PROTAC EZH2 Degrader-35
PROTAC EZH2 Degrader-35 (compound U3i (44)) is a PROTAC protein degrader targeting EZH2 with a human EZH2 Ka of 16.19 nM. PROTAC EZH2 Degrader-35 exhibits antiproliferative activity in triple-negative breast cancer cells and minimal cytotoxicity in normal human epithelial, hepatic, renal cells.PROTAC EZH2 Degrader-35 can be used for the research of triple-negative breast cancer.
(Pink: EZH2 ligand (HY-181393); Blue: Cereblon ligand (HY-10984); Black: linker).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 3034875-56-1
- Formel: C66H87N13O13
- Molecular Weight:1270.48
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.4 μM
Compound: U3i
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Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
Antiproliferative activity against human BT-549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay
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[PMID: 35623249] |
PROTAC EZH2 Degrader-35 binds to the PRC2 complex with high affinity, as shown by a Kd of 16.19 nM[1].
PROTAC EZH2 Degrader-35 potently inhibits the proliferation of MDA-MB-231 and MDA-MB-468 triple-negative breast cancer cells, with IC50 values of 0.57 μM and 0.38 μM, respectively[1].
PROTAC EZH2 Degrader-35 induces CRBN- and proteasome-dependent degradation of PRC2 complex components, reduces oncogenic histone modifications, triggers mitochondrial dysfunction and apoptosis in cancer cells, and shows minimal toxicity to normal human cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 3034875-56-1
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Molecular Weight 1270.48
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Formel C66H87N13O13
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SMILES
O=C(C1=CC(C2=CC=C(N3CCN(CC3)C(CCCCCCCCC4=CN(CCOCCOCCOCCOCCOCCOCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O)N=N4)=O)N=C2)=CC8=C1C=NN8C(C)C)NCC9=C(C)C=C(C)NC9=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)