GSK484
Based on 57 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.14%
- CAS No.: 1652629-23-6
- 화학식: C27H31N5O3
- 분자량:473.57
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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HY-108882
DNase I, Bovine pancreasEnzyme -
HY-100514
GSK484 hydrochloridePAD4 Inhibitor -
HY-100574A
Cl-amidine hydrochloridePAD Inhibitor -
HY-103058
GSK199PAD4 Inhibitor -
HY-137655
BMS-P5PAD4 Inhibitor -
HY-120343
GSK106 -
HY-100579
Ferrostatin-1Ferroptosis Inhibitor -
HY-112879
Mito-TEMPOAntioxidant -
HY-100965
Diphenyleneiodonium chlorideNOX Inhibitor -
HY-14622A
Necrostatin 2 racemateRIPK1 Inhibitor -
HY-K0301
Cell Counting Kit-8 -
HY-137655A
BMS-P5 free basePAD4 Inhibitor
Publications Citing Use of MedChemExpress (MCE) GSK484
More- Cancer Cell. 2025 Sep 8;43(9):1758-1775.e8. [Abstract]
- Cancer Cell. 2021 Mar 8;39(3):423-437.e7. [Abstract]
- Immunity. 2023 Dec 12;56(12):2755-2772.e8. [Abstract]
- Immunity. 2020 May 19;52(5):856-871.e8. [Abstract]
- Cancer Commun (Lond). 2025 Dec 15.
- Cell Mol Immunol. 2024 May;21(5):510-526. [Abstract]
- Adv Funct Mater. 2025 Aug 3.
- Nat Commun. 2023 Feb 16;14(1):872. [Abstract]
- J Adv Res. 2026 Jun 5:S2090-1232(26)00460-1. [Abstract]
- Mol Cell. 2025 Oct 2;85(19):3588-3604.e11. [Abstract]
- Adv Sci (Weinh). 2026 Apr;13(20):e18588. [Abstract]
- Adv Sci (Weinh). 2025 Aug 20:e11873. [Abstract]
- Adv Sci (Weinh). 2025 Jul 21:e00950. [Abstract]
- Adv Sci (Weinh). 2025 Apr;12(16):e2411524. [Abstract]
- Adv Sci (Weinh). 2025 Mar;12(11):e2406359. [Abstract]
- Adv Sci (Weinh). 2023 Oct;10(29):e2301835. [Abstract]
- Cell Death Differ. 2026 Jan 15. [Abstract]
- Research (Wash D C). 2026 May 8:9:1266. [Abstract]
- Pharmacol Res. 2021 Aug:170:105712. [Abstract]
- J Immunother Cancer. 2024 Jun 26;12(6):e009082. [Abstract]
- Phytomedicine. 2026 Aug:158:158386. [Abstract]
- Diabetologia. 2025 Apr;68(4):866-889. [Abstract]
- J Tissue Eng. 2025 Aug 19:16:20417314251348038. [Abstract]
- Apoptosis. 2023 Oct;28(9-10):1484-1495. [Abstract]
- Aging Cell. 2026 Aug;25(8):e70640.
- Cell Rep. 2026 Jul 28:117684.
