1. Cell Cycle/DNA Damage Apoptosis
  2. CDK Apoptosis DNA/RNA Synthesis
  3. CDK-IN-9

CDK-IN-9 (compound 24) 是一种有效的 CDK 抑制剂,也作为一个分子胶诱导 CDK12 和 DDB1 的互作,对 CDK2/E 的 IC50 为 4 nM。CDK-IN-9 导致细胞周期蛋白 K (cyclin K) 的多泛素化及其随后的降解。CDK-IN-9 通过去磷酸化视网膜母细胞瘤蛋白和 RNA 聚合酶 II 诱导细胞凋亡 (apoptosis)。

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CDK-IN-9

CDK-IN-9 Chemical Structure

CAS No. : 3031561-92-6

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规格 价格 是否有货 数量
1 mg ¥3432
1 - 2 周
5 mg 询价 1 - 2 周
10 mg 询价 1 - 2 周
50 mg   询价  
100 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK-IN-9 (compound 24) is a potent CDK inhibitor, also as a molecular glue inducing an interaction between CDK12 and DDB1, with an IC50 values of 4 nM for CDK2/E. CDK-IN-9 leads to polyubiquitination of cyclin K and its subsequent degradation. CDK-IN-9 induce apoptosis through dephosphorylation of retinoblastoma protein and RNA polymerase II[1].

IC50 & Target[1]

CDK2/E

4 nM (IC50)

Cdk5/p25

39 nM (IC50)

CDK9/T1

20 nM (IC50)

CDK12/K

64 nM (IC50)

CDK13/K

22 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DB GI50
0.02 μM
Compound: 24
Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human DB cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
NU-DUL-1 GI50
0.015 μM
Compound: 24
Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human NU-DUL-1 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
OCI-LY19 GI50
0.465 μM
Compound: 24
Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human OCILY19 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
SUD4 GI50
0.028 μM
Compound: 24
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
U2932 GI50
0.055 μM
Compound: 24
Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
Antiproliferative activity against human U2932 cells assessed as cell growth inhibition measured after 72 hrs by resazurin dye based microplate reader analysis
[PMID: 35749742]
体外研究
(In Vitro)

CDK-IN-9 (compound 24) (0.005, 0.05, 0.5, or 5 μM; 2 h) potently decreases the level of cyclin K in MINO cells at 5 nM, and makes cyclin K disappear completely at 50 nM[1].
CDK-IN-9 makes siRNA silencing of DDB1 effectively stabilizes cyclin K at the protein level in treated MINO cells[1].
CDK-IN-9 (2.5-40 nM; 24 h) activates caspases 3/7/9 and decreases anti-apoptotic proteins Mcl-1 and XIAP in MINO cells[1].

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

体内研究
(In Vivo)

CDK-IN-9 (0.1-10 mg/kg; IP, single dosage) causes the decrease in cyclin K and CDK12 levels[1].

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

分子量

420.53

Formula

C21H24N8S

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
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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.

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CDK-IN-9
目录号:
HY-150641
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