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.
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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]. |
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]. |
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 |
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 |