- Cell Rep. 2021 Sep 21;36(12):109750. [Abstract]
- Br J Pharmacol. 2026 May 27. [Abstract]
- Front Immunol. 2022 Feb 16:13:781273. [Abstract]
- JCI Insight. 2026 May 22;11(10):e191979. [Abstract]
- JCI Insight. 2026 Feb 3:e199307. [Abstract]
- OncoImmunology. 2022 Mar 16;11(1):2052418. [Abstract]
- Int Immunopharmacol. 2025 Jun 26:159:114939. [Abstract]
- Int Immunopharmacol. 2022 Sep:110:108965. [Abstract]
- Int Immunopharmacol. 2021 May:94:107486. [Abstract]
- Front Cell Infect Microbiol. 2025 Jun 11:15:1540634. [Abstract]
- Mucosal Immunol. 2025 Apr 19:S1933-0219(25)00044-3. [Abstract]
- J Thromb Haemost. 2024 Jan;22(1):188-198. [Abstract]
- Rheumatology (Oxford). 2025 Aug 13:keaf437. [Abstract]
- Transl Stroke Res. 2024 Dec 28. [Abstract]
- FEBS J. 2023 Nov;290(22):5395-5410. [Abstract]
- Transl Stroke Res. 2022 Feb;13(1):112-131. [Abstract]
- Parasit Vectors. 2025 Jul 1;18(1):248. [Abstract]
- Kidney Dis (Basel). 2025 May 9;11(1):450-468. [Abstract]
- Fitoterapia. 2025 Sep:185:106771. [Abstract]
- Vet Microbiol. 2026 May:316:110968. [Abstract]
- Physiol Res. 2026 Mar 11;75(1):29-43. [Abstract]
- STAR Protoc. 2026 Jan 12;7(1):104326. [Abstract]
- Res Sq. 2026 Jun 30.
- Hlife. 2026 Mar 18.
- bioRxiv. 2025 Sep 5.
- bioRxiv. 2024 Oct 4:2024.10.04.616580. [Abstract]
- bioRxiv. 2024 July 01.
- Sci Tradit Chin Med. 2023 Sep 20.
- Research Square Preprint. 2023 May 11.
- bioRxiv. 2023 Apr 3.
- Aging Cell. 2019 Aug 31;11(17):6951-6959. [Abstract]
Customer Validation & Images
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Biological Activity
제품 설명
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.
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Cell Line:Rheumatoid arthritifibroblast-like synoviocytes (RA-FLs)
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Concentration:10 μM
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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
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Result:Inhibited erastin-induced increase in HLA-I.
Inhibited erastin-induced T cell activation marker expression increase.
Parmacokinetics
| Species | Dose | Route | T1/2 | CLblood |
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| 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) 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.
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Animal Model:DBA/1J mice with Rheumatoid arthritis (male, 8 weeks old, 21±2 g, SPF grade, collagen-induced arthritis model)[1]
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Dosage:10 mg/kg
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Administration:i.p.; three times a week; total of 6 times
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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.
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Animal Model:homozygous BERK sickle (HbSS) mcie with Sickle cell disease[3]
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Dosage:20 mg/kg
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Administration:s.c.; daily; 30 days
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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.
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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]
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Dosage:10 μM
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Administration:single dose (30 minutes prior to thrombosis induction)
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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.
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Animal Model:C57BL/6 mice with Inflammatory bowel disease (male, 7 weeks of age at study start, 2% w/v DSS-induced colitis)[6]
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Dosage:4 mg/kg
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Administration:i.p.; every second day; 9 days
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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.
Chemical Information
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CAS No. 1652629-23-6
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Appearance Solid
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분자량 473.57
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화학식 C27H31N5O3
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Color White to off-white
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (57)
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Journal Impact Factor
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Most Recent
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Cancer Cell
DNASE1L3-expressing dendritic cells promote CD8+ T cell function and anti-PD-(L)1 therapy efficacy by degrading neutrophil extracellular traps. [Abstract]2025 Sep 8;43(9):1758-1775.e8. PMID: 40816293
GSK484 purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Sep 8;43(9):1758-1775.e8. [Abstract]
Schema for GSK484 treatment protocol and summary tumor growth curves of MC38 in Dnase1l3fl/fl and Dnase1l3cko mice (n = 7).
