1. Apoptosis Stem Cell/Wnt JAK/STAT Signaling NF-κB Immunology/Inflammation
  2. Apoptosis STAT NF-κB NO Synthase COX TNF Receptor Interleukin Related
  3. GYY4137

GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity.

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

CAS No. : 106740-09-4

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of GYY4137:

Top Publications Citing Use of Products

    GYY4137 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jan 12;22(1):33.  [Abstract]

    The number of TUNEL-positive neurons was notably increased after SCIRI, which was significantly decreased by GYY4137 treatment (50 mg/kg; IP; 30 min before the onset of spinal cord reperfusion; Single dose).

    GYY4137 purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jan 12;22(1):33.  [Abstract]

    The Western blotting results demonstrated that expression of the p-MLKL, p-RIP1, and p-RIP3 in the SCIRI group were higher than those in the sham group, and the p-MLKL/MLKL, p-RIP1/RIP1, and p-RIP3/RIP3 ratios were increased. With GYY4137 treatment (50 mg/kg; IP; 30 min before the onset of spinal cord reperfusion; Single dose), these changes were largely reversed.

    GYY4137 purchased from MedChemExpress. Usage Cited in: Molecules. 2023 Jun 14;28(12):4770.

    Representative Western blots for Gpx4, FTH-1, and TF expression in MRGECs of the control, 100 µg/mL LPS-treated, and 100 µg/mL LPS + GYY4137 (0.2, 0.4, 0.8, or 1 mM; for 24 h) treatment groups. β-actin was used as the internal control.

    GYY4137 purchased from MedChemExpress. Usage Cited in: Molecules. 2023 Jun 14;28(12):4770.

    MRGECs were incubated in 100 µg/mL LPS and 0.8 mM GYY4137 for 24 h, and this was followed by detection of cell viability with the CCK-8 assay.

    GYY4137 purchased from MedChemExpress. Usage Cited in: Molecules. 2023 Jun 14;28(12):4770.

    Representative Western blots for Gpx4, FTH-1, and TF expression in the kidney tissues from mice subjected to CLP and treated with different concentrations of GYY4137 (5, 10, 25, or 50 mg/kg; IP; 30 min after CLP treatment; Single dose).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity[1][2][3][4][5][6].

    IC50 & Target[6]

    Stat-3

     

    Cellular Effect
    Cell Line Type Value Description References
    MCF7 IC50
    368.2 μM
    Compound: 1, GYY4137
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    [PMID: 26147240]
    MCF7 IC50
    > 500 μM
    Compound: 1, GYY4137
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    [PMID: 26147240]
    MDA-MB-231 IC50
    239.6 μM
    Compound: 1, GYY4137
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
    Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay
    [PMID: 26147240]
    PC-3 IC50
    > 200 μM
    Compound: 1, GYY4137
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    [PMID: 26147240]
    SK-OV-3 IC50
    332 μM
    Compound: 1, GYY4137
    Cytotoxicity against human SKOV3 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    Cytotoxicity against human SKOV3 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    [PMID: 26147240]
    WI-38 IC50
    1977 μM
    Compound: 1, GYY4137
    Toxicity in human WI38 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    Toxicity in human WI38 cells assessed as inhibition of cell proliferation after 4 days by crystal violet assay
    [PMID: 26147240]
    In Vitro

    GYY4137 (400-800 μM) causes concentration-dependent killing of seven different human cancer cell lines (HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS) but did not affect survival of normal human lung fibroblasts (IMR90, WI-38)[2].
    GYY4137 (0.1-0.5 mM) decreases LPS-induced production of nitrite (NO2 ), PGE2, TNF-α and IL-6 from human synoviocytes (HFLS) and articular chondrocytes (HAC), reduces the levels and catalytic activity of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) and reduced LPS-induced NF-κB activation[3].

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

    Cell Viability Assay[2]

    Cell Line: HeLa, HCT-116, Hep G2, HL-60, MCF-7, MV4-11 and U2OS
    Concentration: 400 or 800 µM
    Incubation Time: 5 days
    Result: Significantly affected cancer cell survivability.
    In Vivo

    GYY4137 (100-300 mg/kg; i.p.; daily for 14 days) significantly reduces the tumor volume in both animal models, in a dose-dependent manner[2].
    In the complete Freund's adjuvant (CFA)-treated mouse, GYY4137 (50 mg/kg, i.p.) injected 1 hr prior to CFA increased knee joint swelling while an anti-inflammatory effect, as demonstrated by reduced synovial fluid myeloperoxidase (MPO) and N-acetyl-β-D-glucosaminidase (NAG) activity and decreased TNF-α, IL-1β, IL-6 and IL-8 concentration, was apparent when GYY4137 was injected 6 hrs after CFA[3].
    GYY4137 significantly inhibited tumor growth in the subcutaneous HepG2 xenograft model by inhibiting STAT3 activation and its target gene expression[4].
    GYY4137 prevents nitrative stress and α-synuclein nitration in an MPTP mouse model of parkinson’s disease[5].

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

    Animal Model: Female, severe combined immunodeficiency (SCID) mice (bearing HL-60 or MV4-11 cells)[2]
    Dosage: 100, 200 and 300 mg/kg
    Administration: I.p.; daily for 14 days
    Result: Reduced tumor volume by 52.5% and 55.3% in HL-60 and MV4–11 injected animals.
    Molecular Weight

    376.47

    Formula

    C15H25N2O3PS2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    SP(N1CCOCC1)(C2=CC=C(OC)C=C2)=S.N3CCOCC3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    -20°C, stored under nitrogen

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (265.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 19.23 mg/mL (51.08 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.6563 mL 13.2813 mL 26.5625 mL
    5 mM 0.5313 mL 2.6563 mL 5.3125 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). 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  PBS

      Solubility: 50 mg/mL (132.81 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    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: 98.08%

    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 (stored under nitrogen). 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 / DMSO 1 mM 2.6563 mL 13.2813 mL 26.5625 mL 66.4064 mL
    5 mM 0.5313 mL 2.6563 mL 5.3125 mL 13.2813 mL
    10 mM 0.2656 mL 1.3281 mL 2.6563 mL 6.6406 mL
    15 mM 0.1771 mL 0.8854 mL 1.7708 mL 4.4271 mL
    20 mM 0.1328 mL 0.6641 mL 1.3281 mL 3.3203 mL
    25 mM 0.1063 mL 0.5313 mL 1.0625 mL 2.6563 mL
    30 mM 0.0885 mL 0.4427 mL 0.8854 mL 2.2135 mL
    40 mM 0.0664 mL 0.3320 mL 0.6641 mL 1.6602 mL
    50 mM 0.0531 mL 0.2656 mL 0.5313 mL 1.3281 mL
    DMSO 60 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1068 mL
    80 mM 0.0332 mL 0.1660 mL 0.3320 mL 0.8301 mL
    100 mM 0.0266 mL 0.1328 mL 0.2656 mL 0.6641 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.

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Requested Quantity *

    Applicant Name *

     

    Salutation

    Email Address *

     

    Phone Number *

    Department

     

    Organization Name *

    City

    State

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GYY4137
    Cat. No.:
    HY-107632
    Quantity:
    MCE Japan Authorized Agent: