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.
- CAS No.: 2101206-26-0
- Formula: C18H16FNO2S
- Molecular Weight:329.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
CLK1 7 nM (IC50) |
CLK4 2.3 nM (IC50) |
HDAC1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | GI50 |
2.8 μM
Compound: 21b
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Cytotoxicity against human HepG2 cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 5 days by MTT assay
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[PMID: 28561591] |
| MDA-MB-231 | GI50 |
9.6 μM
Compound: 21b
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Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 5 days by MTT assay
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[PMID: 28561591] |
| T-24 | GI50 |
0.6 μM
Compound: 21b
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Cytotoxicity against human T24 cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human T24 cells assessed as growth inhibition after 5 days by MTT assay
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[PMID: 28561591] |
| T47D | GI50 |
15.3 μM
Compound: 21b
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Cytotoxicity against human T47D cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human T47D cells assessed as growth inhibition after 5 days by MTT assay
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[PMID: 28561591] |
| THP-1 | GI50 |
27.2 μM
Compound: 21b
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Cytotoxicity against human THP1 cells assessed as growth inhibition after 5 days by MTT assay
Cytotoxicity against human THP1 cells assessed as growth inhibition after 5 days by MTT assay
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[PMID: 28561591] |
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. Further protocols information, click here.
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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)
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Concentration:/
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Incubation Time:5 days (cancer/HEK293 cells); 2 days (peripheral blood lymphocytes)
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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.
Chemical Information
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CAS No. 2101206-26-0
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Molecular Weight 329.39
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Formula C18H16FNO2S
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SMILES
O=C(C=1SC=2C=CC(OC)=CC2C1)N(C)CC=3C=CC=C(F)C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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