prc2

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.

MAK683 hydrochloride embryonic ectodermal development (EED) inhibitor, also a potent PRC2 inhibitor, blocked cancer cell proliferation (IC50=1.014nM), with IC50 values of 59, 26, and 89 nM measured in EED Alphascreen, ELISA, and LC-MS assays, respectively.

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.

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.

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).

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).

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

Boc-NH-C4-acid is a PROTAC linker of the Alkyl ether class, utilized in the synthesis of PROTAC1 for the degradation of EED, EZH2, and SUZ12 in [PRC2].

PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a 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

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a potent EZH2 degrader that exhibits strong inhibitory effects not only on EZH2 protein expression but also on the levels of other PRC2 subunits and H3k27me3 protein. Additionally, PROTAC EZH2 Degrader-3 demonstrates antiproliferative activity by blocking the cell cycle at the G0-G1 phase and inducing apoptosis (cell death). At a concentration of 5 μM and over a period of 24 hours, it effectively suppresses the expression of these critical proteins involved in cell regulation and growth.

ORIC-944 TFA is an orally available selective polycomb repressive complex 2 (PRC2) inhibitor with antitumor activity, useful in metastatic prostate cancer research.

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

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

16-Hydroxycleroda-3,13-dien-15,16-olide and prodigiosin are candidates for autophagy inducers that can trigger cell death as a supplement or alternative medicine for cancer therapy. 16-Hydroxycleroda-3,13-dien-15,16-olide regulates the expression of histone-modifying enzymes (PRC2 complex) and induces apoptosis in CML [K562] cells; it also exhibits anti-inflammatory activity, showing promising NO inhibitory activity at 10 ug mL.

ORIC-944 is an orally available and selective variant of PRC2 with anticancer activity for prostate cancer research.

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

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].

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

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.

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.