Pyridostatin
Based on 34 publication(s) in Google Scholar
Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM) and can target DNA and RNA G4s in cells. Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
For research use only. We do not sell to patients.
- Purity: 96.03%
- CAS No.: 1085412-37-8
- Formula: C31H32N8O5
- Molecular Weight:596.64
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Pyridostatin
More- J Hepatol. 2020 Aug;73(2):371-382. [Abstract]
- Cancer Res. 2025 Oct 1. [Abstract]
- Nat Commun. 2026 Feb 23;17(1):3076. [Abstract]
- Nat Commun. 2022 Sep 16;13(1):5456. [Abstract]
- Nat Commun. 2022 Mar 17;13(1):1444. [Abstract]
- J Am Chem Soc. 2021 Dec 15;143(49):20779-20791. [Abstract]
- Redox Biol. 2024 Sep:75:103247. [Abstract]
- Mol Cell. 2024 Jun 6;84(11):2070-2086.e20. [Abstract]
- Nat Chem Biol. 2025 Aug 7. [Abstract]
- Nucleic Acids Res. 2024 Mar 21;52(5):2142-2156. [Abstract]
- Nucleic Acids Res. 2023 Oct 27;51(19):10752-10767. [Abstract]
- Nucleic Acids Res. 2022 Jun 24;50(12):6953-6967. [Abstract]
- Nucleic Acids Res. 2019 Aug 22;47(14):7306-7320. [Abstract]
- Int J Biol Macromol. 2025 Jun 20;319(Pt 1):145405. [Abstract]
- Int J Biol Macromol. 2025 Jan 31:140556. [Abstract]
- Int J Biol Macromol. 2021 Nov 1:190:178-188. [Abstract]
- J Natl Cancer Inst. 2023 Nov 8;115(11):1383-1391. [Abstract]
- J Med Chem. 2026 Feb 12;69(3):2685-2702. [Abstract]
- Anal Chem. 2025 Jun 10;97(22):11617-11626. [Abstract]
- Emerg Microbes Infect. 2025 Jan 2:2447620. [Abstract]
- J Ethnopharmacol. 2024 Apr 6:323:117694. [Abstract]
- Eur J Med Chem Rep. 2025 Dec.
- ACS Omega. 2023 Sep 25;8(40):37369-37373. [Abstract]
- J Mol Med (Berl). 2019 Aug;97(8):1183-1193. [Abstract]
- PLoS Pathog. 2023 Jan 26;19(1):e1011131. [Abstract]
- iScience. 2022 Oct 9;25(11):105312. [Abstract]
- J Med Virol. 2023 Jan;95(1):e28299. [Abstract]
- Med Chem Res. 2024 Nov 14.
- Biochemistry. 2024 Oct 15;63(20):2609-2620. [Abstract]
- Biochem Biophys Res Commun. 2025 Dec 9:795:153117. [Abstract]
- Biol Pharm Bull. 2019 May 1;42(5):721-727. [Abstract]
- Biochem Mol Biol Educ. 2020 Jul;48(4):329-336. [Abstract]
- bioRxiv. 2026 Mar 30.
- bioRxiv. 2025 March 14.
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Cell Proliferation/Viability Assay
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RT-PCR
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RT-PCR
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WB
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Histological Imaging/Staining
Biological Activity
Kd: 490 nM (G-quadruplexe)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | IC50 |
5.38 μM
Compound: Pyridostatin
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Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay
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[PMID: 29323491] |
| MRC5 | IC50 |
5.4 μM
Compound: PDS
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Cytotoxicity against human MRC5 cells
Cytotoxicity against human MRC5 cells
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[PMID: 38971047] |
Pyridostatin (RR82) (10 μM; 48 hours) induces cell cycle arrest[1].
Pyridostatin is a very selective G-quadruplex DNA-binding small molecule designed to form a complex with and stabilize G-quadruplex structure. Pyridostatin causes neurite retraction, synaptic loss, and dose-dependent neuronal death. In cultured primary neurons, Pyridostatin induces the formation of DNA DSBs. Remarkably, Pyridostatin (1-5 μM, overnight) downregulates the BRCA1 protein, a protein that guards and repairs the neuronal genome, at the transcriptional level[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Over 60 different cancer cell lines
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Concentration:10 μM
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Incubation Time:48 hours
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Result:Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
Chemical Information
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CAS No. 1085412-37-8
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Appearance Solid
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Molecular Weight 596.64
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Formula C31H32N8O5
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Color White to off-white
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SMILES
O=C(C1=CC(OCCN)=CC(C(NC2=NC3=C(C(OCCN)=C2)C=CC=C3)=O)=N1)NC4=CC(OCCN)=C5C=CC=CC5=N4
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Synonyms
RR82
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (34)
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Journal Impact Factor
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Most Recent
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J Hepatol
2020 Aug;73(2):371-382. PMID: 32165252
Pyridostatin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2020 Aug;73(2):371-382. [Abstract]
Levels of miR-26a in MPHs transfected with miR-26a-WT or miR-26a-G4mut plasmids and stimulated with Pyridostatin hydrochloride (PDS, 10 μM; 48 h). The results showed that PDS significantly diminished the increase in miR-26a expression induced by miR-26a-WT plasmids, but not by miR-26a-G4mut plasmids, indicating that the G/A mutations are sufficient to abolish the inhibitory effect of PDS on miR-26a expression.
