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MS147

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Catalog No. T209960

MS147 is a VHL-based PROTAC PRC1 degrader. It shows binding affinity (Kd) of 3.0 μM to EED and 450 nM to VHL. The compound selectively targets the EED protein, a crucial component of PRC2, through its EED ligand portion, and interacts with PRC1 core components BMI1 and RING1B. This interaction enables MS147 to recruit BMI1 and RING1B near VHL, leading to their degradation. As a result, MS147 reduces the ubiquitination level of H2AK119ub, thereby impacting the proliferation of cancer cells.

MS147

MS147

😃Good
Catalog No. T209960
MS147 is a VHL-based PROTAC PRC1 degrader. It shows binding affinity (Kd) of 3.0 μM to EED and 450 nM to VHL. The compound selectively targets the EED protein, a crucial component of PRC2, through its EED ligand portion, and interacts with PRC1 core components BMI1 and RING1B. This interaction enables MS147 to recruit BMI1 and RING1B near VHL, leading to their degradation. As a result, MS147 reduces the ubiquitination level of H2AK119ub, thereby impacting the proliferation of cancer cells.
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Product Introduction

Bioactivity
Description
MS147 is a VHL-based PROTAC PRC1 degrader. It shows binding affinity (Kd) of 3.0 μM to EED and 450 nM to VHL. The compound selectively targets the EED protein, a crucial component of PRC2, through its EED ligand portion, and interacts with PRC1 core components BMI1 and RING1B. This interaction enables MS147 to recruit BMI1 and RING1B near VHL, leading to their degradation. As a result, MS147 reduces the ubiquitination level of H2AK119ub, thereby impacting the proliferation of cancer cells.
Chemical Properties
FormulaC54H70N12O6S
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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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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