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.
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- Formule: C31H39FN8O7S
- Masse moléculaire:686.75
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Stockage:
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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Activité biologique
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Chemical Information
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Activité biologique
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.
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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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Masse moléculaire 686.75
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRDT-IN-1 Related Classifications
HY-183247 Related Classifications
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