Pyridostatin trihydrochloride (Synonyms: RR82 trihydrochloride)

Name: Pyridostatin trihydrochloride
Brand: MedChemExpress
SKU: HY-15176C
Rating: 5.0 (34 reviews)

Cat. No.: HY-15176C Purity: 99.85%: Data Sheet
COA

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Handling Instructions
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Pyridostatin (RR82) trihydrochloride is a G-quadruplex (G4) inducer/stabilizer with a K_d of 490 nM. Pyridostatin trihydrochloride also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC₅₀ of 11.0 μM. Pyridostatin trihydrochloride interacts with G-quadruplex structures, regulates the expression of SRC and SUB1, and induces replication- and transcription-dependent DNA damage, growth arrest, and genomic instability. Pyridostatin trihydrochloride exhibits antiproliferative and antiviral activities. Pyridostatin trihydrochloride can be used in studies related to breast cancer, cervical cancer, and Zika virus infection.

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

CAS No. : 2517456-88-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Based on 34 publication(s) in Google Scholar

Other Forms of Pyridostatin trihydrochloride:

34 Publications Citing Use of MCE Pyridostatin trihydrochloride

Cell Proliferation/Viability Assay

RT-PCR

Histological Imaging/Staining

: Pyridostatin trihydrochloride 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 trihydrochloride 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 trihydrochloride 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 trihydrochloride 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 trihydrochloride 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
Customer Review

Description

In Vitro

Pyridostatin (2 μM; 72 h) trihydrochloride potently inhibits the proliferation of SV40-transformed human MRC5 fibroblasts^[1].
Pyridostatin (2 μM; 1-10 days) trihydrochloride induces G2-phase cell cycle arrest and activates the DNA damage response in SV40-transformed human MRC5 fibroblasts and various human cancer cell lines. Long-term treatment causes G1-phase arrest in some cells, and checkpoint inhibition reverses this cell cycle arrest^[1].
Pyridostatin (2 μM) trihydrochloride induces DNA double-strand breaks (DSBs) in SV40-transformed human MRC5 fibroblasts. DNA-PKcs mediates sustained DSB repair during treatment, and DNA-PKcs-deficient MO59J cells are more sensitive to Pyridostatin than MO59K cells with normal DNA-PKcs expression^[1].
Pyridostatin (2 μM) trihydrochloride induces transcription-dependent DNA damage in SV40-transformed human MRC5 fibroblasts at the G1 and G2 phases, while it induces both transcription-dependent and replication-dependent DNA damage in S-phase cells^[1].
At low concentrations, Pyridostatin (2 μM; 24 h) trihydrochloride primarily targets non-telomeric DNA sites in SV40-transformed human MRC5 fibroblasts, whereas telomeric targeting occurs at higher doses, and inhibition of DNA-PKcs enhances Pyridostatin-induced mitotic chromosomal DNA damage^[1].
Pyridostatin (2 μM; 8-24 h) trihydrochloride induces DNA damage (γH2AX enrichment) in gene ontologies containing clusters of G-quadruplex-forming sequences, including the human proto-oncogene SRC, and downregulates the mRNA levels of these damaged genes in SV40-transformed human MRC5 fibroblasts^[1].
Pyridostatin (2 μM; 24 h) trihydrochloride reduces SRC protein levels by approximately 60% in SV40-transformed human MRC5 fibroblasts^[1].
Pyridostatin (2 μM; 24 h, 48 h) trihydrochloride reduces SRC-dependent cell motility in MDA-MB-231 human breast cancer cells, and its mechanism of action may involve downregulating SRC mRNA and protein levels rather than inducing widespread DNA damage^[1].
Pyridostatin (10 μM; 24 h) trihydrochloride alters the proteome of human HeLa cervical cancer cells, significantly downregulating 22 proteins including SUB1 (4.76-fold) while upregulating 16 proteins, and most of the affected genes contain potential G-quadruplex sequences^[2].
Pyridostatin (10 μM; 24 h) trihydrochloride regulates gene transcription in human HeLa cervical cancer cells in a sequence-dependent manner, significantly downregulating THRAP3, ARL6IP4 and GPC1, but exerts no such effect on SUB1 or COL5A1^[2].
Pyridostatin (2-10 μM; 24 h) trihydrochloride downregulates the expression of PC4 protein in human HeLa cervical cancer cells in a concentration-dependent manner, and treatment with 10 μM for 24 h almost completely abolishes the expression level of PC4^[2].
Pyridostatin (10 μM; 24 h) trihydrochloride increases the accumulation of trans-PtTz in human HeLa cervical cancer cells, as detected by ToF-SIMS imaging^[2].
Pyridostatin (10 μM; 24 h) trihydrochloride increases the platinum modification level of genomic DNA in human HeLa cervical cancer cells by 4-fold compared with treatment with trans-PtTz alone^[2].
Pyridostatin (2 μM; overnight) trihydrochloride alters the transcriptional processes of primary mouse cortical neurons cultured in vitro for 14 days, differentially regulates 901 genes, and enriches pathways including nervous system development, immune response and p53 signaling pathway, among which the Pirh2 gene is significantly up-regulated^[3].
Pyridostatin (2 μM; overnight) trihydrochloride induces distinct transcriptional responses in primary cortical neurons cultured in vitro for 4 days and 14 days, significantly downregulating Atg7 and Brca1 in immature neurons, while upregulating Pirh2 in both immature and mature neurons^[3].
Pyridostatin (2 μM; overnight) trihydrochloride modulates the morphology of BFP-Pirh2-positive intranuclear foci in primary cortical neurons, enhancing the intensity and reducing the area of the foci^[3].
Pyridostatin (2 μM; overnight) trihydrochloride enhances the colocalization of nucleolar DDX21 and nucleolin in primary cortical neurons, which is associated with nucleolar condensation^[3].
Pyridostatin (1.25-20 μM) trihydrochloride binds with high affinity to G-quadruplexes in 3'-UTR, NS3, NS5A and NS5B RNAs of Zika virus (ZIKV), with the highest affinity for NS5A (K_A = 36.7 μM)^[4].
Pyridostatin (400 μM) trihydrochloride forms stable complexes with the 3'-UTR, NS3, NS5A and NS5B G-quadruplexes of Zika virus (ZIKV) RNA, among which the binding affinity with NS5A is the highest (K_A = 40.0 μM)^[4].
Pyridostatin (10 μM; 2 h) trihydrochloride binds to and stabilizes the ZIKV NS5A RNA G-quadruplex in the cytoplasm of Vero cells, increasing the detectable level of stable RNA G-quadruplex structures^[4].
Pyridostatin (10 μM; 4 days) trihydrochloride potently reduces the cytopathic effect induced by Zika virus (ZIKV) in Vero cells^[4].
Pyridostatin (0.625-25 μM; 3-4 days) trihydrochloride exhibits potent anti-Zika virus (ZIKV) activity in Vero cells, with an EC₅₀ of 4.2 μM, and shows low cytotoxicity, maintaining >85% cell viability even at concentrations as high as 25 μM^[4].
Pyridostatin (1.25-10 μM; 72 h) trihydrochloride inhibits ZIKV mRNA replication and the mRNA expression of E and NS1 proteins in Vero cells in a dose-dependent manner, and reduces viral mRNA levels by > 94% at a concentration of 10 μM^[4].
Pyridostatin (2.5-10 μM; 72 h) trihydrochloride inhibits the expression of ZIKV E and NS1 proteins in Vero cells in a dose-dependent manner, with a significant reduction in expression levels observed at concentrations of 5 μM and higher^[4].
Treatment with Pyridostatin (10 μM; 72 h) trihydrochloride reduces NS1 protein levels and the number of ZIKV-positive Vero cells^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

706.02

Formula

C₃₁H₃₅Cl₃N₈O₅

CAS No.

2517456-88-9

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.Cl.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (141.64 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.4164 mL	7.0820 mL	14.1639 mL
5 mM	0.2833 mL	1.4164 mL	2.8328 mL
10 mM	0.1416 mL	0.7082 mL	1.4164 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 (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.85%

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Data Sheet (281 KB) SDS (254 KB)

COA (252 KB) HNMR (149 KB) RP-HPLC (247 KB) LCMS (107 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	1.4164 mL	7.0820 mL	14.1639 mL	35.4098 mL
	5 mM	0.2833 mL	1.4164 mL	2.8328 mL	7.0820 mL
	10 mM	0.1416 mL	0.7082 mL	1.4164 mL	3.5410 mL
	15 mM	0.0944 mL	0.4721 mL	0.9443 mL	2.3607 mL
	20 mM	0.0708 mL	0.3541 mL	0.7082 mL	1.7705 mL
	25 mM	0.0567 mL	0.2833 mL	0.5666 mL	1.4164 mL
	30 mM	0.0472 mL	0.2361 mL	0.4721 mL	1.1803 mL
	40 mM	0.0354 mL	0.1770 mL	0.3541 mL	0.8852 mL
	50 mM	0.0283 mL	0.1416 mL	0.2833 mL	0.7082 mL
	60 mM	0.0236 mL	0.1180 mL	0.2361 mL	0.5902 mL
	80 mM	0.0177 mL	0.0885 mL	0.1770 mL	0.4426 mL
	100 mM	0.0142 mL	0.0708 mL	0.1416 mL	0.3541 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Pyridostatin trihydrochloride 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:

Pyridostatin trihydrochloride2517456-88-9RR82 trihydrochlorideG-quadruplexDNA/RNA SynthesisFlavivirusSrcVirus ProteasestructureDNAdamageneurodegenerationDSBcyclearrestSRCInhibitorinhibitorinhibit

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Pyridostatin trihydrochloride (Synonyms: RR82 trihydrochloride)

Customer Review

Other Forms of Pyridostatin trihydrochloride:

Pyridostatin trihydrochloride Related Antibodies

34 Publications Citing Use of MCE Pyridostatin trihydrochloride

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Biological Activity

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Customer Review

Pyridostatin trihydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Pyridostatin trihydrochloride Related Classifications

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