BRD4-IN-42
BRD4-IN-42 is a BRD4 BD1 inhibitor with an IC50 of 108.50 nM. BRD4-IN-42 can be used for the synthesis of PROTACs and serves as the target protein moiety of PROTAC BET Degrader-18 (HY-184335). BRD4-IN-42 inhibits the proliferation of wild-type and SHP099-resistant acute myeloid leukemia cells. BRD4-IN-42 is applicable to research related to acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C30H36N4O7S
- Molecular Weight:596.69
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BRD4 108.50 nM (IC50) |
BRD4-IN-42 (compound 16) potently inhibits BRD4 BD1 in a cell-free TR-FRET assay with an IC50 of 108.50 nM[1].
BRD4-IN-42 (10 μM; 3-fold serial dilution across 10 data points) inhibits proliferation of wild-type MV4-11 acute myeloid leukemia cells with an IC50 of 493.95 nM[1].
BRD4-IN-42 (10 μM; 3-fold serial dilution across 10 data points) inhibits proliferation of SHP099-resistant MV4-11 acute myeloid leukemia cells with an IC50 of 365.3 nM[1].
BRD4-IN-42 can be used in the synthesis of PROTACs and serves as the target protein-binding moiety for PROTAC BET Degrader-18 (compound 36) (HY-184335)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 596.69
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Formula C30H36N4O7S
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SMILES
CC(C1=C(NC(C(NC2=C(C=CC(S(=O)(N3CCOCC3)=O)=C2)OCCCC(NCC)=O)=O)=C1C4=CC=CC=C4)C)=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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRD4-IN-42 Related Classifications
HY-184339 Related Classifications
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- BRD4-IN-42
- Ligands for Target Protein for PROTAC
- Epigenetic Reader Domain
- acetylpyrrole scaffold BRD4 inhibitor
- competitive binding
- BRD4 BD1 domain binding
- hydrogen bond interaction with Asn140
- solvent-exposed side chain
- PROTAC warhead
- antiproliferative activity
- MV4-11 cells
- SHP099-resistant MV4-11 cells
- acute myeloid leukemia
- c-Myc downregulation
- Inhibitor
- inhibitor
- inhibit