2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK12-IN-4

CDK12-IN-4 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 0.641 μM。CDK12-IN-4 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。

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CDK12-IN-4 Chemical Structure

CDK12-IN-4 Chemical Structure

CAS No. : 2651196-69-7

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CDK12-IN-4 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

CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].

IC50 & Target[1]

CDK12

0.641 μM (IC50)

CDK2/cyclinE

>20 μM (IC50)

CDK9/cyclinT1

>20 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1].
CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].

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

CDK12-IN-4 相关抗体:
分子量

426.42

Formula

C20H20F2N8O
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

CDK12-IN-4 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

CDK12-IN-42651196-69-7CDKCyclin dependent kinasepyrazolotriazineBRCA1MRNAMDA-MB-231CAL-120Inhibitorinhibitorinhibit

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产品名称：
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目录号：
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