Droxinostat
(Synonyms: 4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺,NS 41080) 目录号 : GC13706
An inhibitor of HDAC3, HDAC6, and HDAC8
Cas No.:99873-43-5
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
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 value of 16.9 ± 5.0 μM, 2.47 ± 1.09 μM, and 1.46 ± 0.11 μM, respectively [1].
HDACs (histone deacetylases) are enzymes responsible of the deacetylation of lysine that residues of core histones and play a pivotal role in controlling chromatin remodeling and transcriptional activation. It is also reported that HDACs control the acetylation and activation status of multiple non-histone proteins, including the heat shock protein 90 (Hsp90) which is an essential molecular chaperone for fungal virulence and antifungal resistance. Multiple HDACs have been identified and HDAC1 to HDAC10 are shown to express in malignant cells which reminds the HDAC inhibitor as a target for cancer therapy [2] [3].
Droxinostat is a selective HDAC inhibitor and is different from the known pan-HDACi TSA which inhibits all tested HDAC. When tested with prostate cancer line PPC-1 cells, droxinostat treatment selectively inhibited HDAC3, HDAC6, and HDAC8 activity at the concentration of 50 μM/L which sensitized cells to death ligands [1]. In androgen-dependent CaP cells, administration of droxinostat selectively inhibited HDACs and downregulated c-FLP expression which resulted in cells apoptosis [4].
References:
[1]. Wood, T.E., et al., Selective inhibition of histone deacetylases sensitizes malignant cells to death receptor ligands. Mol Cancer Ther, 2010. 9(1): p. 246-56.
[2]. Lamoth, F., P.R. Juvvadi, and W.J. Steinbach, Histone deacetylase inhibition as an alternative strategy against invasive aspergillosis. Front Microbiol, 2015. 6: p. 96.
[3]. Mackmull, M.T., et al., Histone deacetylase inhibitors cause the selective depletion of bromodomain containing proteins. Mol Cell Proteomics, 2015.
[4]. McCourt, C., et al., Elevation of c-FLIP in castrate-resistant prostate cancer antagonizes therapeutic response to androgen receptor-targeted therapy. Clin Cancer Res, 2012. 18(14): p. 3822-33.
| Cas No. | 99873-43-5 | SDF | |
| 别名 | 4-(4-氯-2-甲基苯氧基)-N-羟基丁酰胺,NS 41080 | ||
| 化学名 | 4-(4-chloro-2-methylphenoxy)-N-hydroxybutanamide | ||
| Canonical SMILES | CC1=C(C=CC(=C1)Cl)OCCCC(=O)NO | ||
| 分子式 | C11H14ClNO3 | 分子量 | 243.69 |
| 溶解度 | ≥ 11.35 mg/mL in DMSO, ≥ 102.8 mg/mL in EtOH | 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 | 4.1036 mL | 20.5179 mL | 41.0357 mL |
| 5 mM | 0.8207 mL | 4.1036 mL | 8.2071 mL |
| 10 mM | 0.4104 mL | 2.0518 mL | 4.1036 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。