BRD4-BD1-IN-4
BRD4-BD1-IN-4 is a selective BRD4 BD1 inhibitor with an IC50 of 0.82 μM and a Kd of 0.98 μM. BRD4-BD1-IN-4 downregulates the expression of c-myc and anti-apoptotic proteins, elevates ROS levels, reduces mitochondrial membrane potential, induces DNA damage and triggers apoptosis. BRD4-BD1-IN-4 inhibits the migration and proliferation of cancer cells. BRD4-BD1-IN-4 can be used in the research of lung cancer, breast cancer and colon cancer.
For research use only. We do not sell to patients.
- Formula: C29H32N4O2
- Molecular Weight:468.59
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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
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Biological Activity
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BRD4 (BD1) 0.82 μM (IC50) |
BRD4 (BD1) 0.98 μM (Kd) |
BRD4-BD1-IN-4 (Compound B12) (0.5-40 μM; 48 h) potently inhibits the proliferation of A549, MDA-MB-231 and MC-38 cancer cells, with IC50 values of 0.73, 3.71 and 3.92 μM, respectively[1].
BRD4-BD1-IN-4 (0.5-2 μM; 24-48 h) effectively inhibits the migration of A549 cells[1].
BRD4-BD1-IN-4 (0.5-2 μM; 14 days) effectively reduces the clonogenic proliferation capacity of A549 cells[1].
BRD4-BD1-IN-4 (0.5-2 μM; 48 h) induces DNA double-strand breaks and inhibits DNA damage repair in A549 cells, which is confirmed by elevated γ-H2AX levels[1].
BRD4-BD1-IN-4 (0.5-2 μM; 14 days) induces apoptosis in A549 cells[1].
BRD4-BD1-IN-4 (0.5-2 μM; 48 h) increases the intracellular ROS level in A549 cells in a concentration-dependent manner[1].
BRD4-BD1-IN-4 (0.5-2 μM; 48 h) reduces the mitochondrial membrane potential of A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549 cells
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Concentration:0.5, 1, and 2 μM
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Incubation Time:24 and 48 h
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Result:Dose and time-dependently inhibited cell migration.
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Cell Line:A549 cells
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Concentration:0.5, 1, and 2 μM
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Incubation Time:48 h
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Result:Induced cell apoptosis.
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Cell Line:A549 cells
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Concentration:0.5, 1, and 2 μM
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Incubation Time:48 h
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Result:Increased γ-H2AX levels.
Down-regulated anti-apoptotic proteins (bcl-2, c-myc), up-regulated pro-apoptotic proteins (BAX), and activated the Caspase cascade reaction (increasing the expression of Cleaved Caspase3 and Cleaved PARP).
Chemical Information
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Molecular Weight 468.59
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Formula C29H32N4O2
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SMILES
CN(CC1)CCN1C2=CC=C(N=C(C3=CC(C)=C(O)C(C)=C3)C(N4CC5=CC=CC=C5C)=O)C4=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)
BRD4-BD1-IN-4 Related Classifications
HY-187207 Related Classifications
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