PROTAC EZH2 Degrader-38
PROTAC EZH2 Degrader-38 (Compound 17) is a EZH2 PROTAC degrader with an IC50 of 165.00 nM. PROTAC EZH2 Degrader-38 functionally inhibits the methyltransferase activity of EZH2 and competitively binds to the SAM-binding pocket of the EZH2 SET domain.
(Pink: EZH2 ligand (HY-147230); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2653338-74-8
- Formula: C58H75N7O8
- Molecular Weight:998.26
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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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Cereblon |
EZH2 |
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 both a target of 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. 2653338-74-8
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Molecular Weight 998.26
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Formula C58H75N7O8
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SMILES
CCN(C1CCOCC1)C2=CC(C3=CC=C(C=C3)CN4CCN(CC4)CCCCCCCCCCCOC5=C(C6=CC=C5)C(N(C6=O)C7CCC(NC7=O)=O)=O)=CC(C(NCC8=C(C=C(NC8=O)C)C)=O)=C2C
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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-38 Related Classifications
HY-181333 Related Classifications
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