1. Epigenetics
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    PROTAC
  3. PROTAC BRD2/BRD4 degrader-1

PROTAC BRD2/BRD4 degrader-1 

Cat. No.: HY-130612
Handling Instructions

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A.

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

PROTAC BRD2/BRD4 degrader-1 Chemical Structure

PROTAC BRD2/BRD4 degrader-1 Chemical Structure

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Description

PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A[1].

IC50 & Target[1]

BRD4

 

BRD2

 

Cereblon

 

In Vitro

PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 (100 nM; ≥8 hours) shows anti-proliferation activity with IC50 value of 12.25 nM, and the BRD4 protein is reduced very efficiently at treatment time of ≥8 h in MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 (1 nM, 3 nM, 0.1 μM, 0.3 μM; 24-48 hours) induces MV4-11 apoptosis lines[1].
PROTAC BRD2/BRD4 degrader-1 exhibits excellent anti-proliferative activity in 6 leukemia cell lines of NCI. Among them, the GI50 values of the three leukemia cell lines were lower than 50 nM, consistent with the activity of leukemia MV4-11 cells[1].
PROTAC BRD2/BRD4 degrader-1 has good anti-proliferation activity including prostate Cancer (22RV1 IC50: 0.081 μM), colon cancer (colo-205 IC50: 0.1557 μM) and thyroid cancer(TT IC50: 0.037451 μM)[1].

Cell Proliferation Assay[1]

Cell Line: MV4-11 leukemia cells
Concentration: 100 nM
Incubation Time: ≥8 hours
Result: The BRD4 protein was reduced very efficiently.

Western Blot Analysis[1]

Cell Line: MV4-11 leukemia cells
Concentration: 10 , 50, 100, 500 nM
Incubation Time: 18 hours
Result: Performed depletion selectivity for BRD4 and BRD2 over BRD3, with good selectivity intra-BET proteins selectivity.
Molecular Weight

766.82

Formula

C₃₉H₃₈N₆O₉S

SMILES

O=C(NCCCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CCC4=CC5=C(NS(=O)(C6=CC=CC=C6OC)=O)C=CC(N(C)C7=O)=C5C7=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

PROTAC BRD2/BRD4 degrader-1Epigenetic Reader DomainPROTACProteolysis-targeting chimeraBETdegraderlowcytotoxicleukemiacellstumorslong-lastingselectiveantiproliferativeInhibitorinhibitorinhibit

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PROTAC BRD2/BRD4 degrader-1
Cat. No.:
HY-130612
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