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PROTAC BRD2/BRD4 degrader-1

Catalog No. T18598   CAS T18598

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].

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PROTAC BRD2/BRD4 degrader-1 Chemical Structure
PROTAC BRD2/BRD4 degrader-1, CAS T18598
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Biological Description
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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].
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].
Molecular Weight 766.82
Formula C39H38N6O9S
CAS No. T18598

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Jiang F, et al. Discovery of novel small molecule induced selective degradation of the bromodomain and extra-terminal (BET) bromodomain protein BRD4 and BRD2 with cellular potencies. Bioorg Med Chem. 2019 Nov 11:115181.

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Keywords

PROTAC BRD2/BRD4 degrader-1 T18598 Others PROTAC BRD2/BRD4 degrader 1 PROTAC BRD-2/BRD4 degrader-1 PROTAC BRD2/BRD4 degrader1 inhibitor inhibit

 

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