histone h4

Histone H4 (2-21) is a pivotal core histone involved in the process of chromatinization specific to the genomes of herpes simplex virus 1 (HSV-1).

Crebinostat 是一种有效的组蛋白去乙酰化酶 (HDAC) 抑制剂，对 HDAC1、HDAC2、HDAC3 和 HDAC6 有抑制作用， IC50 分别为 0.7 nM、1.0 nM、2.0 nM 和 9.3 nM。Crebinostat 可增加在体外神经元的突触蛋白 1 斑点沿树突 (synapsin-1 punctae along dendrites) 的密度。Crebinostat 可调节染色质介导的神经可塑性，增强小鼠的记忆。Crebinostat 可诱导组蛋白 H3 和组蛋白 H4 乙酰化，并增强 cAMP 反应元件结合蛋白 (CREB) 靶基因 Egr1 的表达。

1-Naphthohydroxamic acid 是一种选择性 HDAC8抑制剂，IC50为 14 μM。它对 HDAC8的选择性高于 I 类 HDAC1 和 II 类 HDAC6，IC50大于100 μM，可诱导微管蛋白乙酰化。

(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) 作为一种化合物，主要作用是抑制蛋白质精氨酸甲基转移酶 1 (PRMT1；组蛋白 H4 甲基化试验中IC50=11 μM)。此外，在 10 和 100 μM 的浓度下，此物质还能有效抑制 PRMT8 引起的组蛋白 H4 甲基化，但对于由 CARM1 或 Set7 9 引起的组蛋白 H3.1 甲基化则无影响。

AC-93253 iodide is a selective inhibitor of SIRT2. It significantly enhances the acetylation of tubulin p53 and histone H4.

MS2177 is a potent and selective inhibitor of SETD8, the only methyltransferase known to catalyze monomethylation of histone H4 lysine 20 (H4K20). MS2177 has an in vitro IC50 of 1.9 μM (σ = 1.05 μM, n = 4) in ascintillation proximity assay. Binding of MS2

CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300 CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid . At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.

Trichostatin C is a glycosylated derivative of trichostatin A , the antifungal antibiotic that reversibly inhibits histone deacetylase. Trichostatin C is reported to be the first example of a glucopyranosyl hydroxamate identified in nature. It has been shown to induce the differentiation of a mouse erythroleukemia cell line and to increase histone H4 acetylation in B cells, though at higher concentrations than trichostatin A.

Amredobresib is a potent BET inhibitor that impedes the interaction between bromodomains and acetylated lysines on histone H3 and H4, thereby serving as crucial regulators of gene transcription. It proves valuable in the investigation of acute myeloid leukemia (AML) and cancer.

[Nle20] H4 peptide (16−23) 是一种多肽,对组蛋白甲基转移酶SETD8展示出高度的抑制效力 (Kd=0.14 μM).该多肽通过竞争性结合SETD8的底物结合位点,有效阻断了SETD8对组蛋白 H4 的甲基化.因其显著的生物活性,[Nle20] H4 peptide (16−23) 可被视为抗癌治疗的潜在先导化合物.

Dihydrochlamydocinanalog-1 (compound 2) 是 Chlamydocin 的类似物，能够有效抑制组蛋白 H4 肽的去乙酰化，其 IC50 值为 30 nM。