hydroxamic

Caracemide (NSC-253272) 抑制大肠杆菌的核糖核苷酸还原酶。 Caracemide 可用于抗癌研究。

Vorinostat (SAHA) 是一种泛的组蛋白脱乙酰酶 (HDAC) 抑制剂 (IC50=10 nM)，对 HDAC1 2 3 6 7 11 均有抑制活性。 Vorinostat 具有抗肿瘤活性，可以诱导细胞分化，阻滞细胞周期，诱导细胞凋亡。

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. [1] coumarin-Suberoylanilide hydroxamic acid (c-SAHA) is a SAHA derivative where the anilino cap group is replaced by 7-amino-4-methylcoumarin to produce a fluorescent probe that competitively binds HDAC. [2] The fluorescence excitation and emission maxima of free c-SAHA is 325 and 400 nm

Acetohydroxamic acid (N-Hydroxyacetamide) 是一种不可逆的细菌和植物尿素酶抑制剂，可研究慢性尿路感染。

Suberoyl bis-hydroxamic acid (SBHA) 是一种竞争性且可透过细胞的HDAC1和HDAC3抑制剂，ID50值分别为 0.25 μM 和 0.30 μM。它使肿瘤细胞易于凋亡并促进线粒体凋亡途径，可研究甲状腺髓样癌。

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。

4-(tert-Butyl)-benzhydroxamic Acid is a PqsR antagonist with IC50s of 12.5 μM and 23.6 μM for E. coli and P. aeruginosa, respectively, and it reduces the production of the virulence factor pyocyanin in P. aeruginosa with an IC50 of 87.2 μM[1].

Butyrylhydroxamic acid (N-Hydroxybutanamide) 是一类高效的组蛋白去乙酰化酶 (HDAC) 抑制剂。它在啮齿动物行为模型中表现出增强记忆的作用，适用于记忆增强剂、情绪稳定剂以及 β-链血红蛋白疾病的研究。

n-Decanohydroxamic acid is a biochemical.

Phosphoglycolohydroxamic acid 是有效抑制醛缩酶(aldolase)和磷酸丙糖异构酶(triose-phosphate isomerase)的化合物，同时在抗菌和抗真菌领域的研究中具有应用潜力。

Salicylhydroxamic acid (2-Hydroxybenzohydroxamic acid; N,2-Dihydroxybenzamide) 是用于生命科学研究的生化试剂，亦可作为相关的生物材料或有机化合物。

Idrapril 是一种血管紧张素转换酶(ACE)抑制剂，通过将具有重要催化作用的锌离子与羟基肟基团结合而起作用。

Piroctone olamine (Piroctone ethanolamine) 是一种吡啶衍生物，可用于治疗真菌感染。

Rac-Belinostat (PX-105684) 是一种具有抗肿瘤活性的新型异羟肟酸型组蛋白脱乙酰酶 (HDAC) 抑制剂。 Belinostat 靶向 HDAC 酶，从而抑制肿瘤细胞增殖、诱导细胞凋亡、促进细胞分化和抑制血管生成。这种药物可以使耐药肿瘤细胞对其他抗肿瘤药物敏感，可能是通过一种涉及胸苷酸合酶下调的机制。

Belinostat (PXD101) 是一种异羟肟酸型组蛋白脱乙酰酶抑制剂，具有抗肿瘤活性，在 HeLa 细胞提取物中的IC50为 27 nM。

Remetinostat (SHP-141) 是一种基于异羟肟酸的组蛋白脱乙酰酶抑制剂，可用于治疗皮肤 T 细胞淋巴瘤的研究。

STAT3 HDAC-IN-2（化合物18）为STAT3与HDAC的双重抑制剂，通过促进细胞自噬及细胞凋亡发挥作用。该化合物是以天然产物异丙醇内酯 (IAL) 为基础制成的两亲性羟肟酸杂化物，并表现为纳米级抗癌剂。在水中，STAT3 HDAC-IN-2 能自组装成纳米颗粒，相较于游离态，其在肿瘤组织中的积累量和细胞摄取率更高，从而展现出更强大的抗癌效能。

HDAC8-IN-12（compound 5k）作为一个非羟肟酸类，选择性地抑制HDAC8（IC50：0.12 nM），同时对乳腺癌具有显著的抑制效果。该化合物通过促进T细胞激活而引发抗肿瘤免疫反应，可以提高M1型巨噬细胞的数量，减少M2型巨噬细胞的数量。在乳腺癌原位小鼠模型中，HDAC8-IN-12（50 mg kg）展现出优异的抑制肿瘤生长的能力。

N(alpha)-Acetylfusarinines is a group of naturally occurring hydroxamic acids produced by unidentified species of Penicillium when grown on iron-deficient media.

Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access. SAHA-BPyne is a SAHA derivative with a benzophenone crosslinker and an alkyne tag intended to be used for profiling HDAC activities in proteomes and live cells. Such terminal alkyne groups can be used in linking reactions, known as click chemistry, characterized by high dependability and specificity of azide-alkyne bioconjugation reactions. SAHA-BPyne labels HDAC complex proteins both in proteomes at 100 nM and in live cells at 500 nM and demonstrates an IC50 value of ~3 μM for inhibition of HDAC activity in HeLa cell nuclear lysates in an HDAC activity assay.

L-Pyrohomoglutamic acid is an amino acid building block.1,2It has been used in the synthesis of ligands for FK506-binding proteins (FKBPs) and histone deacetylase (HDAC) inhibitors. 1.Pomplun, S., Wang, Y., Kirschner, A., et al.Rational design and asymmetric synthesis of potent and neurotrophic ligands for FK506-binding proteins (FKBPs)Angew. Chem. Int. Ed.54(1)345-348(2015) 2.Taddei, M., Cini, E., Giannotti, L., et al.Lactam based 7-amino suberoylamide hydroxamic acids as potent HDAC inhibitorsBioorg. Med. Chem. Lett.24(1)61-64(2014)

CAY17c is an inhibitor of bromodomain-containing protein 4 (BRD4; IC50= 0.71 μM), as well as class I histone deacetylases (HDACs; IC50s = 0.046, 0.058, 0.075, and 0.167 μM for HDAC1, -2, -3, and -8, respectively) and class IIb HDACs (IC50s = 0.073 and 0.923 μM for HDAC6 and HDAC10, respectively).1It is selective for these enzymes over BRD2, -3, and -T (IC50s = >20 μM for all), as well as over HDAC4, -5, -7, -9, and -11 (IC50s = >10 μM for all). CAY17c inhibits the proliferation of HCT116, SW620, and DLD-1 colorectal cancer cells (IC50s = 0.45, 1.78, and 2.11 μM, respectively), as well as induces apoptosis and autophagy in HCT116 cells. It reduces tumor growth in an HCT116 mouse xenograft model when administered at doses of 15 and 30 mg/kg. 1.Pan, Z., Li, X., Wang, Y., et al.Discovery of thieno[2,3-d]pyrimidine-based hydroxamic acid derivatives as bromodomain-containing protein 4/histone deacetylase dual inhibitors induce autophagic cell death in colorectal carcinoma cellsJ. Med. Chem.63(7)3678-3700(2020)

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.

Microtubule destabilizing agent-1 (Compound 12b)为基于异羟肟酸的微管去稳定剂(MDA)。该化合物表现出良好的代谢稳定性、高生物利用度及有效的抗肿瘤活性。