Pyridostatin (Synonyms: RR82)

Cat. No.: HY-15176 Purity: 96.03%: Data Sheet
COA

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Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (K_d=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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form that retains the same biological activity.

For research use only. We do not sell to patients.

CAS No. : 1085412-37-8

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5 mg		Ask For Quote & Lead Time
10 mg		Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Pyridostatin:

Pyridostatin hydrochloride Pyridostatin TFA Pyridostatin trihydrochloride

Other Forms of Pyridostatin:

34 Publications Citing Use of MCE Pyridostatin

Cell Proliferation/Viability Assay

RT-PCR

Histological Imaging/Staining

: 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.

: 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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Biological Activity
Purity & Documentation
References
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Description

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]
MRC5	IC₅₀	5.4 μM Compound: PDS	Cytotoxicity against human MRC5 cells Cytotoxicity against human MRC5 cells	[PMID: 38971047]

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.

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.

1085412-37-8

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

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
10 mM	0.1676 mL	0.8380 mL	1.6761 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 96.03%

Select Batch:

Data Sheet (275 KB) SDS (396 KB)

COA (250 KB) HNMR (403 KB) RP-HPLC (246 KB) LCMS (89 KB)

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

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

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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