Pyridostatin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2020 Aug;73(2):371-382. [Abstract]
Pyridostatin hydrochloride (PDS, 10 μM; 48 h) markedly inhibited insulin-induced AKT activation, a central hallmark of insulin sensitivity, in MPHs (isolated from C57BL/6 mice) transfected with miR-26a-WT plasmids.
Pyridostatin purchased from MedChemExpress. Usage Cited in: J Hepatol. 2020 Aug;73(2):371-382. [Abstract]
8- to 10-week-old mice were infused with Pyridostatin hydrochloride (PDS, 6 mg/kg body weight) or saline (NC) via caudal vein twice a day (n = 5). 12 h post the second injection, the following measurements were performed. Representative H&E staining of paraffin liver sections. Scale bars: 20 μm. The results showed that no significant differences in histology and morphology were observed between PDS-treated mice and saline-treated mice.
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Cancer Res
Targeting SUV4-20H Epigenetic Enzymes Enhances Topoisomerase II Poisoning in Prostate Cancer. [Abstract]2025 Oct 1. PMID: 41032740 -
Nat Commun
2026 Feb 23;17(1):3076. PMID: 41730904 -
Nat Commun
WRN promotes bone development and growth by unwinding SHOX-G-quadruplexes via its helicase activity in Werner Syndrome. [Abstract]2022 Sep 16;13(1):5456. PMID: 36114168
Pyridostatin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 16;13(1):5456. [Abstract]
Stacked bar graphs of zebrafish embryos in dead, deformd, and normal status with different G4 stabilizer (Pyridostatin hydrochloride, 0.05-20 ng/μL, 5 nL) concentration at 24 hpf (d) and 48 hpf (e).
Pyridostatin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2022 Sep 16;13(1):5456. [Abstract]
qRT-PCR measurement of shox. The mRNA expression level of the shoxgene was detected at different time points (3, 7, and 14 days post-fertilization; i.e., 3 dpf, 7 dpf, and 14 dpf). The results showed that, compared with wild-type zebrafish, the G4 stabilizer Pyridostatin hydrochloride (0.05-0.1 ng/μL) significantly reduced the shox mRNA expression level in wrn−/− zebrafish.
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Nat Commun
2022 Mar 17;13(1):1444. PMID: 35301316 -
J Am Chem Soc
Monitoring and Modulating mtDNA G-Quadruplex Dynamics Reveal Its Close Relationship to Cell Glycolysis. [Abstract]2021 Dec 15;143(49):20779-20791. PMID: 34865478 -
Redox Biol
2024 Sep:75:103247. PMID: 39047636 -
Mol Cell
The MYCN oncoprotein is an RNA-binding accessory factor of the nuclear exosome targeting complex. [Abstract]2024 Jun 6;84(11):2070-2086.e20. PMID: 38703770 -
Nat Chem Biol
2025 Aug 7. PMID: 40775047 -
Nucleic Acids Res
2024 Mar 21;52(5):2142-2156. PMID: 38340342 -
Nucleic Acids Res
Unfolding of an RNA G-quadruplex motif in the negative strand genome of porcine reproductive and respiratory syndrome virus by host and viral helicases to promote viral replication. [Abstract]2023 Oct 27;51(19):10752-10767. PMID: 37739415 -
Nucleic Acids Res
DNA G-quadruplex structure participates in regulation of lipid metabolism through acyl-CoA binding protein. [Abstract]2022 Jun 24;50(12):6953-6967. PMID: 35748856 -
Nucleic Acids Res
Identification of LARK as a novel and conserved G-quadruplex binding protein in invertebrates and vertebrates. [Abstract]2019 Aug 22;47(14):7306-7320. PMID: 31165881 -
Int J Biol Macromol
An RNA G-quadruplex within the sclerostin 3' untranslated region enhances sclerostin expression by blocking miR-4648 binding. [Abstract]2025 Jun 20;319(Pt 1):145405. PMID: 40545075 -
Int J Biol Macromol
Diphenylaminothiophen-derived fluorescent ligands targeting mitochondrial DNA G-quadruplexes potentially for triple-negative breast cancer therapy. [Abstract]2025 Jan 31:140556. PMID: 39894118 -
Int J Biol Macromol
2021 Nov 1:190:178-188. PMID: 34461156 -
J Natl Cancer Inst
