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
A potent, selective HDAC8 inhibitor
Cas No.:950762-95-5
Sample solution is provided at 25 µL, 10mM.
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PCI-34051 is a potent, specific inhibitor of histone deacetylase 8 (HDAC8) with greater than 200-fold selectivity over the other HDAC isoforms, such as 1, 2, 3, 6 and 10. It induces caspase dependent apoptosis in cell lines derived from T-cell lymphomas or leukemias, but not in other hematopoietic or solid tumor lines. PCI-34051 does not cause detectable histone or tubulin acetylation and also does not inhibit growth or induce apoptosis in normal cells such as PBMCs or fibroblasts. Although a phospholipase C-gamma1 (PLCgamma1) defective line is resistant, cells defective in T-cell receptor signaling are still sensitive to PCI-34051 induced apoptosis.
References:
[1]. S Balasubramanian, J Ramos, W Luo, M Sirisawad, E Verner, J J Buggy. A novel histone deacetylase 8 (HDAC8)-specific inhibitor PCI-34051 induces apoptosis in T-cell lymphomas. Leukemia (2008) 22, 1026–1034.
[2]. Sriram Balasubramanian, Erik Verner, Joseph J. Buggy. Isoform-specific histone deacetylase inhibitors: The next step? Cancer Letters. Volume 280, Issue 2, 8 August 2009, Pages 211–221.
| Kinase experiment [1]: | |
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Histone deacetylase activity |
For PCI-34051 characterization, measurements were perfomed in a reaction volume of 100 μL using 96-well assay plates in a fluorescence plate reader. For each isozyme, the HDAC protein in reaction buffer (50 mM HEPES, 100 mM KCl, 0.001% Tween-20, 5% dimethyl sulfoxide, pH 7.4, supplemented with bovine serum albumin at concentrations of 0 ~ 0.05%) was mixed with PCI-34051 at various concentrations and allowed to incubate for 15 mins. Trypsin was added to a final concentration of 50 nM, and acetyl-Gly-Ala-(N-acetyl-Lys)-amino-4-methylcoumarin was added to a final concentration of 25 ~ 100 μM to initiate the reaction. After a 30 min lag time, the fluorescence was measured over a 30 min time frame using an excitation wavelength of 335 nm and a detection wavelength of 460 nm. The increase in fluorescence with time was used as the measure of the reaction rate. |
| Cell experiment [1]: | |
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Cell lines |
T-cell derived lines (Jurkat, HuT78, HSB-2 and Molt-4 cells) |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
5 μM; 2 days |
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Applications |
The HDAC8-selective inhibitor PCI-34051 was cytotoxic to T-cell derived lines. |
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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 May;22(5):1026-34. | |
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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 | 0.6749 mL | 3.3747 mL | 6.7495 mL |
| 10 mM | 0.3375 mL | 1.6874 mL | 3.3747 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet