BRDT-IN-1
BRDT-IN-1 is a BRDT-BD1 and BRDT-T inhibitor with BRDT-BD1 IC50 19 nM, Ki 8.8 nM, Ka 1.6 nM, and BRDT-T IC50 56 nM, Ka 5.0 nM. BRDT-IN-1 displays in vitro metabolic stability and limited cellular permeability in MDCK-MDR1 cells. BRDT-IN-1 can be used for the research of multiple myeloma.
For research use only. We do not sell to patients.
- Formula: C31H39FN8O7S
- Molecular Weight:686.75
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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
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BRDT (BD1) 19 nM (IC50) |
BRDT-T 56 nM (IC50) |
In Vitro
BRDT-IN-1 (compound 13) exhibits a 14-fold selectivity over BRD4-BD1, a 69-fold selectivity over BRD2-BD1, and a 31-fold selectivity over BRD3-BD1[1].
BRDT-IN-1 inhibits the proliferation of MM.1S multiple myeloma cells with an IC50 of 4.3 μM[1].
BRDT-IN-1 (0.04-10 μM; 6 h) reduces c-Myc protein expression in MM.1S multiple myeloma cells in a dose-dependent manner, and exerts significant inhibitory effects at concentrations ≥2.5 μM after 6 hours of treatment[1].
BRDT-IN-1 exhibits excellent metabolic stability in human and mouse liver microsomes, with half-lives as long as 231 min and 870 min, respectively, but shows low cellular permeability in MDCK-MDR1 cells (<0.22 × 10-6 cm2/s)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MM.1S multiple myeloma cells
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Concentration:0.04-10 μM
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Incubation Time:6 h
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Result:Dose-dependently suppressed c-Myc protein levels in MM.1S cells.
Caused notable reduction of c-Myc protein levels at 2.5 μM.
Induced near-complete inhibition of c-Myc protein levels at 10 μM.
Chemical Information
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Molecular Weight 686.75
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Formula C31H39FN8O7S
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SMILES
OC[C@@H](C(O)=O)NC(C1=CC(NC2=NC(NC3=CC=C(C(NC4CCNCC4)=O)C(F)=C3)=NC=C2C)=CC(NS(=O)(C(C)(C)C)=O)=C1)=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.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRDT-IN-1 Related Classifications
HY-183247 Related Classifications
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