repressive

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).

ZL0580 induces HIV suppression by inhibiting Tat transactivation and transcription elongation as well as by inducing repressive chromatin structure at the HIV promoter.

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).

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.

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

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.

Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 μM.1It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

PRC1-IN-1 (compound RB-4) is an inhibitor of the polycomb repressive complex 1 (PRC1) with an IC50 of 2.3 μM. It targets RING1B-BMI1, RING1A-BMI1, and RING1B-PCGF1, exhibiting IC50 values of 2.8 μM, 2.6 μM, and 1.8 μM, respectively.

TLX agonist 1 is an orphan nuclear receptor tailless (TLX, NR2E1) modulator

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.