1. PROTAC Epigenetics Apoptosis
  2. PROTACs Epigenetic Reader Domain Apoptosis
  3. 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.

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PROTAC BRD4 Degrader-17 Chemical Structure

PROTAC BRD4 Degrader-17 Chemical Structure

CAS No. : 2585561-49-3

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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].

IC50 & Target

BRD4 (BD2)

3.82 ± 0.0 nM (IC50)

BRD4 (BD1)

29.54 ± 2. nM (IC50)

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.

Molecular Weight

877.94

Formula

C49H47N7O9

CAS No.
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

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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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  • 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:
PROTAC BRD4 Degrader-17
Cat. No.:
HY-143328
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