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Cat. No.: HY-143328

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PROTAC BRD4 Degrader-17

PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells.
(Pink: BRD4 ligand (HY-184874); Blue: Cereblon ligand (HY-10984); Black: linker).

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

CAS No.: 2585561-49-3
Formula: C₄₉H₄₇N₇O₉
Molecular Weight:877.94

Storage:

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

Data Sheet (268 KB)

PROTAC BRD4 Degrader-17 Chemical Structure

CAS No.: 2585561-49-3

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Fluorescent Dye

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

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

Biological Activity

Description

PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC₅₀ values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells^[1]. (Pink: BRD4 ligand (HY-184874); Blue: Cereblon ligand (HY-10984); Black: linker).

IC₅₀ & Target

BRD4 (BD2)

3.82 ± 0.0 nM (IC₅₀)

BRD4 (BD1)

29.54 ± 2. nM (IC₅₀)

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	10.67 nM Compound: 13i	Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK8 assay	[PMID: 35395439]

In Vitro

PROTAC BRD4 Degrader-17 (compound 13i) (100 nM, 4-24 h) significantly induces BRD4 L and BRD4 S degradation at a concentration of 100 nM at 4 h and then recovers BRD4 S at 24 h like dBET6 (HY-112588) in MV-4-11 cells^[1].

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

Chemical Information

CAS No. 2585561-49-3
Molecular Weight 877.94
Formula C₄₉H₄₇N₇O₉
SMILES

CN1C=C(C2=C(C1=O)NC(C(NCC3=CC=C(C=C3)C(NCCCCNC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=O)=C2)C7=CC(C(C)(C)O)=CC=C7OC8=CC=CC=C8
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 (268 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]. Chen J, et al. Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold. Eur J Med Chem. 2022 Jun 5;236:114259. [Content Brief]

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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.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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PROTAC BRD4 Degrader-17

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC BRD4 Degrader-17 Related Classifications

HY-143328 Related Classifications