2. Epigenetics Immunology/Inflammation
  3. Protein Arginine Deiminase MHC
  4. GSK484

GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8+ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions.

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CAS No. : 1652629-23-6

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Based on 49 publication(s) in Google Scholar

Other Forms of GSK484:

GSK484 Related Antibodies

Top Publications Citing Use of Products

49 Publications Citing Use of MCE GSK484

In Vivo Efficacy Study

    GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 30:S1535-6108(25)00320-4.  [Abstract]

    Schema for GSK484 treatment protocol and summary tumor growth curves of MC38 in Dnase1l3fl/fl and Dnase1l3cko mice (n = 7).

    GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are BLI quantification of primary tumor growth at day 19.

    GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are BLI quantification of lung metastasis at week 5.

    GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are pulmonary surface nodules at week 5.

    GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are NET formation in lung metastases.

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    Description

    GSK484 is a PAD4 inhibitor that effectively inhibits protein citrullination and the formation of neutrophil extracellular traps (NETs) by blocking the catalytic activity of PAD4. GSK484 suppresses the production of histone H3, MHC-I expression, CD8+ T cell activation, proliferation and inflammatory cytokine release. GSK484 reduces inflammation and bone destruction in collagen-induced rheumatoid arthritis, alleviates pain and mast cell activation in sickle cell disease, and improves myocardial ischemia-reperfusion injury and experimental colitis. In addition, GSK484 restores intestinal microbial homeostasis by reversing ferroptosis-induced dysbiosis. GSK484 can be used to study the disease mechanisms of rheumatoid arthritis, sickle cell disease, thrombosis, myocardial injury, colitis and other conditions[1][2][3][4][5][6].

    In Vitro

    GSK484 (10 μM; 6 h) inhibits the expression of citrullinated histone H3, HLA class I (MHC-I), HLA-A2 induced by Erastin (HY-15763) in human rheumatoid arthritis fibroblast-like synoviocytes; in the co-culture system of human rheumatoid arthritis fibroblast-like synoviocytes and CD8+ T cells, it suppresses the activation, proliferation and inflammatory cytokine release of CD8+ T cells[1].
    GSK484 inhibits the ferroptosis-upregulated expression of PAD4 and the associated inflammatory responses in rheumatoid arthritis fibroblast-like synoviocytes (RA-FLS)[2].
    GSK484 (10 μM) completely abolishes heme/TNFα-induced mast cell extracellular trap (mast cell extracellular trap, MCET) formation in mast cells isolated from the dorsal skin of homozygous BERK sickle cell (HbSS) mice[3].
    Pretreatment with GSK484 (10 μM) for 2 hours before hypoxia maintains intracellular ATP levels in primary cultured neonatal wild-type mouse cardiomyocytes at 4 h of reoxygenation, and improves their metabolic activity at 20 h of reoxygenation. In contrast, administration of GSK484 at the onset of reoxygenation only improves metabolic activity at 20 h of reoxygenation, but fails to maintain ATP levels[4].
    GSK484 (10 μM; 15 min pre-treatment) potently inhibits extracellular DNA production and H3Cit+ neutrophil formation induced by Ionomycin (HY-13434) in human neutrophils after 3 h of stimulation; however, it exerts no such effect on neutrophils stimulated with PMA (HY-18739) or isolated from patients with SCD[5].

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

    GSK484 Related Antibodies

    ELISA Assay[1]

    Cell Line: Rheumatoid arthritifibroblast-like synoviocytes (RA-FLs)
    Concentration: 10 μM
    Incubation Time: 6 h; with or without the ferroptosis activator Erastin (HY-15763) (0, 2.5, 5, or 7.5 μM) or the Fer-1 (HY-100579) (0, 5, 10, or 15 μM) for 48 h
    Result: Inhibited erastin-induced increase in HLA-I.
    Inhibited erastin-induced T cell activation marker expression increase.
    Parmacokinetics
    Species Dose Route T1/2 CLblood
    Mice[6] 4 mg/kg i.p. 3.8 h 19 mL/min/kg
    In Vivo

    GSK484 (10 mg/kg; i.p.; 3 times per week; 6 total administrations) inhibits joint inflammation, bone destruction, synovial hyperplasia, and expression of inflammatory markers exacerbated by Erastin (HY-15763) in CIA mice, and alleviates the pathological effects caused by enhanced ferroptosis in this disease model[1].
    GSK484 (10 mg/kg; i.p.; 3 times per week; 6 total administrations) reduces joint inflammation and bone destruction in CIA mice, reverses intestinal dysbiosis, restores metabolic profiles to normal, and alleviates the deterioration of RA-related pathologies induced by Erastin (HY-15763)[2].
    GSK484 (20 mg/kg; s.c.; daily; 30 d) produces sustained inhibition of neuropathic hyperalgesia in homozygous BERK sickle cell mice, while exerting extensive anti-inflammatory and hematological benefits without the development of analgesic tolerance[3].
    GSK484 (10 μM; single dose; 30 minutes prior to thrombus induction) significantly prolongs the blood flow cessation time of cerebral arterioles and venules in C57BL/6 mice in a light-activated thrombosis model, and significantly increases the blood flow cessation time of cerebral arterioles and venules in sickle cell transgenic mice[5].
    GSK484 (4 mg/kg; i.p.; once every 2 days; 9 d) significantly reduces the density of neutrophil extracellular traps (NETs) in the colonic mucosa of mice with colitis induced by 2% (w/v) DSS (HY-116282C) (36-50 kd), but fails to improve clinical or inflammatory disease biomarkers[6].

