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
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cereblon |
EZH2 |
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.
Chemical Information
-
CAS No. 2653338-74-8
-
Molecular Weight 998.26
-
Formula C58H75N7O8
-
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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)