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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

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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].
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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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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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