PCI-34051
(Synonyms: N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺,PCI34051, PCI 34051) 目录号 : GC18008
PCI-34051是一种高效且选择性的HDAC8抑制剂，其IC50为10nM。
Cas No.:950762-95-5
Sample solution is provided at 25 µL, 10mM.
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PCI-34051 is a potent and selective HDAC8 inhibitor with an IC50 of 10nM[1]. Histone deacetylase 8 (HDAC8) is a class I histone deacetylase that modulates chromatin structureplays by removing acetyl groups from histones and influences transcriptional activity[2]. PCI-34051 is usually used to study the mechanisms of tumor cell apoptosis and the regulation of related signaling pathways[3].
In vitro, treatment of wild-type p53 ovarian cancer cells with PCI-34051 (20µM; 24-72h) significantly suppresses cell proliferation, enhances cell apoptosis, and inhibits cell migration[4]. Treatment of human bronchial epithelial cells (HBECs) with PCI-34051 (10µM; 4 days) induced the release of exosomes containing miR-381-3p, inhibited cell proliferation, and triggered cell apoptosis[5].
In vivo, PCI-34051 (0.5mg/kg; intraperitoneal injection at days 0, 7, and 14) significantly reduced airway hyperresponsiveness, inflammation and airway remodeling in the ovalbumin-sensitized and challenged asthma mice model[6]. PCI-34051 (20mg/kg; intraperitoneal injection before cisplatin and daily thereafter) significantly reduced renal tubular damage, apoptosis, and DNA damage, and promoted homologous recombination repair in a mice model of cisplatin-induced acute kidney injury (AKI)[7].
References:
[1] Balasubramanian S, Ramos J, Luo W, Sirisawad M, Verner E, Buggy JJ. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia. 2008;22(5):1026-1034.
[2] Zhao Q, Liu H, Peng J, et al. HDAC8 as a target in drug discovery: Function, structure and design. Eur J Med Chem. 2024;280:116972.
[3] Amin SA, Adhikari N, Jha T. Structure-activity relationships of HDAC8 inhibitors: Non-hydroxamates as anticancer agents. Pharmacol Res. 2018;131:128-142.
[4] Kim JY, Han SY, Yoo J, et al. HDAC8-Selective Inhibition by PCI-34051 Enhances the Anticancer Effects of ACY-241 in Ovarian Cancer Cells. Int J Mol Sci. 2022;23(15):8645.
[5] Bai SY, Li ML, Ren Y, Su XM. HDAC8-inhibitor PCI-34051-induced exosomes inhibit human bronchial smooth muscle cell proliferation via miR-381-3p mediated TGFB3. Pulm Pharmacol Ther. 2021;71:102096.
[6] Bai S, Su X, Kong D, et al. Selective HDAC8 inhibition by PCI-34051 attenuates inflammation and airway remodeling in asthma via miR-381-3p-TGFβ3 axis. J Transl Int Med. 2025;12(6):592-601.
[7] Wang Y, Yu C, Yu J, et al. Inhibition of HDAC8 mitigates AKI by reducing DNA damage and promoting homologous recombination repair. J Cell Mol Med. 2024;28(18):e70114.
