PROTAC EZH2 Degrader-13
PROTAC EZH2 Degrader-13 is an EZH2-targeting PROTAC with an IC50 of 2.70 nM. PROTAC EZH2 Degrader-13 exerts antiproliferative effects in cancer cells. PROTAC EZH2 Degrader-13 can be used for the research of cancer.
(Pink: EZH2 ligand (HY-13470); Blue: Cereblon ligand (HY-103596); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 2653338-63-5
- Formula: C51H60N8O7
- Molecular Weight:897.07
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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
[1]|
EZH2 2.70 nM (IC50) |
EZH1 4.50 μM (IC50) |
In Vitro
PROTAC EZH2 Degrader-13 (compound 4) potently inhibits EZH2 enzymatic activity (IC50 = 2.7 nM), induces CRBN-mediated proteasomal degradation of PRC2 subunits, reduces H3K27me2/3 levels, and exerts antiproliferative effects in Pfeiffer and prostate cancer cell lines[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. 2653338-63-5
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Molecular Weight 897.07
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Formula C51H60N8O7
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SMILES
CC[C@H](C)N1C=C(C)C2=C(C(NCC3=C(C)C=C(C)NC3=O)=O)C=C(C4=CN=C(N5CCN(CCCCCCCOC6=C7C(N(C8CCC(NC8=O)=O)C(C7=CC=C6)=O)=O)CC5)C=C4)C=C21
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC EZH2 Degrader-13 Related Classifications
HY-181308 Related Classifications
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