Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

ZLD1039 is a potent, orally bioavailable EZH2 (Enhancer of Zeste Homolog 2) inhibitor with high selectivity. It demonstrates strong, concentration-dependent inhibition of both wild-type and mutant (Y641F and A677G) PRC2 (Polycomb Repressive Complex 2) enzymatic activities, exhibiting IC50 values of 5.6, 15, and 4.0 nM, respectively. Additionally, ZLD1039 effectively suppresses breast tumor growth and metastasis.

Tazemetostat hydrobromide (E-7438 hydrobromide) is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27),is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.11.

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

Boc-NH-C4-acid is a PROTAC linker belonging to the Alkyl/ether class, which can be used for the synthesis of PROTAC1 and can degrade EED, EZH2, and SUZ12 in PRC2.

PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.

JQEZ5 is an inhibitor of EZH2 lysine methyltransferase (IC50 = 11.1 nM).

BRD9539 is an inhibitor of euchromatin histone methyltransferase 2 (EHMT2), also known as G9a, with an IC50 value of 6.3 μM

16-Hydroxycleroda-3,13-dien-15,16-olide, and prodigiosin are presented as candidates for autophagy inducers that can trigger cell death in a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expre

SPEN-IN-1 binding suppresses histone H3K27 trimethylation and blocks initiation of X-chromosome inactivation. SPEN-IN-1 binding reduces the conformational space of RepA and displaces cognate interacting protein factors including PRC2 and SPEN.

MS177, a potent and rapid EZH2 degrader, functions as a PROTAC comprised of a CRBN ligand, linker, and a powerful enzymatic EZH2 inhibitor C24 (C24 IC50: 12 nM). It successfully targets and depletes both canonical EZH2–PRC2 and noncanonical EZH2–cMyc complexes. Furthermore, MS177 inhibits leukemia cell growth, induces apoptosis, and arrests cell cycle progression.

EED226 is a potent, selective, and orally bioavailable embryonic ectoderm development (EED) inhibitor with an IC50 of 22 nM.

EED226-COOH, derived from EED226, serves as a ligand targeting the EED protein for PROTAC applications. It attaches to a VHL ligand through a linker, culminating in the formation of UNC6852, which specifically degrades PRC2[1].

UNC6852 contains an EED ligand (IC50 = 247 nM) and a von Hippel-Lindau ligand and is a selective polycomb repressive complex 2 (PRC2) degrader based on PROTAC.

A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12, IC50: 18 nM).

EED ligand 1 is a highly versatile, potent, and effective inhibitor that specifically targets the EED subunit of the polycomb repressive complex 2 (PRC2) methyltransferase.

EZH2-IN-14 is a selective inhibitor of EZH2 (Histone Methyltransferase), demonstrating potent inhibition with an IC50 value of 12 nM. It specifically targets the methyltransferase activity of EZH2/PRC2, effectively reducing H3K27me3 levels. Moreover, EZH2-IN-14 exhibits more than 200-fold selectivity for EZH2 over the closely related H3K27 methyltransferase, EZH1.