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:

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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)

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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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:

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

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