repressive

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

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).

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.

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

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.

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.

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

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.

MS181 (compound 1) is an efficient PROTAC degrader that recruits cereblon (CRBN) and binds to the ubiquitin complex polycomb repressive complex 1 (PRC1). It reduces the expression of EED, EZH2, SUZ12, BMI1, and RING1B, and exhibits antiproliferative activity.

rel-A-395 hydrochloride is the relative configuration of A-395 hydrochloride. A-395 is an antagonist of protein-protein interactions within the polycomb repressive complex 2 (PRC2). It inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 value of 18 nM.

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.

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.

FX-909 is a covalent peroxisome proliferator–activated receptor gamma (PPARγ) inverse agonist developed for advanced solid malignancies, including muscle-invasive bladder cancer, and functional profiling and NMR studies demonstrate that FX-909 exhibits enhanced corepressor-selective inverse agonism and superior stabilization of a transcriptionally repressive PPARγ ligand-binding domain conformation compared with T0070907.

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

H3K27(Me) (15-34) is a histone peptide derived from human histones and serves as a repressive mark. The methylation of H3K27(Me) is catalyzed by PRC2.

H3K27(Me2) (15-34) is a histone peptide originating from human histones, known as an inhibitory chromatin marker. The Polycomb Repressive Complex 2 (PRC2) is a multiprotein complex that catalyzes the methylation of H3K27(Me).