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Chemical Structure| 1652591-81-5 Chemical Structure| 1652591-81-5

Structure of GSK484 HCl
CAS No.: 1652591-81-5

Chemical Structure| 1652591-81-5

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GSK484 is a reversible and selective inhibitor of PAD4 with IC50 of 50 nM. GSK484 blocks the citrullination of PAD4 target proteins in human neutrophils and inhibits the formation of neutrophil extracellular traps in both mouse and human neutrophils.

Synonyms: GSK484 (hydrochloride); GSK484 hydrochloride

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Product Details of GSK484 HCl

CAS No. :1652591-81-5
Formula : C27H32ClN5O3
M.W : 510.03
SMILES Code : O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3C(N=C(C(N4CC5CC5)=CC6=C4C=CC=C6)N3C)=C2.[H]Cl
Synonyms :
GSK484 (hydrochloride); GSK484 hydrochloride
MDL No. :MFCD30343874
InChI Key :MULKOGJHUZTANI-ADMBKAPUSA-N
Pubchem ID :86340151

Safety of GSK484 HCl

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of GSK484 HCl

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Primary mouse neutrophils 10 μmol/L 3 hours Inhibited NET formation Cell Mol Gastroenterol Hepatol. 2022;14(3):587-607.
PC12 cells 150 μM 24 hours Evaluate the effect of T-GSK on intracellular ROS clearance, results showed that T-GSK significantly reduced ROS levels after H2O2 stimulation Adv Sci (Weinh). 2024 Jun;11(21):e2308719.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Traumatic brain injury (TBI) and middle cerebral artery occlusion (MCAO) models Intravenous injection 8 mg/kg Injections at MCAO onset, 24 h, and 48 h after occlusion, lasting for 72 hours Evaluate the neuroprotective effects of T-GSK in TBI and MCAO models, results showed that T-GSK significantly reduced brain infarction area, brain edema, and neurological deficits, and inhibited the formation of NETs Adv Sci (Weinh). 2024 Jun;11(21):e2308719.
Mice Myocardial ischemia/reperfusion injury model Intraperitoneal injection 10 mg/kg Once daily for 3 days after surgery To evaluate the therapeutic effect of GSK484 on myocardial ischemia/reperfusion injury, results showed that GSK484 significantly reduced myocardial damage and NETosis. Eur Heart J. 2024 May 13;45(18):1662-1680
C57BL/6 mice CLP-induced SAE model Tail vein injection 4 mg/kg Three days before and two days after CLP surgery, total 5 days To evaluate the effect of GSK484 on neuroinflammation, BBB integrity, and cognitive function in SAE mice, results showed that GSK484 significantly reduced neuroinflammatory responses, improved BBB integrity, and enhanced cognitive function. J Neuroinflammation. 2025 Mar 18;22(1):87
ApoE-/- mice Experimental superficial erosion model Systemic administration 4 mg/kg Once daily for 7 days or three times in 7 days To evaluate the effect of GSK484 on NET accumulation and endothelial continuity Cardiovasc Res. 2021 Nov 22;117(13):2652-2663
ApoE−/− mice Hyperlipidemia-associated myocardial ischemia-reperfusion injury model induced by high-cholesterol diet Intraperitoneal injection 4 mg/kg 5 days GSK484 significantly alleviated myocardial ischemia-reperfusion injury in hyperlipidemic mice by inhibiting neutrophil extracellular traps (NETs) release. Adv Sci (Weinh). 2025 Mar;12(11):e2406359
BALB/c nude mice Oesophageal squamous cell carcinoma xenograft model 4 mg/kg/2 days 14 days Evaluate the effect of GSK484 on tumour growth and cisplatin resistance in oesophageal squamous cell carcinoma xenograft models Clin Transl Med. 2025 Mar;15(3):e70272
Mice 4NQO-induced esophageal squamous cell carcinoma model Intraperitoneal injection 4 mg/kg body weight Twice weekly for 4 weeks Evaluate the effect of GSK484 on tumor growth, results showed significant reduction in tumor numbers and sizes J Immunother Cancer. 2024 May 9;12(5):e008662
Mice Type 2 diabetes model Intraperitoneal injection 4 mg/kg Daily for 4 weeks Inhibition of NETosis, reduction of intestinal neutrophil infiltration, and slowing of diabetic retinopathy progression Diabetologia. 2025 Apr;68(4):866-889
Mice D-GalN/LPS-induced acute liver failure model Intraperitoneal injection 20 mg/kg body weight Single dose, 24 hours before ALF induction Significantly attenuated liver necrosis and neutrophil infiltration, reduced ALT and AST levels, and improved survival rate Cell Mol Gastroenterol Hepatol. 2022;14(3):587-607.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.80mL

1.96mL

0.98mL

19.61mL

3.92mL

1.96mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.

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