Nexturastat A
目录号 : GC13764
A potent, cell-permeable HDAC6 inhibitor
Cas No.:1403783-31-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Kinase experiment [1]: | |
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HDAC inhibition assays |
HDAC inhibition assays were performed by Reaction Biology Corp. using isolated human, recombinant full-length HDAC1 and -6 from a baculovirus expression system in Sf9 cells. An acetylated fluorogenic peptide, RHKKAc, derived from residues 379 ~ 382 of p53 was used as substrate. The reaction buffer was made up of 50 mM Tris-HCl pH 8.0, 127 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA, and a final concentration of 1% DMSO. Compounds were delivered in DMSO and delivered to enzyme mixture with preincubation of 5 ~ 10 mins followed by substrate addition and incubation for 2 hrs at 30 °C. Trichostatin A and developer were added to quench the reaction and generate fluorescence, respectively. Dose-response curves were generated starting at 30 μM compound with three-fold serial dilutions to generate a 10-dose plot. IC50 values were then generated from the resulting plots, and the values expressed were the average of duplicate trials ± standard deviation. |
| Cell experiment [1]: | |
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Cell lines |
B16 murine melanoma 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 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
100 μM; 48 hrs |
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Applications |
In B16 murine melanoma cells, Nexturastat A dose-dependently elevated acetyl α-tubulin levels without increasing histone H3 acetylation. Moreover, Nexturastat A potently inhibited the growth of B16 melanoma cells, with the GI50 value of 14.3 μM. |
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References: [1]. Bergman JA, Woan K, Perez-Villarroel P, Villagra A, Sotomayor EM, Kozikowski AP. Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9. | |
Nexturastat A is a selective inhibitor of histone deacetylase 6 (HDAC6) with IC50 value of 5.2 nM [1].
Nexturastat A is a HDAC inhibitor. It was developed by structural modification of aryl urea HDACIs. The inhibitory activity of Nexturastat A is most potent against HDAC6 with IC50 value of 5.2 nM. Besides that, Nexturastat A also shows inhibition of other HDACs with IC50 values of 3.02, 6.92, 6.68, 9.39, 11.7, 4.46, 0.954, 6.72, 7.57 and 5.14 μM for HDAC1, 2, 3, 4, 5, 7, 8, 9, 10 and 11, respectively. Nexturastat A has been shown to suppress cell proliferation and promote apoptosis in B16 murine melanoma cells [1, 2].
References:
[1] Kalin J H, Bergman J A. Development and therapeutic implications of selective histone deacetylase 6 inhibitors. Journal of medicinal chemistry, 2013, 56(16): 6297-6313.
[2] Zhang L, Han Y, Jiang Q, et al. Trend of Histone Deacetylase Inhibitors in Cancer Therapy: Isoform Selectivity or Multitargeted Strategy. Medicinal research reviews, 2014.
| Cas No. | 1403783-31-2 | SDF | |
| Canonical SMILES | CCCCN(CC1=CC=C(C=C1)C(=O)NO)C(=O)NC2=CC=CC=C2 | ||
| 分子式 | C19 H23 N3 O3 | 分子量 | 341.4 |
| 溶解度 | ≥ 16.3mg/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 | 2.9291 mL | 14.6456 mL | 29.2912 mL |
| 5 mM | 0.5858 mL | 2.9291 mL | 5.8582 mL |
| 10 mM | 0.2929 mL | 1.4646 mL | 2.9291 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。