2. Epigenetics
  3. Epigenetic Reader Domain
  4. 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.

BRDT-IN-2

BRDT-IN-2 Chemical Structure

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BRDT-IN-2 Related Antibodies

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Description

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[1].

IC50 & Target

BRDT (BD1)

 

In Vitro

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.

BRDT-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: MM.1S multiple myeloma cells
Concentration: 0.1% (final DMSO concentration)
Incubation Time: 72 hours (37 °C, 5% CO2)
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).

Western Blot Analysis[1]

Cell Line: MM.1S multiple myeloma cells
Concentration: 0.039-10.000 μM
Incubation Time: 6 hours (37 °C, 5% CO2)
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.
Molecular Weight

728.79

Formula

C33H41FN8O8S
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BRDT-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRDT-IN-2Epigenetic Reader DomainFLT3JAK2BRD4-BD1c-MycX-ray crystallographymultiple myelomaZA channel water networksAlphaScreen assayBRDT-BD1MM.1SInhibitorinhibitorinhibit

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