CDK8/BRD4-IN-1
CDK8/BRD4-IN-1 is a dual CDK8/BRD4 inhibitor, with an IC50 of 5.44 μM against CDK8 and an IC50 of 4.03 μM against BRD4. CDK8/BRD4-IN-1 exhibits anticancer activity against colorectal cancer. CDK8/BRD4-IN-1 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C27H36N6O
- Molecular Weight:460.61
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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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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
CDK8 5.44 μM (IC50) |
BRD4 4.03 μM (IC50) |
In Vitro
CDK8/BRD4-IN-1 (Compound 8d) (20 μM) inhibits purified BRD4 protein with an IC50 of 4.03 μM and 83.53% inhibition at 20 μM[1].
CDK8/BRD4-IN-1 (1-20 μM) inhibits purified CDK8 protein with an IC50 of 5.44 μM, 69.20% inhibition at 20 μM, and 26.30% inhibition at 1 μM[1].
CDK8/BRD4-IN-1 (20 μM) shows favorable selectivity toward CDK8/CycC and CDK19/CycC over other CDK family members when tested at 20 μM[1].
CDK8/BRD4-IN-1 (50 μM) inhibits the proliferation of HCT116 colorectal cancer cells with an IC50 of 12.41 μM, and inhibits SW480 cell proliferation by 98.07% at 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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Molecular Weight 460.61
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Formula C27H36N6O
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SMILES
CN(C(C=C1)=C(N(C(C)C)[C@@H]2C)C=C1NCCCCCCNC3=NC=NC4=C3C=CC=C4)C2=O
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK8/BRD4-IN-1 Related Classifications
HY-184727 Related Classifications
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