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VVD 065

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Catalog No. T212577

VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth.

VVD 065

VVD 065

😃Good
Catalog No. T212577
VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth.
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
VVD 065 is an NRF2 inhibitor that functions through a covalent allosteric binding mechanism. It promotes the degradation of NRF2 by covalently bonding with C151 on KEAP1, thereby enhancing the formation of the KEAP1-CUL3 ubiquitin ligase complex. With potent target binding affinity (TE50 of 9 nM in KYSE70 cells) and selectivity for unrelated targets, VVD 065 effectively inhibits NRF2-associated cell growth.
In vitro
VVD 065 inhibits NRF2 transcriptional activity and reduces the expression of NRF2 target genes.
In vivo
VVD 065 promotes tumor growth inhibition and downregulates the NRF2 signaling pathway in both cell lines and mouse xenograft models, acting synergistically with other combinations. Additionally, VVD 065 is orally bioavailable.
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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In Vivo Formulation Calculator (Clear solution)

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:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

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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