1. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK Anti-infection
  2. G-quadruplex DNA/RNA Synthesis Flavivirus Src Virus Protease
  3. Pyridostatin TFA

Pyridostatin TFA  (Synonyms: RR82 TFA)

Cat. No.: HY-15176B Purity: 99.17%
Handling Instructions Technical Support

Pyridostatin (RR82) TFA is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin TFA also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin TFA 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 TFA exhibits antiproliferative and antiviral activities. Pyridostatin TFA 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. : 1472611-44-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Customer Review

Based on 34 publication(s) in Google Scholar

Other Forms of Pyridostatin TFA:

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Pyridostatin TFA

Cell Proliferation/Viability Assay
RT-PCR
WB
Histological Imaging/Staining

    Pyridostatin TFA 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 TFA 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 TFA 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 TFA 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 TFA 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

    Pyridostatin (RR82) TFA is a G-quadruplex (G4) inducer/stabilizer with a Kd of 490 nM. Pyridostatin TFA also acts as an inhibitor of Zika virus (ZIKV) NS2B-NS3 protease, with an IC50 of 11.0 μM. Pyridostatin TFA 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 TFA exhibits antiproliferative and antiviral activities. Pyridostatin TFA can be used in studies related to breast cancer, cervical cancer, and Zika virus infection[1][2][3][4].

    In Vitro

    Pyridostatin (2 μM; 72 h) TFA potently inhibits the proliferation of SV40-transformed human MRC5 fibroblasts[1].
    Pyridostatin (2 μM; 1-10 days) TFA 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) TFA 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) TFA 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) TFA 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) TFA 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) TFA reduces SRC protein levels by approximately 60% in SV40-transformed human MRC5 fibroblasts[1].
    Pyridostatin (2 μM; 24 h, 48 h) TFA 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) TFA 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) TFA 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) TFA 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) TFA increases the accumulation of trans-PtTz in human HeLa cervical cancer cells, as detected by ToF-SIMS imaging[2].
    Pyridostatin (10 μM; 24 h) TFA 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) TFA 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) TFA 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) TFA 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) TFA enhances the colocalization of nucleolar DDX21 and nucleolin in primary cortical neurons, which is associated with nucleolar condensation[3].
    Pyridostatin (1.25-20 μM) TFA 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 (KA = 36.7 μM)[4].
    Pyridostatin (400 μM) TFA 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 (KA = 40.0 μM)[4].
    Pyridostatin (10 μM; 2 h) TFA 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) TFA potently reduces the cytopathic effect induced by Zika virus (ZIKV) in Vero cells[4].
    Pyridostatin (0.625-25 μM; 3-4 days) TFA 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) TFA 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) TFA 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) TFA 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.

    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

    710.66

    Formula

    C33H33F3N8O7

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1=NC(C(NC2=NC3=CC=CC=C3C(OCCN)=C2)=O)=CC(OCCN)=C1)NC4=NC5=CC=CC=C5C(OCCN)=C4.O=C(O)C(F)(F)F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    H2O : 100 mg/mL (140.71 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4071 mL 7.0357 mL 14.0714 mL
    5 mM 0.2814 mL 1.4071 mL 2.8143 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 (sealed storage, 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.

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O 1 mM 1.4071 mL 7.0357 mL 14.0714 mL 35.1786 mL
    5 mM 0.2814 mL 1.4071 mL 2.8143 mL 7.0357 mL
    10 mM 0.1407 mL 0.7036 mL 1.4071 mL 3.5179 mL
    15 mM 0.0938 mL 0.4690 mL 0.9381 mL 2.3452 mL
    20 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7589 mL
    25 mM 0.0563 mL 0.2814 mL 0.5629 mL 1.4071 mL
    30 mM 0.0469 mL 0.2345 mL 0.4690 mL 1.1726 mL
    40 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8795 mL
    50 mM 0.0281 mL 0.1407 mL 0.2814 mL 0.7036 mL
    60 mM 0.0235 mL 0.1173 mL 0.2345 mL 0.5863 mL
    80 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4397 mL
    100 mM 0.0141 mL 0.0704 mL 0.1407 mL 0.3518 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.

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      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.

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