97 µM for HepG-2, A549 and MCF-7, respectively.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 1.39 µM
Incubation Time: 24 hours
Result: Increased G2/M phase by 2.6 folds compared with the control cells.

Apoptosis Analysis[1]

Cell Line: A549 cells
Concentration: 1.39 µM
Incubation Time: 24 hours
Result: Increased the overall percentage of the apoptotic cells.
分子量

288.36

Formula

C15H16N2O2S
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

CDK1/2/4-IN-1 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:

CDK1/2/4-IN-12414633-49-9CDKApoptosisBcl-2 FamilyCaspaseCyclin dependent kinaseapoptosisBclcaspaseanticancerInhibitorinhibitorinhibit

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