EZH2-IN-23

EZH2-IN-23 (Compound 25) is an EZH2 inhibitor that exhibits potent enzymatic inhibition of the PRC2 complex (EZH2, EED, SUZ12, AEBP2, RbAp48) with a biochemical IC50 of 0.8 nM. EZH2-IN-23 inhibits H3K27 trimethylation in cellular assays, showing an IC50 of 40 nM. EZH2-IN-23 displays good rat PKproperties with 100 % oral bioavailability[1].

Product Specifications

CAS Number

[3095068-20-2]

UNSPSC

12352100

Target

Histone Methyltransferase

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

CC(N1)=CC(C)=C(CN2CCC(SC([C@H](C)C3CCN(CC4=NC=C(Cl)C=C4)CC3)=C5C)=C5C2=O)C1=O

Molecular Formula

C29H35ClN4O2S

Molecular Weight

539.13

References & Citations

[1]Tian X, et, al. Asymmetric synthesis of potent and orally bioavailable thiophene-based EZH2 inhibitors. Bioorg Med Chem Lett. 2025 May 30;127:130291.