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Submit ReviewPyridostatin pentahydrochloride
Description: Stabilizes G-quadruplexes; induces DNA damage and cell cycle arrest
Chemical Name: 4-(2-Aminoethoxy)N2,N6-bis[(4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinecarboxamide pentahydrochloride
Purity: ≥95% (HPLC)
Biological Activity for Pyridostatin pentahydrochloride
Binds and stabilizes G-quadruplexes, inducing DNA damage and cell cycle arrest (Kd = 490 nM); targets the proto-oncogene Src, reducing Src protein abundance and Src-dependent motility in human breast cancer cells. Also targets telomeric G-quadruplexes, inducing telomerase dysfunction. Activates the DNA-dependent protein kinase catalytic sunbunit (DNA-PKcs).
Technical Data for Pyridostatin pentahydrochloride
| M. Wt | 778.94 |
| Formula | C31H32N8O5.5HCl |
| Storage | Desiccate at RT |
| Purity | ≥95% (HPLC) |
| CAS Number | 1781882-65-2 |
| PubChem ID | 78243739 |
| InChI Key | SRIZPFGTXSQRFM-UHFFFAOYSA-N |
| Smiles | NCCOC1=CC(C(NC2=NC(C=CC=C3)=C3C(OCCN)=C2)=O)=NC(C(NC4=CC(OCCN)=C(C=CC=C5)C5=N4)=O)=C1.Cl.Cl.Cl.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Pyridostatin pentahydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 15.58 | 20 |
Preparing Stock Solutions for Pyridostatin pentahydrochloride
The following data is based on the product molecular weight 778.94. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 6.42 mL | 32.09 mL | 64.19 mL |
| 1 mM | 1.28 mL | 6.42 mL | 12.84 mL |
| 2 mM | 0.64 mL | 3.21 mL | 6.42 mL |
| 10 mM | 0.13 mL | 0.64 mL | 1.28 mL |
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Product Datasheets for Pyridostatin pentahydrochloride
References for Pyridostatin pentahydrochloride
References are publications that support the biological activity of the product.
Rodriguez et al (20112) Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat.Chem.Biol. 8 301 PMID: 22306580
Müller et al (2010) Small-molecule-mediated G-quadruplex isolation from human cells. Nat.Chem. 2 1095 PMID: 21107376
Koirala et al (2011) A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat.Chem. 3 782 PMID: 21941250
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1 Citation for Pyridostatin pentahydrochloride
Citations are publications that use Tocris products. Selected citations for Pyridostatin pentahydrochloride include:
Sven et al (2021) Inosine Substitutions in RNA Activate Latent G-Quadruplexes. J Am Chem Soc 143 15120-15130 PMID: 34520206
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Literature in this Area
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Cell Cycle and DNA Damage Research Product Guide
This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:
- Cell Cycle and Mitosis
- DNA Damage Repair
- Targeted Protein Degradation
- Ubiquitin Proteasome Pathway
- Chemotherapy Targets
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.