1. Cell Cycle/DNA Damage Apoptosis Epigenetics
  2. CDK Apoptosis c-Myc Caspase PARP
  3. CDK9-IN-42

CDK9-IN-42 是一种强效且具有选择性的 CDK9 抑制剂,其 IC50 值为 3.8 nM。CDK9-IN-42 可通过下调 Myc-1c-Myc 来抑制癌细胞生长并诱导细胞凋亡 (apoptosis)。CDK9-IN-42 可用于癌症研究,如乳腺癌和肺癌。

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CDK9-IN-42

CDK9-IN-42 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK9-IN-42 is a potent and selective CDK9 inhibitor with an IC50of 3.8 nM. CDK9-IN-42 can inhibit the growth of cancer cells and induce apoptosis by downregulating Myc-1 and c-Myc. CDK9-IN-42 can be used for the research of cancer, such as breast and lungcancer[1].

IC50 & Target[1]

CDK9

3.8 nM (IC50)

Caspase 3

 

体外研究
(In Vitro)

CDK9-IN-42 (Compound L18) (72 h) 可抑制多种血液肿瘤细胞的增殖,对 MV4-11、MOLM-13、THP-1、KG-1 和 HL-60 细胞的 IC50 值分别为 0.049 μM、0.071 μM、0.062 μM、0.093 μM 和 0.175 μM[1]
CDK9-IN-42 (72 h) 可抑制多种实体肿瘤细胞的增殖,对 HepG2、MCF-7、22RV1 和 A549 细胞的 IC50 值分别为 0.045 μM、0.166 μM、0.247 μM 和 0.225 μM[1]
CDK9-IN-42 (0.1-1 μM, 72 h) 对正常人支气管上皮细胞的细胞毒性较低,对 BEAS-2B 细胞的 IC50 值为 0.402 μM[1]
CDK9-IN-42 对 CDK9 表现出优异的选择性,对 CDK 家族成员 CDK1、CDK4、CDK6 和 CDK7 的 IC50 均大于 1 μM[1]
CDK9-IN-42 (0.1-0.5 μM, 12 h) 可下调 MV4-11 细胞中 p-RNAPII-ser2、Mcl-1、c-Myc、CDK9 和细胞周期蛋白 T1 的蛋白水平[1]
CDK9-IN-42 (0.5-1 μM, 12 h) 可诱导 MV4-11 细胞凋亡[1]

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

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1, 0.25, 0.5, 1 and 2 μM
Incubation Time: 2, 4, 8, 12 and 24 h
Result: Decreased levels of p-RNAPII-ser2, Mcl-1, c-Myc, CDK9 and Cyclin T1 protein.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.5 and 1 μM
Incubation Time: 12 h
Result: Increased apoptosis rates.
Downregulated PARP and Caspase-3 proteins.
Upregulated Cleaved-PARP and Cleaved-Caspase-3.
体内研究
(In Vivo)

CDK9-IN-42 (Compound L18) (15-50 mg/kg,静脉注射,单剂量) 在 ICR 小鼠中未出现死亡或显著体重减轻的情况[1]

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

Animal Model: ICR mice[1]
Dosage: 15, 30 and 50 mg/kg
Administration: Intravenously, Subcutaneous
Result: Showed no death or significant weight loss.
分子量

498.55

Formula

C22H19FN6O3S2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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CDK9-IN-42
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HY-178039
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