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EBET-1055

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Catalog No. T87715

EBET-1055 is a degrader of bromodomain and extra-terminal (BET) proteins, consisting of a BET inhibitor (EBET-590), an E3 ubiquitin ligase ligand, and connectors. It effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC) and also modulates cancer-associated fibroblast (CAF) activity, enhancing all reporter gene activities in organoid co-cultures [1].

EBET-1055

EBET-1055

😃Good
Catalog No. T87715
EBET-1055 is a degrader of bromodomain and extra-terminal (BET) proteins, consisting of a BET inhibitor (EBET-590), an E3 ubiquitin ligase ligand, and connectors. It effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC) and also modulates cancer-associated fibroblast (CAF) activity, enhancing all reporter gene activities in organoid co-cultures [1].
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Product Introduction

Bioactivity
Description
EBET-1055 is a degrader of bromodomain and extra-terminal (BET) proteins, consisting of a BET inhibitor (EBET-590), an E3 ubiquitin ligase ligand, and connectors. It effectively inhibits the growth of pancreatic ductal adenocarcinoma (PDAC) and also modulates cancer-associated fibroblast (CAF) activity, enhancing all reporter gene activities in organoid co-cultures [1].
In vitro
EBET-1055 (1 nM, 10 nM; 2 d) reduces IL-6 and LIF secretion during the co-culture of mouse CAFs with PC-3 or PC-42 cancer cells [1]. This compound shows potential anti-inflammatory or anti-fibrotic properties. It may inhibit BRD protein interaction with STAT3 and SMAD3, thereby hindering myofibroblast differentiation and reducing SMAD3 and STAT3 phosphorylation levels in fibrotic mouse kidneys [1]. In a Western Blot Analysis using PC-3 cells or mouse CAFs, EBET-1055 at concentrations of 0.1, 1, 10, and 100 nM for 24 hours decreased the phosphorylation levels of STAT3Y705, SMAD2S465/467, and SMAD3S423/425 [1].
Chemical Properties
Molecular Weight923.02
FormulaC51H54N8O9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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