BRDT-IN-2
BRDT-IN-2 is a BRDT-BD1-preferring inhibitor (Ki=10 μM) with higher affinity for BRDT-BD1 than BRD4-BD1. BRDT-IN-2 preferentially binds BRDT-BD1 without direct interaction with BRDT-BD1’s Arg54 residue. BRDT-IN-2 binds BRD4-BD1 with lower affinity via structured water molecule displacement in its binding pocket. BRDT-IN-2 can be used for the research of multiple myeloma.
For research use only. We do not sell to patients.
- Formula: C33H41FN8O8S
- Molecular Weight:728.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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BRDT (BD1) |
BRDT-IN-2 inhibits the growth of MM.1S multiple myeloma cells with an IC50 of 6.8 μM[1].
BRDT-IN-2 (0.039-10.000 μM; 6 h) dose-dependently downregulates the expression of c-Myc protein in MM.1S multiple myeloma cells in in vitro treatments[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:0.1% (final DMSO concentration)
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Incubation Time:72 hours (37 °C, 5% CO2)
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Result:Inhibited MM.1S cell growth with an IC50 value of 6.8 μM.
Was less potent than reference inhibitors JQ1 (IC50 = 0.12 μM) and I-BET151 (IC50 = 0.33 μM).
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Cell Line:MM.1S multiple myeloma cells
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Concentration:0.039-10.000 μM
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Incubation Time:6 hours (37 °C, 5% CO2)
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Result:Dose-dependently suppressed c-Myc protein levels.
Caused measurable reduction of c-Myc protein levels at concentrations ≥0.630 μM relative to untreated control cells.
Chemical Information
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Molecular Weight 728.79
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Formula C33H41FN8O8S
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SMILES
CC1=C(NC2=CC(C(N[C@@H](CCC(O)=O)C(O)=O)=O)=CC(NS(=O)(C(C)(C)C)=O)=C2)N=C(NC3=CC(F)=C(C(NC4CCNCC4)=O)C=C3)N=C1
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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)