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DC-PRC2in-01

DC-PRC2in-01 is a potent EZH2-EED interaction inhibitor with an IC50 of 4.21 μM and a Kd of 4.56 μM. DC-PRC2in-01 disrupts the EZH2-EED interaction, leading to degradation of PRC2 core proteins and decrease of H3K27me3 levels, inhibition of PRC2-driven lymphoma cell proliferation, and cell cycle arrest. DC-PRC2in-01 can be used for the research of PRC2-related cancers, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL) [1].

Product Specifications

CAS Number

[120430-77-5]

UNSPSC

12352005

Target

Histone Methyltransferase

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

FC1=CC=C(CN2C(NC3CN(CC3)CCC4=CC=C(C=C4)OC)=NC5=C2C=CC=C5)C=C1

Molecular Formula

C27H29FN4O

Molecular Weight

444.54

References & Citations

[1]Du D, et al. Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction. J Med Chem. 2021;64 (12) :8194-8207.

Shipping Conditions

Room temperature

Scientific Category

Oligonucleotides

Clinical Information

No Development Reported

Isoform

EZH2

Curated Selection

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