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.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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CLK1 7 nM (IC50) |
CLK4 2.3 nM (IC50) |
HDAC1 |
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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] |
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.
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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