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BRD4-IN-11

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Catalog No. T211473

BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis.

BRD4-IN-11

BRD4-IN-11

Copy Product Info
😃Good
Catalog No. T211473
BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis.
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Product Introduction

Bioactivity
Description
BRD4-IN-11 is an orally active and selective inhibitor of BRD4 with an IC50 of 26.35 nM for BD1 and 72.81 nM for BD2. Its potency against BRD4 is approximately 3 to 18 times greater than against BRr2, BRD3, and BRDT. BRD4-IN-11 increases H2S release and inhibits the upregulation of fibrosis markers (α-SMA and fibronectin), c-Myc, and CDC25B. It also reduces apoptosis in LO2 hepatic cells. In liver and lung fibrosis models, BRD4-IN-11 significantly improves liver and lung function, making it suitable for research on liver and lung fibrosis.
Targets&IC50
BRD4 BD1:26.35 nM
In vitro
BRD4-IN-11 (Compound 11r) demonstrates inhibitory effects on LX-2 cells. When applied at concentrations of 0.5-2.0 μM for 48 hours, BRD4-IN-11 reduces the apoptosis rate in LO2 cells treated with Carbon tetrachloride (CCl_4) and inhibits the expression of CDC25B, α-SMA, c-Myc, and fibronectin.
In vivo
BRD4-IN-11 (Compound 11r), administered orally at 15-30 mg/kg once daily for 3 days, serves to prevent liver injury and fibrosis via a dual mechanism: it inhibits hepatocyte apoptosis and fibrosis protein expression in a CCl4-induced mouse liver injury model. Additionally, BRD4-IN-11 given at the same dosage and frequency for 15 days can prevent pulmonary fibrosis in a Bleomycin (BLM)-induced lung fibrosis (PF) model.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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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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