histone deacetylation

CG-200745 is a potent inhibitor of HDAC. CG200745 induces apoptosis and also inhibits the deacetylation of histone H3 and tubulin.

Ac-RGK(Ac)-AMC, fluorogenic substrate for assaying histone deacetylase (HDAC) activity in a two-step enzymatic reaction. The assay consists of the initial lysine deacetylation by HDAC followed by the release of the fluorescent group by trypsin.

Ivaltinostat (CG-200745) formic 是一种口服具有活力的泛 HDAC 抑制剂，具有异羟肟酸部分，能够在催化袋底部结合锌。Ivaltinostat formic 对组蛋白 H3 和微管蛋白的脱乙酰作用具有抑制效果。Ivaltinostat formic 能够促使 p53 的积累，诱导 p53 依赖性反式激活，并提高 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 增加 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU) 的敏感性。Ivaltinostat formic 诱导凋亡，并具有抗肿瘤效果。

MDL-800，一种选择性SIRT6激活剂，通过将SIRT6的脱乙酰化活性提高多达22倍，有效促进了人类肝细胞癌(HCC)细胞中H3K9ac和H3K56ac水平的全面降低。SIRT6，作为一种肿瘤抑制因子，主要负责去乙酰化组蛋白H3 Nε-乙酰基赖氨酸9 (H3K9ac) 和56 (H3K56ac)，在多种癌症中常发现其表达量低下。此外，MDL-800通过SIRT6驱动的细胞周期阻滞，抑制了HCC细胞的增殖，并在肿瘤异种移植模型中显示出了效果。

Bisthianostat, also known as CF367 or CF367;-C, is a novel Orally Efficacious Pan-HDAC Inhibitor. Bisthianostat selectively binds to and inhibits HDACs, which inhibits deacetylation of histone proteins and leads to the accumulation of highly acetylated histones. This may result in an induction of chromatin remodeling, the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes. This prevents cell division, induces cell cycle arrest and apoptosis. This may inhibit the proliferation of susceptible tumor cells. HDACs, upregulated in many tumor cell types, are a family of enzymes that deacetylate histone proteins.

Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.

JAK/HDAC-IN-2 是一款高效的 JAK/HDAC 双靶点抑制剂，能在纳摩尔浓度范围内有效抑制 HDAC3/6 与 JAK1/2。此化合物不仅促进细胞凋亡，还能抑制组蛋白去乙酰化和 STAT3 磷酸化，对血液肿瘤和实体肿瘤细胞展现出了显著的抗增殖效果。

BMf-BH3 belongs to the Bcl-2 apoptosis mediator family. This peptide belongs to the Bcl-2 apoptosis mediator family. Bmf is a key player in histone deacetylase (HDAC) inhibition, which alters the balance between deacetylation and acetylation.

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。