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

    Animal Model: DBA/1J mice with Rheumatoid arthritis (male, 8 weeks old, 21±2 g, SPF grade, collagen-induced arthritis model)[1]
    Dosage: 10 mg/kg
    Administration: i.p.; three times a week; total of 6 times
    Result: Inhibited erastin-exacerbated paw inflammation and reduced paw thickness compared to erastin-only treatment.
    Inhibited erastin-exacerbated bone destruction, with micro-CT showing reduced joint damage relative to erastin-only treatment.
    Reduced erastin-increased joint inflammation scores, bone erosion scores, and synovial hyperplasia scores via histological scoring.
    Reduced erastin-increased MHC-I, citrullinated histone H3 (cit-h3), PAD4, CD8, TNF-α, and IFN-γ positive cell percentages in joint tissue via immunohistochemical analysis.
    Animal Model: homozygous BERK sickle (HbSS) mcie with Sickle cell disease[3]
    Dosage: 20 mg/kg
    Administration: s.c.; daily; 30 days
    Result: Significantly reduced cold hyperalgesia at 48 hours.
    Significantly reduced heat hyperalgesia at 72 hours.
    Significantly reduced mechanical hyperalgesia after 1 week with attenuation persisting through 30 days and no analgesic tolerance observed.
    Decreased skin mast cell degranulation by 90%.
    Significantly reduced white blood cell counts.
    Significantly reduced serum GM-CSF levels.
    Significantly increased hematocrit.
    Reduced skin levels of inflammatory cytokines CCL2/MCP-1, TNFα, and RANTES by approximately 50% relative to baseline/control groups.
    Animal Model: Cerebrovascular thrombosis model in C57BL/6 mice (male and female, 8-10 weeks of age), Townes mice (male and female, 8-10 weeks of age, sickle transgenic)[5]
    Dosage: 10 μM
    Administration: single dose (30 minutes prior to thrombosis induction)
    Result: Significantly prolonged blood flow cessation time in both cerebrovascular arterioles and venules compared to vehicle-treated mice (C57BL/6).
    Significantly increased blood flow cessation time in both cerebrovascular arterioles and venules compared to vehicle-treated mice (Townes), with a mean flow cessation time of ~28 minutes in arterioles and ~21 minutes in venules.
    Animal Model: C57BL/6 mice with Inflammatory bowel disease (male, 7 weeks of age at study start, 2% w/v DSS-induced colitis)[6]
    Dosage: 4 mg/kg
    Administration: i.p.; every second day; 9 days
    Result: Significantly diminished colonic mucosal neutrophil extracellular trap (NET) density to levels similar to control mice.
    Did not improve disease activity index scores, weight loss, colon length, colon weight/length ratio, fecal hemoglobin levels, or colonic/faecal calprotectin levels compared to DSS-only treated mice.
    Did not reduce DSS-induced colon histoarchitectural damage, goblet cell loss, or mast cell density, nor alter levels of inflammatory cytokines IL-1β, IL-4, or IL-10.
    Caused a statistically significant reduction in total superoxide dismutase (SOD) activity in colonic tissue.
    Had no effect on catalase activity, Nrf2, GPx4, or SOD1 protein expression, or colonic lipid peroxidation.
    Molecular Weight

    473.57

    Formula

    C27H31N5O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3C(N=C(C(N4CC5CC5)=CC6=C4C=CC=C6)N3C)=C2
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (105.58 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 2.1116 mL 10.5581 mL 21.1162 mL
    5 mM 0.4223 mL 2.1116 mL 4.2232 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:

    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 (5.28 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 (5.28 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.
    In Vivo Dissolution Calculator
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    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).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    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 2.1116 mL 10.5581 mL 21.1162 mL 52.7905 mL
    5 mM 0.4223 mL 2.1116 mL 4.2232 mL 10.5581 mL
    10 mM 0.2112 mL 1.0558 mL 2.1116 mL 5.2791 mL
    15 mM 0.1408 mL 0.7039 mL 1.4077 mL 3.5194 mL
    20 mM 0.1056 mL 0.5279 mL 1.0558 mL 2.6395 mL
    25 mM 0.0845 mL 0.4223 mL 0.8446 mL 2.1116 mL
    30 mM 0.0704 mL 0.3519 mL 0.7039 mL 1.7597 mL
    40 mM 0.0528 mL 0.2640 mL 0.5279 mL 1.3198 mL
    50 mM 0.0422 mL 0.2112 mL 0.4223 mL 1.0558 mL
    60 mM 0.0352 mL 0.1760 mL 0.3519 mL 0.8798 mL
    80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6599 mL
    100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5279 mL
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    GSK484 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:

    GSK4841652629-23-6GSK 484GSK-484Protein Arginine DeiminaseMHCPeptidylarginine DeiminaseMajor Histocompatibility Complexprotein arginine residue citrullinationhistone H3 citrullinationrheumatoid arthritis-associated cellssickle cell disease modelsextracellular trap formationcollagen-induced arthritis micepeptidyl arginine deiminase 4gut microbiotaPAD4cardiomyocyteInhibitorinhibitorinhibit

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