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VCP/p97 IN-3

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Catalog No. T211477

VCP/p97 IN-3 is an allosteric inhibitor of VCP/p97. It exhibits inhibitory activity against VCP, with an IC50 of 9 nM, and shows IC50 values of 12 nM (N660K) and 19 nM (V474A/D649A) for mutant VCP proteins. VCP/p97 IN-3 increases the levels of K48 ubiquitination and caspase-3. It activates endoplasmic reticulum stress and the unfolded protein response (UPR). In a subcutaneous xenograft mouse model with RPMI-8226 cells, VCP/p97 IN-3 suppresses tumor growth. This compound is applicable for research in multiple myeloma.

VCP/p97 IN-3

VCP/p97 IN-3

Copy Product Info
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Catalog No. T211477
VCP/p97 IN-3 is an allosteric inhibitor of VCP/p97. It exhibits inhibitory activity against VCP, with an IC50 of 9 nM, and shows IC50 values of 12 nM (N660K) and 19 nM (V474A/D649A) for mutant VCP proteins. VCP/p97 IN-3 increases the levels of K48 ubiquitination and caspase-3. It activates endoplasmic reticulum stress and the unfolded protein response (UPR). In a subcutaneous xenograft mouse model with RPMI-8226 cells, VCP/p97 IN-3 suppresses tumor growth. This compound is applicable for research in multiple myeloma.
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Product Introduction

Bioactivity
Description
VCP/p97 IN-3 is an allosteric inhibitor of VCP/p97. It exhibits inhibitory activity against VCP, with an IC50 of 9 nM, and shows IC50 values of 12 nM (N660K) and 19 nM (V474A/D649A) for mutant VCP proteins. VCP/p97 IN-3 increases the levels of K48 ubiquitination and caspase-3. It activates endoplasmic reticulum stress and the unfolded protein response (UPR). In a subcutaneous xenograft mouse model with RPMI-8226 cells, VCP/p97 IN-3 suppresses tumor growth. This compound is applicable for research in multiple myeloma.
In vivo
VCP/p97 IN-3 (Compound 38) administered intraperitoneally at doses of 50-100 mg/kg every other day for 23 days effectively inhibits tumor growth in an RPMI-8226 cell subcutaneous xenograft mouse 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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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:
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2 Enter the in vivo formulation:
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% Saline/PBS/ddH2O

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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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