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  2. Epigenetic Reader Domain
  3. BRD4 Inhibitor-25

BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.

For research use only. We do not sell to patients.

BRD4 Inhibitor-25 Chemical Structure

BRD4 Inhibitor-25 Chemical Structure

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Description

BRD4 Inhibitor-25 is a BRD4 inhibitor with IC50s of 0.82 μM, 1.94 μM for BD1 and BD2 domains of BRD4. BRD4 Inhibitor-25 induces apoptotic and autophagy cell death in ovarian cancer cells. BRD4 Inhibitor-25 can be used in the research of cancers, cardiovascular, neuromuscular and inflammatory disorders.

IC50 & Target[1]

BRD4-BD1

0.82 μM (IC50)

BRD4 (BD2)

1.94 μM (IC50)

BRD4 BD1

0.419 μM (Ki)

BRD4 BD2

0.686 μM (Ki)

BRD2 BD1

15.91 μM (IC50)

BRD2 BD1

7.43 μM (Ki)

In Vitro

BRD4 Inhibitor-25 (compound 11a) inhibits cell proliferation in OC cell lines (SKOV-3, OVCAR-3, SW626, ES-2 and A2780)[1].
BRD4 Inhibitor-25 promotes moderate levels of NO release (10.587 μM) when treated with an excess of cysteine[1].
BRD4 Inhibitor-25 (1 and 2 μM, 24 h) induces apoptosis and autophagy of SKOV-3 cells[1].
BRD4 Inhibitor-25 (2 μM, 24 h) inhibits autophagosome and lysosome fusion, leading to the blockage of autophagic flux in SKOV-3 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: OC cell lines (SKOV-3, OVCAR-3, SW626, ES-2 and A2780)
Concentration: 0-20 μM approximately
Incubation Time: 24 h
Result: Inhibited cell proliferation with IC50s of 1.38, 2.69, 8.47, 3.44, 3.44 μM respectively.

Western Blot Analysis[1]

Cell Line: SKOV-3 cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Increased cytochrome c and cleaved-caspase 3.
Reduced the anti-apoptosis protein Bcl-2.
Increased the autophagy-related proteins LC3II/I, p62/SQSTM1, and Beclin1.
In Vivo

BRD4 Inhibitor-25 (compound 11a, 30 mg/kg, i.p.) inhibits tumor growth in SKOV-3 subcutaneous xenograft model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SKOV-3 subcutaneous xenograft model[1]
Dosage: 30 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced Ki-67, a cell proliferation marker (IHC staining).
Molecular Weight

573.62

Formula

C29H27N5O6S

SMILES

[O-][N+]1=C(C(C2=CC=CC=C2)=NO1)COC(COC3=C(C=C(C=C3C)C4=NC5=C(C6=C(S5)CN(CC6)C)C(N4)=O)C)=O

Shipping

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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BRD4 Inhibitor-25 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.

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Product Name:
BRD4 Inhibitor-25
Cat. No.:
HY-151972
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