2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics
  3. CDK EGFR HDAC
  4. CLK1/4-IN-2

CLK1/4-IN-2 是一种选择性 CLK1/4 抑制剂，对 CLK1 的 IC50 为 7 nM，对 CLK4 的 IC50 为 2.3 nM。CLK1/4-IN-2 可在癌细胞中诱导蛋白耗竭并展现抗癌活性。CLK1/4-IN-2 可用于乳腺癌、单核细胞白血病、膀胱癌、乳腺腺癌、肝细胞癌的相关研究。

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CLK1/4-IN-2

CLK1/4-IN-2 Chemical Structure

CAS No. : 2101206-26-0

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CLK1/4-IN-2 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 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 HDAC 亚型特异性产品:

查看所有亚型
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CLK1/4-IN-2 is a selective CLK1/4 inhibitor, with an IC50 of 7 nM against CLK1 and an IC50 of 2.3 nM against CLK4. CLK1/4-IN-2 induces protein depletion in cancer cells and exhibits anticancer activity. CLK1/4-IN-2 can be used in research related to breast cancer, monocytic leukemia, bladder cancer, mammary adenocarcinoma and hepatocellular carcinoma[1].

IC50 & Target[1]

CLK1

7 nM (IC50)

CLK4

2.3 nM (IC50)

HDAC1

 

体外研究
(In Vitro)

CLK1/4-IN-2 (2-5 days) 可强效抑制人类癌细胞系的增殖，且对非肿瘤性外周血淋巴细胞和 HEK293 细胞的细胞毒性较低[1]。
CLK1/4-IN-2 (1.25-20 μM; 3 days) 可降低癌症相关蛋白的水平 (T24 细胞中的 EGFR 与 HDAC1；MDA-MB-231 细胞中的 EGFR 与 p70S6 激酶；HepG2 细胞中的 HDAC1 与 p70S6 激酶)，其效力与细胞系对增殖抑制的敏感性相关[1]。

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

CLK1/4-IN-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Human cancer cell lines (T24 urinary bladder carcinoma, MDA-MB-231 breast adenocarcinoma, HepG2 hepatocellular carcinoma, THP-1 monocytic leukemia, T47D breast carcinoma) and non-tumor cells (peripheral blood lymphocytes, HEK293 human embryonic kidney cells)
Concentration: /
Incubation Time: 5 days (cancer/HEK293 cells); 2 days (peripheral blood lymphocytes)
Result: Inhibited proliferation of T24 cells with a GI50 of 0.6 μM.
Inhibited proliferation of HepG2 cells with a GI50 of 2.8 μM.
Inhibited proliferation of MDA-MB-231 cells with a GI50 of 9.6 μM.
Inhibited proliferation of T47D cells with a GI50 of 15.3 μM.
Inhibited proliferation of THP-1 cells with a GI50 of 27.2 μM.
Showed low cytotoxicity against non-tumor cells, with an LC50 of 29.4 μM for peripheral blood lymphocytes.
Showed no significant inhibition (GI50 > 30 μM) for HEK293 cells.
分子量

329.39

Formula

C18H16FNO2S
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

CLK1/4-IN-2 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

CLK1/4-IN-22101206-26-0CDKEGFRHDACCyclin dependent kinaseEpidermal growth factor receptorErbB-1HER1Histone deacetylasesurinary bladder carcinomaCLK4breast carcinomaHDAC1monocytic leukemiahepatocellular carcinomap70 S6 kinaseDyrk1ACLK1Inhibitorinhibitorinhibit

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