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iBRD4-BD1

Names

[ CAS No. ]:
2839318-17-9

[ Name ]:
iBRD4-BD1

Biological Activity

[Description]:

iBRD4-BD1 is selective BRD4 bromodomain inhibitor. iBRD4-BD1 has inhibition activity for BRD4 bromodomain with an IC50 value of 12 nM. iBRD4-BD1 can be used for the research of inflammation and oncology[1].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[In Vitro]

iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD1 with an IC50 value of 12 nM[1]. iBRD4-BD1 has affinity and selectivity for the BET-family BRD4-BD2, BRD3-BD1, BRD3-BD2, BRD2-BD1 and BRD2-BD2 with IC50 values of 16 μM, 1.0 μM , 75 μM , 280 nM and 7.1 μM, respectively[1]. iBRD4-BD1 (0-50 μM; 72 h) has cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells[1]. Western Blot Analysis[1] Cell Line: MM.1S cells Concentration: 0-300 pM Incubation Time: 1 h Result: Prevented the denaturation of BRD4 in a dose-dependent manner and showed stabilization of BRD4 at concentrations above 3 nM. Cell Cytotoxicity Assay[1] Cell Line: MM.1S cells Concentration: 0-50 μM Incubation Time: 72 h Result: Showed cytotoxicity with an EC50 value of 2.3 μM in MM.1S cells.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H30F3N5O

[ Molecular Weight ]:
521.58


Related Compounds

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