2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK9-IN-22

CDK9-IN-22 是一种有效的 CDK9 抑制剂，对 CDK9 和 CDK 的 IC50 分别为 10.4、876.2 nM。CDK9-IN-22 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G2/M 期。CDK9-IN-22 降低 p-RNAPII (S2) 和 CDK9 蛋白的表达。CDK9-IN-22 具有抗增殖和抗肿瘤活性。

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CDK9-IN-22 Chemical Structure

CDK9-IN-22 Chemical Structure

CAS No. : 2872677-61-5

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CDK9-IN-22 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK9-IN-22 is a potent CDK9 inhibitor with IC50s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity[1].

IC50 & Target[1]

CDK9/cyclinT1

10.4 nM (IC50)

cdk2/cyclin A

876.2 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-431 IC50
0.1 μM
Compound: 8d
Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
A549 IC50
0.66 μM
Compound: 8d
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
HCT-116 IC50
0.09 μM
Compound: 8d
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
L02 IC50
1.43 μM
Compound: 8d
Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
NCI-H1975 IC50
0.43 μM
Compound: 8d
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
PANC-1 IC50
0.08 μM
Compound: 8d
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay
[PMID: 36332552]
体外研究
(In Vitro)

CDK9-IN-22 (compound 8 d) (0.1, 0.5, 2.5 µM; 24, 48 h) 在 PANC-1 细胞中以浓度依赖性方式诱导细胞凋亡和细胞周期停滞在 G2/M 期[1 ].
CDK9-IN-22 (0.1, 0.5, 2.5 µM; 24 h) 降低 PANC-1 细胞中 p-RNAPII (S2) 和 CDK9 蛋白的表达[1]。

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

CDK9-IN-22 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549, H1975, A431, PANC-1, HCT-116, LO2 cells
Concentration: 0-100 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.66, 0.43, 0.10, 0.08, 0.09, 1.43 μM for A549, H1975, A431, PANC-1, HCT-116, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 48 h
Result: Induced apoptosis with the percentage of total apoptotic cells was 43.6, 54.1 and 65.8% at 0.1, 0.5 and 2.5 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 24 h
Result: Arrested the cell cycle at the G2/M phase in a dose-dependent manner (21.83% for 0.1 μM, 25.85% for 0.5 μM and 34.26% for 2.5 μM).

Western Blot Analysis[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 0.5, 2.5 µM
Incubation Time: 24 h
Result: Decreased the expression of p-RNAPII (S2) and CDK9 protein in a dose-dependent manner.
体内研究
(In Vivo)

CDK9-IN-22 (5, 10, 20 mg/kg; i.p.; every other day for four weeks) 抑制异种移植小鼠模型中的肿瘤生长[1]。

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

Animal Model: BALB/c nude mice (PANC-1 tumor xenograft murine model)[1]
Dosage: 5, 10, 20 mg/kg
Administration: I.p.; every other day for four weeks
Result: Inhibited the tumor growth with the tumor inhibition rate (TIR) was 6.2, 32.6 and 54.2% at the dose of 5, 10 and 20 mg/kg, respectively.
分子量

485.55

Formula

C28H28FN5O2
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

CDK9-IN-22 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:

CDK9-IN-222872677-61-5CDKCyclin dependent kinaseantiproliferativeaiti-tumorapoptosisG2/M phasep-RNAPII (S2)PANC-1 cellsInhibitorinhibitorinhibit

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