histone acetylation

R306465 (JNJ-16241199) 是一种具有口服活性和选择性的 I类组蛋白去乙酰化酶 (HDAC 1) 抑制剂，IC50 为 3.3 nM 。R306465 具有广谱的抗肿瘤活性，可诱导组蛋白 3 乙酰化，诱导细胞凋亡，可用于研究实体瘤和血液系统恶性肿瘤。

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。

Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。

Histone Acetyltransferase Inhibitor II 是一种选择性的细胞渗透性 p300 组蛋白乙酰转移酶抑制剂，IC50值为 5 µM。它在哺乳动物细胞中具有抗乙酰化酶活性，可用于癌症研究。

L002 是一种细胞可渗透的，可逆特定性乙酰转移酶 p300(KAT3B)抑制剂，IC50为 1.98 μM。 它结合乙酰辅酶 A 口袋并竞争性抑制 FATp300 催化结构域，阻断组蛋白乙酰化和 p53 乙酰化，且抑制 STAT3 激活，有用于高血压引起的心脏肥大和纤维化的研究潜力。

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。

HDAC-IN-7 是 Tucidinostat (Chidamide) 的类似物，是一种 HDAC 抑制剂。HDAC-IN-7 通过抑制组蛋白 H3 的乙酰化作用，诱导人类结肠癌细胞系的凋亡[1]。

PSF-IN-1 (Compound No.10-3) 是一种 RNA 结合蛋白 (PSF) 的抑制剂，能有效抑制 PSF-RNA 相互作用 (IC50: 2.2 pM)。它可以增加组蛋白乙酰化，抑制肿瘤细胞增殖并诱导细胞凋亡 (apoptosis)，具有抗肿瘤活性。

HDAC-IN-27 dihydrochloride (Compound 11h) 是一种有效的口服活性选择性HDACI抑制剂，对HDAC1-3的IC50值为0.43至3.01 nM。此外，HDAC-IN-27 dihydrochloride 在体内和体外均展现出抗癌活性。该化合物对急性髓系白血病 (AML) 细胞系表现出强抗增殖活性，并通过诱导细胞凋亡 (apoptosis) 和组蛋白乙酰化 (AcHH3和AcHH4) 发挥作用，对于急性髓系白血病 (AML) 的研究具有重要潜力。

CS4 是一种选择性HDAC抑制剂，其对HDAC1、HDAC6、HDAC8、HDAC4和HDAC11的IC50值分别为38 nM、12 nM、5.8 μM、19 μM和61 μM。CS4 促进α-微管蛋白和组蛋白3 (histone 3) 的乙酰化，同时激活PPARγ并抑制糖酵解 (glycolysis)。此外，CS4 可诱导细胞周期在G2期阻滞及细胞凋亡 (apoptosis)，并在体内外表现出抗癌活性。

EGFR/HDAC-IN-1 (Compound 22c2) 是一种有效抑制表皮生长因子受体 (EGFR) 和组蛋白去乙酰化酶 (HDAC) 的双重抑制剂，分别对 EGFR、HDAC1 和 HDAC3 的 IC50 值为 4.81 nM、119.4 nM 和 354.8 nM。EGFR/HDAC-IN-1 通过阻断EGFR信号通路和影响组蛋白乙酰化状态，抑制肿瘤细胞增殖。此化合物有望在非小细胞肺癌 (NSCLC) 的研究中发挥作用。

HDAC6-IN-41 (Compound E24) 是一种选择性抑制组蛋白脱乙酰酶 6 (HDAC6) 的化合物，对 HDAC6 和 HDAC8 的活性抑制分别表现出 IC50 为 14 和 422 nM。HDAC6-IN-41 可增加 α-微管蛋白和组蛋白位点 SMC3 的乙酰化水平。

NU 9056 是一种有效且选择性的 KAT5 组蛋白乙酰转移酶抑制剂，IC50 为 2 µM。 NU 9056 阻断 DNA 损伤反应并抑制前列腺癌细胞系中的蛋白质乙酰化。

HDAC3-IN-T247 (HDAC3 inhibitor T247) 是一种具有选择性和有效性的组蛋白去乙酰化酶 3（HDAC3） 抑制剂，具有抗癌和抗病毒活性。HDAC3-IN-T247 以剂量依赖的方式诱导人结肠癌 HCT116 细胞中 NF-κB 乙酰化。HDAC3-IN-T247 抑制癌细胞增殖。

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

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.

Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.1 and 3.2 sequences and is biotinylated via a C-terminal GK linker. Histone H3 (21-44) contains a lysine residue at position 23 that is subject to acetylation, an arginine at position 26 subject to methylation, and a serine at position 28 subject to phosphorylation, as well as lysine residues at positions 27 and 36 that are subject to methylation and acetylation. Histone H3 (21-44)-GK-biotin has been used as a substrate for the primate-specific histone methyltransferase PR domain-containing protein 7 (PRDM7) to determine substrate specificity.

Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010). Histone H2B (108-125) is a peptide fragment of histone H2B that corresponds to amino acid residues 109-126 of the human histone H2B sequence. It contains an N-terminal biotinylated lysine followed by a tryptophan linker. Histone H2B can be modified by addition of an O-linked N-acetylglucosamine (GlcNAc) moiety to the serine residue at position 112, which promotes monoubiquitination of the lysine at position 120.1 Both of these modifications are associated with active transcription. Histone H2B also has lysine residues at positions 108, 116, and 120 that are subject to acetylation.2 References1. Fujiki, R., Hashiba, W., Sekine, H., et al. GlcNAcylation of histone H2B facilitates its monoubiquitination. Nature 480(7378), 557-560 (2011).2. Portela, A., and Esteller, M. Epigenetic modifications and human disease. Nat. Biotechnol. 28(10), 1057-1068 (2010).

Selective p300 histone acetyltransferase (HAT) inhibitor (IC50 = 50-500 nM). Exhibits approximately 100-fold selectivity for p300 over PCAF (IC50 = 200 μM). Inhibits p300-dependent transcription. Active in vivo. Lau et al (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol.Cell. 5 589 PMID:10882143 |Liu et al (2008) The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451 846 PMID:18273021 |Burns et al (2005) Iso-coenzyme A. J.Biol.Chem. 280 16550 PMID:15708855 |Cebrat et al (2003) Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg.Med.Chem. 11 3307 PMID:12837541

Givinostat(ITF-2357)是一种非选择性和口服活性的HDAC抑制剂，能够抑制STAT5磷酸化，对crlf2重排的BCP-ALL具有抗肿瘤活性并诱导凋亡。Givinostat具有抗炎活性，在endotoxin刺激的PBMCs中抑制TNF-α和IL-1β，还能够促进β细胞的存活，可用于糖尿病、急性淋巴细胞白血病和关节炎。

Histone H3 (21-44)-GK-biotin is a peptide fragment of histone H3 that corresponds to amino acid residues 22-45 of the human histone H3.3 sequence and is biotinylated via a C-terminal GK linker. Unlike histone H3.1 and H3.2, the histone H3.3 variant contains a serine residue at position 31 that is phosphorylated during late prometaphase and metaphase of mitosis. Histone H3 (21-44) also contains lysine residues at positions 23, 27, and 36 that are subject to methylation and acetylation, all of which have a role in the regulation of gene expression, and a serine residue at position 28 that is subject to phosphorylation during mitosis.

Histone H3 (23-34) is a peptide consisting of amino acid residues 23 to 34 of the histone H3 protein. This peptide specifically includes lysine residues at positions 23 and 27, which can undergo methylation and acetylation modifications.

CXD101 是一种选择性和具有口服活性的 I 类HDAC 抑制剂，有抗肿瘤活性，对HDAC1、HDAC2和HDAC3的IC50分别为 63、570 和 550 nM。