2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK2-IN-51

CDK2-IN-51 是一种吡唑并吡啶衍生物，一种 CDK2 抑制剂，其 IC50 为 23.47 nM。CDK2-IN-51 导致 DNA 复制因子 (Polα、MCM7、ORC2 和 ORC4) 表达减少和 G1 期前细胞周期阻滞。CDK2-IN-51 不具有促凋亡作用，且对 CDK2 蛋白表达的影响不显著。CDK2-IN-51 可用于结直肠癌的研究。

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CDK2-IN-51

CDK2-IN-51 Chemical Structure

CAS No. : 1443-10-3

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CDK2-IN-51 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 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK2-IN-51 is a pyrazolopyridine derivative, a CDK2 inhibitor with an IC50 of 23.47 nM. CDK2-IN-51 does not have a pro-apoptotic effect and had no significant effect on CDK2 protein expression. CDK2-IN-51 reduces expression of DNA replication factors (Polα, MCM7, ORC2, and ORC4) and pre-G1 cell cycle arrest. CDK2-IN-51 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

CDK2

23.47 nM (IC50)

CDK2

4.11 μM (Ki)

体外研究
(In Vitro)

CDK2-IN-51 (compound 6) (10-50 μM；24-72 小时) 对 HCT-116 和 HT-29 细胞表现出显著的抗增殖活性，对 NCM-460D 细胞无细胞毒性[1]。
CDK2-IN-51 (40-50 μM；48 小时) 在 HCT-116 和 HT-29 细胞中引起 G1 期前阶段阻滞，而不会引起 S 期阻滞[1]。
CDK2-IN-51 (40-50 μM；48 小时) 下调 HCT-116 和 HT-29 细胞中参与 DNA 复制过程的 CDK2 蛋白靶点，包括 Polα、MCM7、ORC2 和 ORC4，不具有促凋亡作用，且对 CDK2 蛋白表达的影响不显著[1]。

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

CDK2-IN-51 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-116, HT-29, NCM-460D
Concentration: 10 μM, 20 μM, 40 μM, 50 μM
Incubation Time: 24 h, 48 h, 72 h
Result: At 72 h, exhibited significant antiproliferative effects on HCT-116 and HT-29 cells, with IC50 values of 46.41 μM and 61.47 μM, respectively, and showed no cytotoxicity on NCM-460D cells, with an IC50 value of >100 μM.

Cell Cycle Analysis[1]

Cell Line: HCT-116, HT-29
Concentration: 40 μM, 50 μM
Incubation Time: 48 h
Result: Caused a significant increase in the pre-G1 phase population in both HCT-116 and HT-29 cells, indicating cell death, and no S-phase arrest was observed, suggesting that the compound did not induce apoptosis.

Western Blot Analysis[1]

Cell Line: HCT-116, HT-29
Concentration: 40 μM, 50 μM
Incubation Time: 48 h, 72 h
Result: Reduced the expression of CDK2 targets, MCM7, ORC2, and ORC4 proteins.
Reduced Polα levels. 
分子量

288.35

Formula

C18H16N4
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-51 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:

CDK2-IN-511443-10-3CDKCyclin dependent kinaseCDK2HT-29PyrazolopyridineHCT-116NCM-460DColorectal CancerPyrazoloStructure-activity relationship (SAR)Pyrazolo[3,4-b]pyridineInhibitorinhibitorinhibit

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