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CAS No.: 1652591-81-5

GSK484 HCl Catalog No. CSN21368

Synonyms: GSK484 hydrochloride

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.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述PAD4 (Peptidyl arginine deiminase 4) is an enzyme that plays an important role in gene expression through catalyzing citrullination of arginine residues. Binding to calcium can promote the bioactive conformation and greatly increase its activity. GSK484 is a potent and reversible PAD4 inhibitor with IC50 value of 50nM. Pretreatment with 10 μM GSK484 could markedly diminish ionomycin-induced citrullination and formation of neutrophil extracellular trap in mouse neutrophils. Administration of GSK484 at dose of 4mg/kg daily for one week improved perfusion and suppressed renal inflammation in kidneys from tumor-bearing MMTV-PyMT mice, as suppression of the elevated number of neutrophils undergoing NETosis in peripheral blood, tumor-induced elevated expression of IL-1ß and IL-6, pro-inflammatory cytokines, the adhesion molecules ICAM-1 and VCAM-1, as well as normalization of podocyte foot processes in the kidneys could be observed. Inhibition of PAD4 through GSK484 could abrogate thrombus formation but not thrombocytopenia in a heparin-induced thrombocytopenia/thrombosis model.
动物研究
剂量
Mice: 4 mg/kg^[1] (i.p.), 40 mg/kg^[2] (i.p.)

给药途径
i.p.

动物研究
剂量	Mice: 4 mg/kg^[1] (i.p.), 40 mg/kg^[2] (i.p.)
给药途径	i.p.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9607 mL
- 9.8034 mL
- 19.6068 mL
- 5 mM
- 0.3921 mL
- 1.9607 mL
- 3.9214 mL
- 10 mM
- 0.1961 mL
- 0.9803 mL
- 1.9607 mL

技术信息

CAS号

1652591-81-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H32ClN5O3

运输

蓝冰

分子量

510.03

别名

GSK484 hydrochloride

溶解度

DMSO	320.0 mg/mL (627.4 mM)
Water	165.0 mg/mL (323.5 mM)

动物实验配方

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