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 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.

For research use only. We do not sell to patients.

CLK1/4-IN-2

CLK1/4-IN-2 Chemical Structure

CAS No. : 2101206-26-0

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CLK1/4-IN-2 Related Antibodies

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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

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

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Description

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

 

In Vitro

CLK1/4-IN-2 (2-5 days) potently inhibits the proliferation of human cancer cell lines, and exhibits low cytotoxicity toward non-tumorigenic peripheral blood lymphocytes and HEK293 cells[1].
CLK1/4-IN-2 (1.25-20 μM; 3 days) reduces the levels of cancer-related proteins (EGFR and HDAC1 in T24 cells; EGFR and p70S6 kinase in MDA-MB-231 cells; HDAC1 and p70S6 kinase in HepG2 cells), and its potency correlates with the sensitivity of cell lines to proliferation inhibition[1].

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

CLK1/4-IN-2 Related Antibodies

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.
Molecular Weight

329.39

Formula

C18H16FNO2S
CAS No.
SMILES

O=C(C=1SC=2C=CC(OC)=CC2C1)N(C)CC=3C=CC=C(F)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CLK1/4-IN-2 Related Classifications

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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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