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Cancer Cell
Cathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. [Abstract]2021 Mar 8;39(3):423-437.e7. PMID: 33450198
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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Immunity
The tumor-derived cytokine Chi3l1 induces neutrophil extracellular traps that promote T cell exclusion in triple-negative breast cancer. [Abstract]2023 Dec 12;56(12):2755-2772.e8. PMID: 38039967 -
Immunity
CXCR1 and CXCR2 Chemokine Receptor Agonists Produced by Tumors Induce Neutrophil Extracellular Traps that Interfere with Immune Cytotoxicity. [Abstract]2020 May 19;52(5):856-871.e8. PMID: 32289253 -
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Cell Mol Immunol
Neutrophil ALDH2 is a new therapeutic target for the effective treatment of sepsis-induced ARDS. [Abstract]2024 May;21(5):510-526. PMID: 38472357 -
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Nat Commun
Oxidized mitochondrial DNA induces gasdermin D oligomerization in systemic lupus erythematosus. [Abstract]2023 Feb 16;14(1):872. PMID: 36797275 -
J Adv Res
PAD4-mediated citrullination of IGF2BP2 stabilizes MCM mRNAs to drive intrahepatic cholangiocarcinoma progression. [Abstract]2026 Jun 5:S2090-1232(26)00460-1. PMID: 42250722 -
Mol Cell
2025 Oct 2;85(19):3588-3604.e11. PMID: 41043392 -
Adv Sci (Weinh)
Bifidobacterium Breve Yang08 Alleviates Atopic Dermatitis By Enriching Akkermansia Muciniphila and Inhibiting Neutrophil Extracellular Traps Formation In Mice. [Abstract]2026 Apr;13(20):e18588. PMID: 41655253 -
Adv Sci (Weinh)
Succinate Dehydrogenase Subunit A (SDHA) Mediated Microglia Extracellular Traps Formation Participating in Cerebral Ischemic Reperfusion Injury. [Abstract]2025 Aug 20:e11873. PMID: 40832885 -
Adv Sci (Weinh)
The CXCL10-CXCR3 Axis Induces Tumor-Associated Neutrophils to Interfere with CTLs-Mediated Antitumor Activity in EBV-Associated Epithelial Cancers. [Abstract]2025 Jul 21:e00950. PMID: 40686457 -
Adv Sci (Weinh)
2025 Apr;12(16):e2411524. PMID: 40013981 -
Adv Sci (Weinh)
ACSL1 Aggravates Thromboinflammation by LPC/LPA Metabolic Axis in Hyperlipidemia Associated Myocardial Ischemia-Reperfusion Injury. [Abstract]2025 Mar;12(11):e2406359. PMID: 39853712 -
Adv Sci (Weinh)
Neutrophil-Mediated Tumor-Targeting Delivery System of Oncolytic Bacteria Combined with ICB for Melanoma Lung Metastasis Therapy. [Abstract]2023 Oct;10(29):e2301835. PMID: 37565362 -
Cell Death Differ
EGFR orchestrates neutrophil activation and NETosis via CEBPβ-dependent PGLYRP1 induction. [Abstract]2026 Jan 15. PMID: 41540251 -
Research (Wash D C)
Neuromodulation and Copper Chelation Reverse Sleep Fragmentation-Aggravated Myocardial Ischemia-Reperfusion Injury by Targeting NET-Induced Endothelial Cuproptosis. [Abstract]2026 May 8:9:1266. PMID: 42109881 -
Pharmacol Res
Targeting P2RX1 alleviates renal ischemia/reperfusion injury by preserving mitochondrial dynamics. [Abstract]2021 Aug:170:105712. PMID: 34091010 -
J Immunother Cancer
Tumor cell-released autophagosomes (TRAPs) induce PD-L1-decorated NETs that suppress T-cell function to promote breast cancer pulmonary metastasis. [Abstract]2024 Jun 26;12(6):e009082. PMID: 38926151 -
Phytomedicine
Shegan Mahuang Decoction ameliorates pulmonary fibrosis progression by inhibiting CCL3-mediated NETosis. [Abstract]2026 Aug:158:158386. PMID: 42275874 -
Diabetologia
