2. Cell Cycle/DNA Damage
  3. G-quadruplex
  4. Pyridostatin

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.

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Pyridostatin Chemical Structure

Pyridostatin Chemical Structure

CAS No. : 1085412-37-8

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Based on 23 publication(s) in Google Scholar

Other Forms of Pyridostatin:

Pyridostatin Related Antibodies

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Description

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[1][2].

IC50 & Target

Kd: 490 nM (G-quadruplexe)[1]
Cellular Effect
Cell Line Type Value Description References
MRC5 IC50
5.38 μM
Compound: Pyridostatin
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
[PMID: 29323491]
In Vitro

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.

Pyridostatin Related Antibodies

Cell Viability Assay[1]

Cell Line: Over 60 different cancer cell lines
Concentration: 10 μM
Incubation Time: 48 hours
Result: Predominantly accumulated in the G2 phase of the cell cycle over 60 different cancer cell lines.
Molecular Weight

596.64

Formula

C31H32N8O5
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (167.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6761 mL 8.3803 mL 16.7605 mL
5 mM 0.3352 mL 1.6761 mL 3.3521 mL
View the 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.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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Pyridostatin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pyridostatin1085412-37-8RR82RR 82RR-82G-quadruplexstructureDNAdamageneurodegenerationDSBcyclearrestSRCInhibitorinhibitorinhibit

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