h3k4

Sinefungin (Adenosyl-Ornithine) 是病毒粒子mRNA (鸟嘌呤-7-)-甲基转移酶、 mRNA (核苷-2'-)-甲基转移酶和病毒增殖的有效抑制剂。它还抑制SET7 9，通过抑制H3K4甲基化来改善肾纤维化。

OICR-9429 是一个新颖的相互作用的小分子Wdr5-MLL 拮抗剂，IC50是 5 uM，在体外抑制急性髓性白血病细胞。

A-366 是一种高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC50分别为 3.3 和 38 nM。它比其他 21 种甲基转移酶具有 1000 倍以上的选择性。它是 Spindlin1-H3K4me3相互作用的抑制剂，IC50为182.6 nM。它对人 H3R 表现出很高的亲和力，Ki 值为 17 nM，在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。

KDM5-C70 是 KDM5-C49 的乙酯衍生物，是一种有效的细胞渗透性泛 KDM5 组蛋白去甲基化酶抑制剂。它在骨髓瘤细胞中具有抗增殖作用，可诱导全基因组 H3K4me3 水平升高。

T-448 是一种可口服且具有高效性的赖氨酸特异性去甲基化酶1 抑制剂（IC50：22 nM），可改善小鼠的学习功能。T-448 可用于研究记忆缺陷。

(iso)-T 448 是一种 T 448 的旋光异构体。T-448 是高效的赖氨酸特异性去甲基化酶1 (LSD1) 抑制剂，可诱导大鼠神经元中H3K4的甲基化。

KDOAM-25 citrate 是有效且具有高选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂，对 KDM5A，KDM5B，KDM5C，KDM5D 的IC50分别为 71 nM，19 nM，69 nM，69 nM。用KDOAM-25 citrate 处理的多发性骨髓瘤 MM1S 细胞显示转录起始位点的整体 H3K4 甲基化增加，增殖受损。

KDOAM-25 trihydrochloride increases global H3K4 methylation at transcriptional start sites and impairs proliferation in multiple myeloma MM1S cells. KDOAM-25 trihydrochloride is a potent and highly selective histone lysine demethylases 5 (KDM5) inhibitor

KDOAM-25, a potent and highly selective inhibitor of histone lysine demethylases 5 (KDM5) with IC50 values of 71 nM for KDM5A, 19 nM for KDM5B, 69 nM for KDM5C, and 69 nM for KDM5D, enhances global H3K4 methylation at transcriptional start sites and reduces proliferation in multiple myeloma MM1S cells.

T-448 free base is a specific, orally active and irreversible lysine-specific demethylase 1 (LSD1, an H3K4 demethylase) inhibitor(IC50 of 22 nM).

CPI-455 is a specific KDM5 inhibitor with IC50 value of 10 ± 1 nM for full-length KDM5A in enzymatic assays, elevating global levels of H3K4 trimethylation (H3K4me3) and decreased the number of DTPs in multiple cancer cell line models treated with target

MM-401 is a specific inhibitor of histone H3K4 methyltransferase MLL1 activity that acts by reprogramming mouse epiblast stem cells to naive pluripotency.

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.

E67-2, a derivative of E67, is a low-toxicity, selective inhibitor of the KIAA1718 Jumonji domain. It has an IC 50 value of 3.4 μM. E67-2 specifically inhibits the Jumonji demethylase for histone H3 lysine 9 (H3K9) and histone H3 lysine 4 (H3K4) demethylase.

cis-4-Br-2,5-F2-PCPA (S1024) 抑制 LSD1 和 LSD2，Ki 值分别为 94 nM 和 8.4 μM。癌症干细胞中 LSD1异常表达，cis-4-Br-2,5-F2-PCPA 能够通过增加 CCRF-CEM 细胞中二甲基化组蛋白 H3 的 K4 (H3K4) 水平，抑制 LSD1活性和癌细胞增殖。

KDOAM-25 trihydrochloride 是一种有效的、高度选择性的组蛋白赖氨酸脱甲基酶 5 (KDM5) 抑制剂，能够作用于 KDM5A (IC50: 71 nM)、KDM5B (IC50: 19 nM)、KDM5C (IC50: 69 nM)、KDM5D (IC50: 69 nM)。KDOAM-25 trihydrochloride 能够提高转录起始位点的整体 H3K4 甲基化，可阻碍多发性骨髓瘤 MM1S 细胞的增殖。

MRK-740 是一种具有高效性和选择性的 PRDM9 组蛋白甲基转移酶抑制剂。MRK-740 对其他组蛋白甲基转移酶具有抑制作用，抑制PRDM9依赖性的 H3K4 三甲基化 。

Bomedemstat (IMG-7289) hydrochloride 是一种口服具有活力的、不可逆的 lysine-specific demethylase 1(LSD1) 抑制剂。Bomedemstat hydrochloride 能够增加 H3K4 和 H3K9 的甲基化，并改变基因表达。Bomedemstat hydrochloride 能够抑制癌细胞增殖并诱导细胞凋亡，表现出抗癌效果。

WDR5-0102为针对WDR5-MLL1的抑制剂(Kdis=7 μM, Kd=4 μM)。该化合物有效抑制MLL1活性，而对人类H3K4甲基转移酶SETD7及其他六种HMT（G9a、EHMT1、SUV39H2、SETD8、PRMT3、PRMT5）不表现出抑制作用。

INCB059872, also known as INCB59872, is a potent, selective, and orally active lysine-specific demethylase 1 inhibitor. INCB059872 binds to and inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone H3 (H3K4) to mono- and unmethylated H3K4, respectively, through amine oxidation. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor-suppressor genes. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes.

MM-401 (TFA) 是一种针对MLL1 H3K4甲基转移酶的抑制剂，通过阻断MLL1与WDR5的相互作用，有效抑制MLL1活性，其IC50值为0.32 µM。此化合物能够诱导细胞周期停滞、凋亡及分化，主要用于MLL白血病的研究。

MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5 MLL 相互作用抑制剂，在 WDR5 结合检测中，IC50为 2.4 nM，Ki 小于 1 nM。