Suppressing c-FOS expression by G-quadruplex ligands inhibits osimertinib-resistant non-small cell lung cancers. [Abstract]2023 Nov 8;115(11):1383-1391. PMID: 37481710 -
J Med Chem
Novel Tetrahydroxanthylium-Based Ligands Targeting Mitochondrial DNA G-Quadruplex Structures for Concurrent Induction of Apoptosis and Inhibition of Autophagy in Liver Cancer. [Abstract]2026 Feb 12;69(3):2685-2702. PMID: 41582454 -
Anal Chem
2025 Jun 10;97(22):11617-11626. PMID: 40408126 -
Emerg Microbes Infect
SARS-CoV-2 and HCoV-OC43 regulate host m6A modification via activation of the mTORC1 signaling pathway to facilitate viral replication. [Abstract]2025 Jan 2:2447620. PMID: 39745173 -
J Ethnopharmacol
The function of Bazhen decoction in rescuing progeroid cell senescence via facilitating G-quadruplex resolving and telomere elongation. [Abstract]2024 Apr 6:323:117694. PMID: 38163559 -
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ACS Omega
Ratio of the Primers Used in Polymerase Chain Reaction-Stop Analysis Impacts the Resultant Banding Pattern. [Abstract]2023 Sep 25;8(40):37369-37373. PMID: 37841166 -
J Mol Med (Berl)
2019 Aug;97(8):1183-1193. PMID: 31201471 -
PLoS Pathog
2023 Jan 26;19(1):e1011131. PMID: 36701392 -
iScience
Genomic G-quadruplex folding triggers a cytokine-mediated inflammatory feedback loop to aggravate inflammatory diseases. [Abstract]2022 Oct 9;25(11):105312. PMID: 36304116 -
J Med Virol
2023 Jan;95(1):e28299. PMID: 36366981 -
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Biochemistry
G-Quadruplex-Mediated Transcriptional Regulation of SYT7: Implications for Tumor Progression and Therapeutic Strategies. [Abstract]2024 Oct 15;63(20):2609-2620. PMID: 39320967 -
Biochem Biophys Res Commun
2025 Dec 9:795:153117. PMID: 41380445 -
Biol Pharm Bull
Astragaloside IV Regulates the PI3K/Akt/HO-1 Signaling Pathway and Inhibits H9c2 Cardiomyocyte Injury Induced by Hypoxia-Reoxygenation. [Abstract]2019 May 1;42(5):721-727. PMID: 30867343 -
Biochem Mol Biol Educ
Forster resonance energy transfer for studying nucleic acids denaturation: A chemical and biological sciences laboratory experiment. [Abstract]2020 Jul;48(4):329-336. PMID: 32268010 -
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Solvent & Solubility
DMSO : ≥ 100 mg/mL (167.61 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Rodriguez R, et al. Small-molecule-induced DNA damage identifies alternative DNA structures in human genes. Nat Chem Biol. 2012;8(3):301-310. Published 2012 Feb 5. [Content Brief]
[2]. Koirala D, et al. A single-molecule platform for investigation of interactions between G-quadruplexes and small-molecule ligands. Nat Chem. 2011;3(10):782-787. Published 2011 Aug 28. [Content Brief]
[3]. Moruno-Manchon JF, Koellhoffer EC, Gopakumar J, et al. The G-quadruplex DNA stabilizing drug pyridostatin promotes DNA damage and downregulates transcription of Brca1 in neurons. Aging (Albany NY). 2017;9(9):1957-1970. [Content Brief]
[4]. Zhang X, et al. Chemical profiling of DNA G-quadruplex-interacting proteins in live cells. Nat Chem. 2021 Jul;13(7):626-633. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6761 mL | 8.3803 mL | 16.7605 mL | 41.9013 mL |
| 5 mM | 0.3352 mL | 1.6761 mL | 3.3521 mL | 8.3803 mL | |
| 10 mM | 0.1676 mL | 0.8380 mL | 1.6761 mL | 4.1901 mL | |
| 15 mM | 0.1117 mL | 0.5587 mL | 1.1174 mL | 2.7934 mL | |
| 20 mM | 0.0838 mL | 0.4190 mL | 0.8380 mL | 2.0951 mL | |
| 25 mM | 0.0670 mL | 0.3352 mL | 0.6704 mL | 1.6761 mL | |
| 30 mM | 0.0559 mL | 0.2793 mL | 0.5587 mL | 1.3967 mL | |
| 40 mM | 0.0419 mL | 0.2095 mL | 0.4190 mL | 1.0475 mL | |
| 50 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8380 mL | |
| 60 mM | 0.0279 mL | 0.1397 mL | 0.2793 mL | 0.6984 mL | |
| 80 mM | 0.0210 mL | 0.1048 mL | 0.2095 mL | 0.5238 mL | |
| 100 mM | 0.0168 mL | 0.0838 mL | 0.1676 mL | 0.4190 mL |