Intestinal neutrophil extracellular traps promote gut barrier damage exacerbating endotoxaemia, systemic inflammation and progression of diabetic retinopathy in type 2 diabetes. [Abstract]2025 Apr;68(4):866-889. PMID: 39875729 -
J Tissue Eng
Formation of neutrophil extracellular traps in the early stages exacerbate the healing process by regulating macrophage polarization in Achilles tendon-bone injury. [Abstract]2025 Aug 19:16:20417314251348038. PMID: 40843411 -
Apoptosis
Neutrophil extracellular traps mediate TLR9/Merlin axis to resist ferroptosis and promote triple negative breast cancer progression. [Abstract]2023 Oct;28(9-10):1484-1495. PMID: 37368176 -
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Cell Rep
Inappropriate use of antibiotics exacerbates inflammation through OMV-induced pyroptosis in MDR Klebsiella pneumoniae infection. [Abstract]2021 Sep 21;36(12):109750. PMID: 34551309 -
Br J Pharmacol
Neutrophil extracellular traps drive tubulointerstitial fibrosis via the coiled-coil domain-containing protein 25 (CCDC25)-Yes-associated protein 1 (YAP1) axis-mediated autophagy regulation. [Abstract]2026 May 27. PMID: 42204873 -
Front Immunol
Reduced Neutrophil Extracellular Trap Formation During Ischemia Reperfusion Injury in C3 KO Mice: C3 Requirement for NETs Release. [Abstract]2022 Feb 16:13:781273. PMID: 35250972 -
JCI Insight
HMGB1-mediated formation of IL-33-abundant NETs drives lung-to-kidney injury in severe pneumonia-associated acute kidney injury. [Abstract]2026 May 22;11(10):e191979. PMID: 42171612 -
JCI Insight
The CHI3L1-neutrophil axis drives immune suppression and breast cancer metastatic dissemination. [Abstract]2026 Feb 3:e199307. PMID: 41632530 -
OncoImmunology
Neutrophil extracellular traps induce tumor metastasis through dual effects on cancer and endothelial cells. [Abstract]2022 Mar 16;11(1):2052418. PMID: 35309732 -
Int Immunopharmacol
The natural compound PEITC ameliorates imiquimod-induced psoriasis in mice by suppressing neutrophil extracellular traps formation. [Abstract]2025 Jun 26:159:114939. PMID: 40414074 -
Int Immunopharmacol
2022 Sep:110:108965. PMID: 35764017 -
Int Immunopharmacol
Protectin D1 decreases pancreatitis severity in mice by inhibiting neutrophil extracellular trap formation. [Abstract]2021 May:94:107486. PMID: 33639566 -
Front Cell Infect Microbiol
Veillonella parvula outer membrane vesicles increase ICAM-1+ neutrophils exhibiting elevated NET formation via ROS-PAD4 signaling. [Abstract]2025 Jun 11:15:1540634. PMID: 40568695 -
Mucosal Immunol
2025 Apr 19:S1933-0219(25)00044-3. PMID: 40258416 -
J Thromb Haemost
NETs induce persistent lung tissue damage via thromboinflammation without altering virus resolution in a mouse coronavirus model. [Abstract]2024 Jan;22(1):188-198. PMID: 37748582 -
Rheumatology (Oxford)
Autophagy inhibitors block pathogenic NET release in immune-mediated inflammatory disease without impairing host defence. [Abstract]2025 Aug 13:keaf437. PMID: 40802538 -
Transl Stroke Res
Neutrophil Extracellular Traps Induce Brain Edema Around Intracerebral Hematoma via ERK-Mediated Regulation of MMP9 and AQP4. [Abstract]2024 Dec 28. PMID: 39733198 -
FEBS J
Neutrophil extracellular traps boost laser-induced mouse choroidal neovascularization through the activation of the choroidal endothelial cell TLR4/HIF-1α pathway. [Abstract]2023 Nov;290(22):5395-5410. PMID: 37552110 -
Transl Stroke Res
