1. PROTAC Epigenetics
  2. PROTACs Histone Methyltransferase
  3. 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.

PROTAC EZH2 Degrader-35

PROTAC EZH2 Degrader-35 Chemical Structure

CAS No. : 3034875-56-1

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Description

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[1]. (Pink: EZH2 ligand (HY-181393); Blue: Cereblon ligand (HY-10984); Black: linker).

In Vitro

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.

Molecular Weight

1270.48

Formula

C66H87N13O13

CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Product Name:
PROTAC EZH2 Degrader-35
Cat. No.:
HY-181392
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