Pyridostatin |
| Katalog-Nr.GC15162 |
Pyridostatin ist eine hochselektive kleine Molekülverbindung, die speziell zur Bindung an G-Quadruplex-Strukturen entwickelt wurde und unabhängig von der Sequenzvariabilität polymorphe G-Quadruplex-Strukturen anspricht.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1085412-37-8
Sample solution is provided at 25 µL, 10mM.
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Pyridostatin 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]: | |
|
Cell lines |
MRC-5 SV40 cells |
|
Preparation Method |
Cells were treated with 2 µM Pyridostatin for 24 h. |
|
Reaction Conditions |
2 µM Pyridostatin;24 h |
|
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. | 1085412-37-8 | SDF | |
| Chemical Name | 4-(2-aminoethoxy)-2-N,6-N-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide | ||
| Canonical SMILES | C1=CC=C2C(=C1)C(=CC(=N2)NC(=O)C3=CC(=CC(=N3)C(=O)NC4=NC5=CC=CC=C5C(=C4)OCCN)OCCN)OCCN | ||
| Formula | C31H32N8O5 | M.Wt | 596.64 |
| Löslichkeit | ≥ 20.85 mg/mL in DMSO, ≥ 30.87 mg/mL in EtOH with gentle warming, ≥ 9.66 mg/mL in Water with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6761 mL | 8.3803 mL | 16.7605 mL |
| 5 mM | 335.2 μL | 1.6761 mL | 3.3521 mL |
| 10 mM | 167.6 μL | 838 μL | 1.6761 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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