repressive

TLX agonist 1 是一种孤核受体tailless (TLX, NR2E1)调节剂 (EC50=1 μM;Kd= 650 nM)。它能够提高 TLX 转录抑制活性。

Tazemetostat hydrobromide (E-7438 hydrobromide) 是口服的EZH2选择性抑制剂。它抑制含有 PRC2 复合体的野生型 EZH2 的活性，Ki 为 2.5 nM。它还抑制 EZH1，IC50为 392 nM。

ZLD1039 是一种口服有效的、高选择性 EZH2 抑制剂。ZLD1039 高效抑制 EZH2 野生型及 Y641F 和 A677G 突变型，IC50 分别为 5.6、15 和 4.0 nM。ZLD1039 抑制乳腺肿瘤的生长和转移。

A-395 是一种多梳抑制复合物 2 (PRC2) 蛋白质-蛋白质相互作用的拮抗剂，可有效抑制三聚体 PRC2 复合物 (EZH2-EED-SUZ12)，IC50为 18 nM。

ZL0580 通过抑制 Tat 反式激活和转录延伸以及通过在 HIV 启动子处诱导抑制性染色质结构来诱导 HIV 抑制。

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 包含一个 EED 配体 (IC50 = 247 nM) 和一个 von Hippel-Lindau 配体，是一种基于 PROTAC 的特异性多梳抑制复合物 2 (PRC2) 降解剂。

PRC1-IN-1（compound RB-4）是一种针对多梳抑制复合物PRC1的抑制剂，IC50为2.3 μM。其靶向 RING1B-BMI1、RING1A-BMI1 和 RING1B-PCGF1 的IC50分别为2.8、2.6 和 1.8 μM。

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.

ORIC-944 TFA 是可口服的且具有选择性的 polycomb 抑制复合物 2 (PRC2) 抑制剂，具有抗肿瘤活性，可用于研究转移性前列腺癌。