deacetylation

Selisistat (EX-527) 是一种去乙酰化酶 SIRT1 的抑制剂 (IC50=38 nM)，具有有效性和特异性。Selisistat 可以用于神经系统疾病如亨廷顿舞蹈病的研究。

4-Hydroxyestrone 是一种内源性雌激素代谢物，可强烈保护神经元细胞免受氧化损伤。

YK-3-237 (B-[2-Methoxy-5-[(1E)-3-oxo-3-(3,4,5-trimethoxyphenyl)-1-propen-1-yl]phenyl]boronic acid) 是 SIRT1 激活剂，靶向突变体 p53。它抑制三阴性乳腺癌细胞的增殖。

Exifone (NSC-680919) 是一种混合的、非必需的 HDAC1 激活剂，能够与游离酶和底物结合酶结合，从而提高 HDAC1 催化的去乙酰化的相对最大速率。

SIRT5 inhibitor 2 (compound 49) 是一种有效的SIRT5抑制剂，IC50=2.3 μM，能够抑制SIRT5 依赖的去乙酰化，可用于研究癌症和神经退行性疾病。

CAY10602 是一种SIRT1激活剂，可剂量依赖性地抑制 THP-1 细胞中脂多糖对 TNF-α 的 NF-κB 依赖性诱导。

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

SRTCX1002 is a SIRT1 Activator Suppressing Inflammatory Responses through Promotion of p65 Deacetylation and NF-κB Activity inhibitor.

Herkinorin is an opioid analgesic and an analogue of the natural product Salvinorin A. herkinorin is a μ-opioid agonist with more than 100x higher μ-opioid affinity and 50x lower κ-opioid affinity compared to Salvinorin A. Herkinorin is a semi-synthetic c

SRTCX1003, a SIRT1 activator, suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB activity.

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.

S2116 is a powerful inhibitor of lysine-specific demethylase 1 (LSD1), and it is a derivative of N-alkylated tranylcypromine (TCP). S2116 exhibits its inhibitory effects by increasing H3K9 methylation and inducing reciprocal H3K27 deacetylation at super-enhancer regions. In TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells, S2116 triggers apoptosis by repressing the transcription of NOTCH3 and TAL1 genes. Furthermore, S2116 demonstrates significant growth retardation of T-ALL cells when xenotransplanted into mice.

BPK-25 is an active acrylamide compound that enhances the degradation of proteins in the nucleosome remodeling and deacetylation (NuRD) complex through a post-translational mechanism involving covalent protein interaction. Additionally, BPK-25 acts as an inhibitor of TMEM173 activation by the cyclic dinucleotide ligand cGAMP.

SIRT5 inhibitor 3 是一种有效和竞争性的 SIRT5 抑制剂，通过抑制 SIRT5 去乙酰化发挥作用，在代谢调节、癌症治疗、神经退行性疾病、心血管疾病和其他疾病中具有潜在的应用价值。

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。

HDAC1 6-IN-1 是一种有效的 GLP (IC50: 1.3 nM)、HDAC6 (IC50: 13 nM) 和 HDAC1 (IC50: 89 nM)的多靶点抑制剂。HDAC1 6-IN-1 能在蛋白水平上抑制 H3K9 的甲基化和去乙酰化。HDAC1 6-IN-1 能够将癌细胞的细胞周期阻滞在 G0 G1 期，能够诱导癌细胞凋亡，可阻止癌细胞迁移和入侵。

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。

MDL-801 is an activator of SIRT6 deacetylation.

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。

Sirt1 2-IN-2 (compound hsa55)是一种针对SIRT1 2的双重抑制剂，具有分别针对SIRT1和SIRT2的IC50值为1.8 μM和2.4 μM。该化合物能有效阻止p53的脱乙酰化作用，并提高p53及α-微管蛋白的乙酰化水平。此外，Sirt1 2-IN-2能诱导细胞凋亡，并展示出对人白血病细胞系的抗增殖效果。

Sirt1 2-IN-3 (compound PS9) 作为SIRT1 2的双重抑制剂，其对SIRT1和SIRT2的IC50值分别为1.4 μM 和 2.0 μM。该化合物能够有效抑制p53脱乙酰化，并提升p53与α-微管蛋白的乙酰化水平。Sirt1 2-IN-3还能诱导细胞凋亡，并展现对人白血病细胞系的抗增殖效果。

Sirt1 2-IN-4（compound PS3）为SIRT1 2 3抑制剂，其IC50分别为1.2 μM (SIRT1)、1.9 μM (SIRT2) 和2.0 μM (SIRT3)。该化合物能完全阻制p53脱乙酰化作用，显示出潜在的抗癌活性。