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PROTAC EZH2 Degrader-44
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Catalog No. T219081 Copy Product Info
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PROTAC EZH2Degrader-44 (compound 60) is a potent PROTAC degrader that targets the EZH2-PRC2 complex. It functions by recruiting the CRBN E3 ligase, relying on the proteasome system to degrade the core components EZH2, SUZ12, and EED, effectively reducing H3K27me3 and CARM1 levels. This compound exhibits antiproliferative effects through a dual mechanism: inducing mitochondrial dysfunction, which leads to decreased membrane potential, and regulating Bcl-2 family proteins (by upregulating Bax, Caspase-3, and PARP and downregulating Bcl-2), thereby significantly promoting apoptosis. PROTAC EZH2Degrader-44 demonstrates minimal cytotoxicity in human normal breast epithelial, liver, and kidney cells, providing a favorable safety profile. It is an ideal tool molecule for exploring targeted therapy mechanisms for triple-negative breast cancer.
PROTAC EZH2 Degrader-44
Cas No. 3093642-25-9
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PROTAC EZH2Degrader-44 (compound 60) is a potent PROTAC degrader that targets the EZH2-PRC2 complex. It functions by recruiting the CRBN E3 ligase, relying on the proteasome system to degrade the core components EZH2, SUZ12, and EED, effectively reducing H3K27me3 and CARM1 levels. This compound exhibits antiproliferative effects through a dual mechanism: inducing mitochondrial dysfunction, which leads to decreased membrane potential, and regulating Bcl-2 family proteins (by upregulating Bax, Caspase-3, and PARP and downregulating Bcl-2), thereby significantly promoting apoptosis. PROTAC EZH2Degrader-44 demonstrates minimal cytotoxicity in human normal breast epithelial, liver, and kidney cells, providing a favorable safety profile. It is an ideal tool molecule for exploring targeted therapy mechanisms for triple-negative breast cancer. |
| Molecular Weight | 1193.50 |
| Formula | C65H84N12O8S |
| Cas No. | 3093642-25-9 |
| Smiles | N(CC)(C1=CC(=CC(C(NCC2=C(C)C=C(C)NC2=O)=O)=C1C)C3=CC=C(CN4CCN(C(=O)C5=CN(CCCCCC(N[C@H](C(=O)N6[C@H](C(NCC7=CC=C(C=C7)C8=C(C)N=CS8)=O)C[C@@H](O)C6)C(C)(C)C)=O)N=N5)CC4)C=C3)C9CCOCC9 |
| Storage | Powder: -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:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
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 DMSO 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 DMSO stock solution to 400 µL PEG300 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 ddH2O 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.
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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