PCI-34051是一种高效且选择性的HDAC8抑制剂，其IC50为10nM[1]。组蛋白去乙酰化酶 8（HDAC8）是一种Ⅰ类组蛋白去乙酰化酶，通过去除组蛋白上的乙酰基团调节染色质结构，进而影响转录活性[2]。PCI-34051常用于研究肿瘤细胞凋亡及相关信号通路的调控机制[3]。
体外实验中，用PCI-34051（3µM；24小时）处理野生型p53卵巢癌细胞可显著抑制细胞增殖，增强细胞凋亡，并抑制细胞迁移[4]。 PCI-34051（10µM；4天）处理人支气管上皮细胞（HBECs）可诱导释放含有miR-381-3p的外泌体，抑制细胞增殖并触发细胞凋亡[5]。
体内实验中，在卵清蛋白致敏和刺激的哮喘小鼠模型中，PCI-34051（0.5mg/kg；腹腔注射于第0、7、14天）显著降低了气道高反应性、炎症和气道重塑[6]。在顺铂诱导的急性肾损伤（AKI）小鼠模型中，PCI-34051（20mg/kg；顺铂治疗前腹腔注射；此后每日注射）显著减轻了肾小管损伤、细胞凋亡和DNA损伤，并促进了同源重组修复[7]。
| Cell experiment [1]: | |
Cell lines | human ovarian cancer cell line, TOV-21G (p53-WT) and A2780 (p53-WT) |
Preparation Method | The human ovarian cancer cell line, TOV-21G (p53-WT) and A2780 (p53-WT) were cultured in Roswell Park Memorial Institute medium (RPMI) contained 10% fetal bovine serum, 100U/mL penicillin, and 100µg/mL streptomycin. Cell lines were maintained in 5% CO2 and 37℃ humidified incubators. Cells were subcultured every 3-4 days. Cells were seeded in 96-well plates containing 130µL medium (3×103 cells per well). Following overnight incubation, PCI-34051 was treated for 24h, 48h, and 72h. Cell growth and viability were determined by CCK-8 assay. Cell apoptosis was determined Annexin V-FITC Apoptosis Detection Kit. Cells were seeded in the upper chamber of the transwell insert plate (PET membrane, 8µM pore) in a 400µL serum-free medium (1×105 cells per well) and 500µL of medium containing 10% FBS was placed in the lower chamber for Transwell Migration Assay. |
Reaction Conditions | 20µM; 24-72h |
Applications | Treatment of wild-type p53 ovarian cancer cells with PCI-34051 significantly suppresses cell proliferation, enhances cell apoptosis, and inhibits cell migration. |
| Animal experiment [2]: | |
Animal models | SPF-grade female BABL/c mice |
Preparation Method | SPF-grade female BABL/c mice aged 6-8 weeks and weighing 20±2g were housed in an SPF-grade room for one week and provided water and food ad libitum. Mice were randomly divided into three groups (n=6 for each group): healthy control (con), mice with asthma (ova), and PCI-34051 treatment (pci). Mice of the ova and pci groups were sensitized by intraperitoneal injection of 0.2mL OVA solution (20μg OVA and 2mg aluminum hydroxide in 0.2mL normal saline) at days 0, 7, and 14 to create the asthma model. The OVA challenge was conducted on day 21 using a 2% OVA saline solution with a nebulizer for 30min daily, three times per week for eight weeks, while mice in the control group were administered saline. In the pci groups, PCI-34051 (0.5mg/kg) was administered intraperitoneally before each challenge, and the con and ova groups were administered saline as a control. Airway resistance was estimated using noninvasive wholebody plethysmography. Cytokine levels were measured by Luminex-based immunoassays. Anesthetized mice were sacrificed by cervical dislocation 1 hour after the last OVA challenge. The left lung was fixed with 0.1mL iced 4% polyoxymethylene, removed, and fixed in 4% polyoxymethylene for 24 hours. After rehydration by running tap water for 6 hours, dehydration and embedding in paraffin were performed, and 4μm sections were cut for further analysis. Proteins and RNA were extracted for further analyses. |
Dosage form | 0.5mg/kg; intraperitoneal injection at days 0, 7, and 14 |
Applications | PCI-34051 significantly reduced airway hyperresponsiveness, inflammation and airway remodeling in the ovalbumin-sensitized and challenged asthma mice model. |
References: | |
| Cas No. | 950762-95-5 | SDF | |
| 别名 | N-羟基-1-(4-甲氧基苄基)-1H-吲哚-6-甲酰胺,PCI34051, PCI 34051 | ||
| 化学名 | N-hydroxy-1-[(4-methoxyphenyl)methyl]indole-6-carboxamide | ||
| Canonical SMILES | COC1=CC=C(C=C1)CN2C=CC3=C2C=C(C=C3)C(=O)NO | ||
| 分子式 | C17H16N2O3 | 分子量 | 296.32 |
| 溶解度 | ≥ 14.8 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.3747 mL | 16.8737 mL | 33.7473 mL |
| 5 mM | 674.9 μL | 3.3747 mL | 6.7495 mL |
| 10 mM | 337.5 μL | 1.6874 mL | 3.3747 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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