2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK2-IN-28

CDK2-IN-28 (compound 22) 是一种 CDK2 抑制机，对其他 CDK 具有良好选择性和细胞效应。CDK2-IN-28 对 MKN1 细胞具有抗增殖作用 (EC50: 0.31 μM)，

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CDK2-IN-28 Chemical Structure

CDK2-IN-28 Chemical Structure

CAS No. : 3025006-64-5

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CDK2-IN-28 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

CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM)[1].

IC50 & Target

CDK7

54.7 nM (Ki, [1])

CDK2

1 nM (Ki, [1])

CDK5

15.8 nM (Ki, [1])

CDK9

12.8 nM (Ki, [1])

体外研究
(In Vitro)

CDK2-IN-28 (37 nM-3 μM; 24 h) 在 MKN1 细胞中显著下调 Rb 在 Ser807/811 和 Ser780 位置磷酸化的水平[1]。
CDK2-IN-28 (333.3 nM; 24 h) 在 MKN1 细胞中引起的 CDK2 抑制，造成了细胞周期在 G2/M 期阻滞[1]。

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

CDK2-IN-28 相关抗体:

Western Blot Analysis[1]

Cell Line: MKN1 cells
Concentration: 37 nM, 111.1 nM, 333.3 nM, 1000 nM, 3000 nM
Incubation Time: 24 h
Result: Significantly downregulated Rb phosphorylation at Ser807/811 and Ser780 in dose dependent way.

Cell Cycle Analysis[1]

Cell Line: MKN1 cells
Concentration: 111.1 nM and 333.3 nM
Incubation Time: 24 h
Result: Caused by CDK2 inhibition is accumulation of G0/G1 cells as the CDK2/cyclin E-mediated phosphorylation of Rb relieves suppression of the E2Fs, thus allowing G1/S transition through the restriction point.
体内研究
(In Vivo)

CDK2-IN-28（10 mg/kg；口服；单剂量）在小鼠中具有较差的血浆暴露，CDK2-IN-28（1 mg/kg；静脉注射；单剂量）在小鼠 PK 测定中也显示出高血浆清除率（159-236 mL/min/kg)[1]。

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

513.66

Formula

C25H35N7O3S
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

CDK2-IN-28 相关分类

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  • 稀释计算器

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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:

CDK2-IN-283025006-64-5CDKCyclin dependent kinaseCCNE1 amplificationCyclin-dependent kinase 2MacrocycleMolecular dynamic simulationsSmall molecule inhibitorInhibitorinhibitorinhibit

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目录号：
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