PROTAC EZH2 Degrader-26
PROTAC EZH2 Degrader-26 (compound 11) is an EZH2 degrader developed based on PROTAC technology. PROTAC EZH2 Degrader-26 has an IC50 of 5.80 nM against EZH2. PROTAC EZH2 Degrader-26 exhibits micromolar-level enzyme inhibitory activity against EZH1, with an EZH1 IC50 of 0.06 μM.
(Pink: EZH2 ligand (HY-147230); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2641601-66-1
- Formula: C52H63N7O8
- Molecular Weight:914.10
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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EZH1 0.06 μM (IC50) |
EZH2 5.80 nM (IC50) |
In Vitro
EZH2 is a histone methyltransferase and the catalytic subunit of Polycomb Repressive Complex 2 (PRC2). It plays a pivotal role in tumor epigenetics by transcriptionally repressing tumor suppressor genes. As an epigenetic enzyme that exerts core regulatory functions in tumorigenesis and development, EZH2 serves as a target for existing therapies and a key research subject for the next-generation protein degradation technology (PROTACs)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 2641601-66-1
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Molecular Weight 914.10
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Formula C52H63N7O8
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SMILES
CC1=C(C=C(C=C1N(CC)C2CCOCC2)C3=CC=C(C=C3)CN4CCN(CC4)CCCCCOC5=C(C6=CC=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)C(NCC8=C(C=C(NC8=O)C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC EZH2 Degrader-26 Related Classifications
HY-181327 Related Classifications
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