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GSK484 HCl {[allProObj[0].p_purity_real_show]}

货号:A268467 同义名: GSK484 (hydrochloride);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.

GSK484 HCl 化学结构 CAS号:1652591-81-5
GSK484 HCl 化学结构
CAS号:1652591-81-5
GSK484 HCl 3D分子结构
CAS号:1652591-81-5
GSK484 HCl 化学结构 CAS号:1652591-81-5
GSK484 HCl 3D分子结构 CAS号:1652591-81-5
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GSK484 HCl 纯度/质量文件 产品仅供科研

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GSK484 HCl 生物活性

描述 GSK484 HCl exhibits strong affinity for PAD4 in its low-calcium state, with IC50s of 50 nM without calcium and 250 nM with 2 mM calcium. It also concentration-dependently inhibits PAD4's citrullination of the BAEE substrate in the presence of 0.2 mM calcium, as shown by an ammonia release assay[1].

GSK484 HCl 动物研究

Animal study In a study to determine if PAD4 inhibition could mitigate cancer-related kidney damage, MMTV-PyMT mice received daily treatments of GSK484 HCl at 4 mg/kg for a week. This treatment reduced the number of neutrophils undergoing NETosis in the blood of cancerous mice and significantly lowered the total protein in their urine, indicating improved kidney health. The same dosage of GSK484 HCl reversed kidney dysfunction indicators in tumor-bearing mice as effectively as DNase I treatment, with no observed toxicity[2].

GSK484 HCl 参考文献

[1]Lewis HD, et al. Inhibition of PAD4 activity is sufficient to disrupt mouse and human NET formation. Nat Chem Biol. 2015 Mar;11(3):189-91.

[2]Cedervall J, et al. Pharmacological targeting of peptidylarginine deiminase 4 prevents cancer-associated kidney injury in mice. Oncoimmunology. 2017 Apr 20;6(8):e1320009.

GSK484 HCl 实验方案

计算器
存储液制备 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

GSK484 HCl 技术信息

CAS号1652591-81-5
分子式C27H32ClN5O3
分子量 510.028
别名 GSK484 (hydrochloride);GSK484 hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 120 mg/mL(235.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(98.03 mM),配合低频超声助溶

动物实验配方
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