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

GSK484 是一种 PAD4 抑制剂，通过阻断 PAD4 催化活性，有效抑制蛋白瓜氨酸化及胞外诱捕网 (NETs) 的形成。GSK484 可抑制组蛋白 H3 的生成、MHC-I 表达、CD8+ T 细胞活化、增殖及炎症细胞因子释放。GSK484 可减轻胶原诱导性类风湿关节炎的炎症与骨破坏、缓解镰状细胞病的疼痛与肥大细胞活化，以及改善心肌缺血再灌注损伤和实验性结肠炎。此外，GSK484 还能通过逆转铁死亡诱导的菌群失调来恢复肠道微生物稳态。GSK484 可用于研究类风湿关节炎、镰状细胞病、血栓、心肌损伤及结肠炎等疾病机制。

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CAS No. : 1652629-23-6

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Other Forms of GSK484:

GSK484 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 44 篇科研文献

In Vivo Efficacy Study

    GSK484 purchased from MCE. 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 MCE. 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 MCE. 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 MCE. 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 MCE. 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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    MHC I MHC II

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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].
    体外研究
    (In Vitro)

    GSK484 (10 μM; 6 h) 可抑制 Erastin (HY-15763) 诱导的人类类风湿关节炎成纤维样滑膜细胞中瓜氨酸化组蛋白 H3、HLA class I (MHC-I)、HLA-A2 的表达；在人类类风湿关节炎成纤维样滑膜细胞与 CD8+ T 细胞共培养体系中，的活化、增殖及炎症因子释放[1]。
    GSK484 抑制铁死亡上调的 PAD4 表达以及类风湿关节炎成纤维样滑膜细胞 (RA-FLS) 中相关的炎症反应[2]。
    GSK484 (10 μM) 可完全消除从纯合 BERK 镰状细胞 (HbSS) 小鼠背部皮肤分离的肥大细胞中由血红素/TNFα 诱导的巨细胞胞外诱捕网 (mast cell extracellular trap, MCET) 形成[3]。
    GSK484 (10 μM) 在缺氧前预孵育 2 小时的情况下，可在复氧 4 h 时维持原代培养的新生野生型小鼠心肌细胞的细胞内 ATP 水平，并在复氧 20 h 时改善其代谢活性；而在复氧开始时给药的情况下，仅能在复氧 20 h 时改善代谢活性，无法维持 ATP 水平[4]。
    GSK484 (10 μM; 15 min 预处理) 可强效抑制人中性粒细胞中由 Ionomycin (HY-13434) 诱导 3 h 后的细胞外 DNA 产生及 H3Cit+ 中性粒细胞形成；但对 PMA (HY-18739) 刺激或 SCD 患者分离的中性粒细胞无该效果[5]。

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

    GSK484 相关抗体:

    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.
    药代动力学
    (Parmacokinetics)
    Species Dose Route T1/2 CLblood
    Mice[6] 4 mg/kg i.p. 3.8 h 19 mL/min/kg
    体内研究
    (In Vivo)

    GSK484 (10 mg/kg; i.p.; 每周 3 次; 共 6 次) 可抑制 Erastin (HY-15763) 加重的 CIA 小鼠关节炎症、骨破坏、滑膜增生及炎症标志物表达，减轻该疾病模型中铁死亡增强带来的病理效应[1]。
    GSK484 (10 mg/kg; i.p.; 每周 3 次; 共 6 次) 可减轻 CIA 小鼠的关节炎症与骨破坏，逆转肠道菌群失调，使代谢谱恢复正常，并缓解 Erastin (HY-15763) 诱导的 RA 相关病理恶化[2]。
    GSK484 (20 mg/kg; s.c.; 每日; 30 d) 可对纯合 BERK 镰状细胞小鼠产生持久的神经病理性痛觉过敏抑制作用，同时发挥广泛的抗炎及血液学益处，且无镇痛耐受现象[3]。
    GSK484 (10 μM; 单剂量; 血栓诱导前 30 分钟) 可在光激活血栓形成模型中显著延长 C57BL/6 小鼠脑小动脉和小静脉的血流停止时间，并显著增加镰状细胞转基因小鼠脑小动脉和小静脉的血流停止时间[5]。
    GSK484 (4 mg/kg; i.p.; 每 2 天 1 次; 9 d) 可显著降低 2% (w/v) DSS (HY-116282C) (36-50 kd) 诱导的结肠炎小鼠结肠黏膜 NET 密度，但无法改善临床或炎症疾病生物标志物[6]。

    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.
    分子量

    473.57

    Formula

    C27H31N5O3
    CAS 号
    性状

    固体

    颜色

    White to off-white

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (105.58 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.28 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.28 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料
    参考文献

    GSK484 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 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
    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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