CDK1/2/4-IN-1
CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research.
For research use only. We do not sell to patients.
- CAS No.: 2414633-49-9
- Formula: C15H16N2O2S
- Molecular Weight:288.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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CDK2 0.78 (IC50) |
CDK4 0.87 (IC50) |
CDK1 1.47 (IC50) |
Caspase 3 |
Bax |
Bcl-2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.39 μM
Compound: Cpd 58
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Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
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[PMID: 33148490] |
| HepG2 | IC50 |
1.56 μM
Compound: Cpd 58
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Cytotoxicity against human HepG2 cells by MTT assay
Cytotoxicity against human HepG2 cells by MTT assay
|
[PMID: 33148490] |
| MCF7 | IC50 |
1.97 μM
Compound: Cpd 58
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Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
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[PMID: 33148490] |
CDK1/2/4-IN-1 (compound 3a) (0.01-100 µM; 24 hours) has antitumor activity in cancer cell lines[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 µM; 24 hours) induces apoptosis and arrests cell cycle at G2/M phase in A549 cells[1].
CDK1/2/4-IN-1 (compound 3a) (1.39 µM; A549 cells) induces up-regulation of the expression of Bax, caspases-3 and p53, and increases the ratio of Bcl-2[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Liver cancer cell line (HepG-2), lung cancer cell line (A549) and breast cancer cell line (MCF-7)
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Concentration:0.01, 0.1, 1.0, 10, 100 µM
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Incubation Time:24 hours
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Result:Displayed cytotoxic activity with IC50 values of 1.56, 1.39 and 1.97 µM for HepG-2, A549 and MCF-7, respectively.
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Cell Line:A549 cells
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Concentration:1.39 µM
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Incubation Time:24 hours
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Result:Increased G2/M phase by 2.6 folds compared with the control cells.
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Cell Line:A549 cells
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Concentration:1.39 µM
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Incubation Time:24 hours
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Result:Increased the overall percentage of the apoptotic cells.
Chemical Information
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CAS No. 2414633-49-9
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Molecular Weight 288.36
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Formula C15H16N2O2S
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SMILES
O=C(C1=C(C)SC(NC)=N1)/C=C/C2=CC=C(OC)C=C2
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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)