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).
For research use only. We do not sell to patients.
- CAS No.: 3034875-56-1
- Formula: C66H87N13O13
- Molecular Weight:1270.48
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BT-549 | IC50 |
0.4 μM
Compound: U3i
|
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
|
[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
-
CAS No. 3034875-56-1
-
Molecular Weight 1270.48
-
Formula C66H87N13O13
-
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
-
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)
Powered by Bioz