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Cat. No.: HY-151972

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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.

CAS No.: 2976403-41-3
Formula: C₂₉H₂₇N₅O₆S
Molecular Weight:573.62

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

BRD4 Inhibitor-25 Chemical Structure

CAS No.: 2976403-41-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

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)

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	3.44 μM Compound: 11a	Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human A2780 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
ES-2	IC₅₀	3.44 μM Compound: 11a	Antiproliferative activity against human ES2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human ES2 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
OVCAR-3	IC₅₀	2.69 μM Compound: 11a	Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
SK-OV-3	IC₅₀	1.38 μM Compound: 11a	Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human SK-OV-3 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]
SW626	IC₅₀	8.47 μM Compound: 11a	Antiproliferative activity against human SW626 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human SW626 cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 36470106]

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).

Chemical Information

CAS No. 2976403-41-3
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al. Design, synthesis and anti-ovarian cancer activities of thieno[2,3-d]pyrimidine based chimeric BRD4 inhibitor/nitric oxide-donator. Eur J Med Chem. 2022 Nov 29;246:114970. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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