Neutrophil Extracellular Traps may be a Potential Target for Treating Early Brain Injury in Subarachnoid Hemorrhage. [Abstract]2022 Feb;13(1):112-131. PMID: 33852132 -
Parasit Vectors
Pentatrichomonas hominis induces extracellular traps formation of macrophages via the TLR2/NADPH/PAD4 pathway. [Abstract]2025 Jul 1;18(1):248. PMID: 40598534 -
Kidney Dis (Basel)
Clinical and Experimental Insights into the Role of NETosis in IgA Nephropathy Pathogenesis. [Abstract]2025 May 9;11(1):450-468. PMID: 40606676 -
Fitoterapia
Er Miao San and its main components phellodendrine and atractylenolide-I exert anti-rheumatoid arthritis effects by inhibiting PAD4 and thereby reducing the formation of NETs. [Abstract]2025 Sep:185:106771. PMID: 40738459 -
Vet Microbiol
The PERK-eIF2α branch activates the NLRP3 inflammasome through the NF-κB signaling pathway to suppress NDV replication. [Abstract]2026 May:316:110968. PMID: 41793984 -
Physiol Res
Targeting the Toll-Like Receptor 4 Ameliorates Heart Failure in Aged Mice by Inhibiting the Formation of Neutrophil Extracellular Traps. [Abstract]2026 Mar 11;75(1):29-43. PMID: 41811699 -
STAR Protoc
Protocol for identification of protein citrullination by immunoprecipitation followed by mass spectrometry. [Abstract]2026 Jan 12;7(1):104326. PMID: 41528850 -
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bioRxiv
APOE Protects Against Severe Infection with Mycobacterium tuberculosis by Restraining Production of Neutrophil Extracellular Traps. [Abstract]2024 Oct 4:2024.10.04.616580. PMID: 39605723 -
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Aging Cell
Kindlin-3 in platelets and myeloid cells differentially regulates deep vein thrombosis in mice. [Abstract]2019 Aug 31;11(17):6951-6959. PMID: 31477636
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (287 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Zhu X, et al. Ferrostatin-1 reduces the inflammatory response of rheumatoid arthritis by decreasing the antigen presenting function of fibroblast-like synoviocytes. J Transl Med. 2025;23(1):280. Published 2025 Mar 6. [Content Brief]
[2]. Zhu X, et al. Ferroptosis Induces gut microbiota and metabolic dysbiosis in Collagen-Induced arthritis mice via PAD4 enzyme. Gene. 2025;936:149106. [Content Brief]
[4]. Mand M, et al. Peptidylarginine deiminase 4 deficiency alleviates hypoxia/reoxygenation-induced cardiomyocyte injury. PLoS One. 2025;20(9):e0330864. Published 2025 Sep 10. [Content Brief]
[5]. Ansari J, et al. Regulating Neutrophil PAD4/NOX-Dependent Cerebrovasular Thromboinflammation. Int J Biol Sci. 2023;19(3):852-864. Published 2023 Jan 9. [Content Brief]
[6]. Xie K, et al. The PAD4 inhibitor GSK484 diminishes neutrophil extracellular trap in the colon mucosa but fails to improve inflammatory biomarkers in experimental colitis. Biosci Rep. Published online May 20, 2025. [Content Brief]
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 |
GSK484 Related Classifications
HY-123606 Related Classifications
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Keywords
- GSK484
- 1652629-23-6
- GSK 484
- GSK-484
- Protein Arginine Deiminase
- MHC
- protein arginine residue citrullination
- histone H3 citrullination
- rheumatoid arthritis-associated cells
- sickle cell disease models
- extracellular trap formation
- collagen-induced arthritis mice
- peptidyl arginine deiminase 4
- gut microbiota
- PAD4
- cardiomyocyte
- Inhibitor
- inhibitor
- inhibit