Pyridostatin (trifluoroacetate salt)
(Synonyms: RR82 TFA) 目录号 : GC48016
Pyridostatin (trifluoroacetate salt)是一种高选择性的g -四重体结合小分子，设计用于靶向多态g -四重体结构，而不考虑序列可变性。
Cas No.:1472611-44-1
Sample solution is provided at 25 µL, 10mM.
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Pyridostatin (trifluoroacetate salt) is a highly selective G-quadruplex-binding small molecule that was designed to target polymorphic G-quadruplex structures regardless of sequence variability. As a highly selective G-quadruplex DNA stabilizer,Kd is 490 nM. Pyridostatin has anti-proliferative effects and induces telomere dysfunction[1-4].
Pyridostatin(2 µM pyridostatin;24 h) induced DNA damage and checkpoint-dependent cell-cycle arrest in MRC-5 SV40 cells[5]. Pyridostatin(0.01-5 µM pyridostatin;24-96 h) induced neurotoxicity and promoted the formation of DNA double-strand breaks (DSBs) in cultured neurons[6]. Pyridostatin(10 µM pyridostatin;24 h) significantly downregulated 22 proteins but upregulated 16 proteins in HeLa cancer cells, of which the genes both contain a number of G4 potential sequences, Pyridostatin regulation on gene expression is far more complicated than inducing/stabilizing G4 structures[7].
References:
[1]. Rodriguez R, MÜller S, et,al. A novel small molecule that alters shelterin integrity and triggers a DNA-damage response at telomeres. J Am Chem Soc. 2008 Nov 26;130(47):15758-9. doi: 10.1021/ja805615w. PMID: 18975896; PMCID: PMC2746963.
[2]. Patel DJ, Phan AT, et,al. Human telomere, oncogenic promoter and 5'-UTR G-quadruplexes: diverse higher order DNA and RNA targets for cancer therapeutics. Nucleic Acids Res. 2007;35(22):7429-55. doi: 10.1093/nar/gkm711. Epub 2007 Oct 2. PMID: 17913750; PMCID: PMC2190718.
[3]. MÜller S, Kumari S, et,al. Small-molecule-mediated G-quadruplex isolation from human cells. Nat Chem. 2010 Dec;2(12):1095-8. doi: 10.1038/nchem.842. Epub 2010 Oct 10. PMID: 21107376; PMCID: PMC3119466.
[4]. Koirala D, Dhakal S, et,al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011 Aug 28;3(10):782-7. doi: 10.1038/nchem.1126. PMID: 21941250; PMCID: PMC3277938.
[5]. Rodriguez R, Miller KM, et,al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10. doi: 10.1038/nchembio.780. PMID: 22306580; PMCID: PMC3433707.
[6]. Moruno-Manchon JF, et,al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017 Sep 12;9(9):1957-1970. doi: 10.18632/aging.101282. PMID: 28904242; PMCID: PMC5636668.
[7]. Hou Y, Gan T, et,al. G-quadruplex inducer/stabilizer pyridostatin targets SUB1 to promote cytotoxicity of a transplatinum complex. Nucleic Acids Res. 2022 Apr 8;50(6):3070-3082. doi: 10.1093/nar/gkac151. PMID: 35258624; PMCID: PMC8989551.
| Cell experiment [1]: | |
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Cell lines |
MRC-5 SV40 cells |
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Preparation Method |
Cells were treated with 2 µM Pyridostatin for 24 h. |
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Reaction Conditions |
2 µM Pyridostatin;24 h |
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Applications |
Pyridostatin induced DNA damage and checkpoint-dependent cell-cycle arrest. |
|
References: [1]. Rodriguez R, Miller KM, et,al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012 Feb 5;8(3):301-10. doi: 10.1038/nchembio.780. PMID: 22306580; PMCID: PMC3433707. |
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| Cas No. | 1472611-44-1 | SDF | |
| 别名 | RR82 TFA | ||
| Canonical SMILES | NCCOC1=CC(NC(C2=NC(C(NC3=CC(OCCN)=C(C=CC=C4)C4=N3)=O)=CC(OCCN)=C2)=O)=NC5=C1C=CC=C5.C#C(F)(F)F.O=O | ||
| 分子式 | C31H32N8O5.C2HF3O2 | 分子量 | 710.7 |
| 溶解度 | DMF: 30 mg/mL,DMSO: 20 mg/mL,Ethanol: 5 mg/ml,Water: 50 mg/mL | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.4071 mL | 7.0353 mL | 14.0706 mL |
| 5 mM | 0.2814 mL | 1.4071 mL | 2.8141 mL |
| 10 mM | 0.1407 mL | 0.7035 mL | 1.4071 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet