NCH 51
(Synonyms: NCH-51) 目录号 : GC15536
An HDAC inhibitor
Cas No.:848354-66-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
NCH 51 is a potent and novel inhibitor of histone deacetylase [1].
Histone deacetylases (HADC) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription.
NCH-51 inhibited cells growth with EC50 values of 2.1 and 4.4 μM in NCI-H460 cells and MDA-MB-231 cells, respectively. Also, it inhibited proliferation of various cancer cell lines with EC50 values of 1.1 - 9.5 μM [1][2]. In HCT 116 cells, NCH-51 increased levels of acetylated histone H4 and p21WAF1/CIP1 in dose-dependent way [2]. In a series of lymphoid malignant cell lines, NCH-51 induced apoptosis. In U266 cells, NCH-51 activated caspase-3, -8 and -9. Also, NCH-51 increased expression of p21 and reduced expression of anti-apoptotic molecules, such as survivin, bcl-w and c-FLIP. At the protein level, NCH-51 increased the levels of peroxiredoxin 1 and 2, glutathione S-transferase and reactive oxygen species (ROS) [3]. In HIV-1 latently infected-cells, NCH 51 increased histone hyperacetylation, reduced HDAC1 occupancy and recruited positive transcription factors at the HIV-1 promoter, which increased the expression of HIV-1 [4].
References:
[1]. Suzuki T, Hisakawa S, Itoh Y, et al. Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor. Bioorg Med Chem Lett, 2007, 17(6): 1558-1561.
[2]. Suzuki T, Nagano Y, Kouketsu A, et al. Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates. J Med Chem, 2005, 48(4): 1019-1032.
[3]. Sanda T, Okamoto T, Uchida Y, et al. Proteome analyses of the growth inhibitory effects of NCH-51, a novel histone deacetylase inhibitor, on lymphoid malignant cells. Leukemia, 2007, 21(11): 2344-2353.
[4]. Victoriano AF, Imai K, Togami H, et al. Novel histone deacetylase inhibitor NCH-51 activates latent HIV-1 gene expression. FEBS Lett, 2011, 585(7): 1103-1111.
| Cas No. | 848354-66-5 | SDF | |
| 别名 | NCH-51 | ||
| 化学名 | S-[7-oxo-7-[(4-phenyl-1,3-thiazol-2-yl)amino]heptyl] 2-methylpropanethioate | ||
| Canonical SMILES | CC(C)C(=O)SCCCCCCC(=O)NC1=NC(=CS1)C2=CC=CC=C2 | ||
| 分子式 | C20H26N2O2S2 | 分子量 | 390.56 |
| 溶解度 | ≥ 14.55mg/mL in DMSO, ≥ 13.47 mg/mL in EtOH with ultrasonic | 储存条件 | Store at 4°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 | 2.5604 mL | 12.8021 mL | 25.6043 mL |
| 5 mM | 0.5121 mL | 2.5604 mL | 5.1209 mL |
| 10 mM | 0.256 mL | 1.2802 mL | 2.5604 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。