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GSK199

GSK199 1549811-53-1
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产品信息
产品名称:GSK199 纯度:98% min
CAS NO:1549811-53-1 溶解度:
分子式:C24H29ClN6O2 包装:可按客户要求包装
分子量:468.97 贮存:-20 ℃
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备注说明

Protein arginine deiminase 4 (PAD4) mediates the transformation of protein arginine into citrulline. Citrullination of proteins has normal roles in gene regulation and pathological roles in immunological and inflammatory diseases. GSK199 is a reversible inhibitor of PAD4 (IC50 = 200 nM) that binds to the low-calcium form of the enzyme and is selective for PAD4 over PAD1-3.It is less potent than the related PAD4 inhibitor GSK484 , which demonstrates an IC50 value of 50 nM. GSK199 can inhibit the citrullination of PAD4 target proteins and diminish the formation of neutrophil extracellular traps in mouse neutrophils.



参考文献
1: Willis VC, Banda NK, Cordova KN, Chandra PE, Robinson WH, Cooper DC, Lugo D, Mehta G, Taylor S, Tak PP, Prinjha RK, Lewis HD, Holers VM. Protein arginine deiminase 4 inhibition is sufficient for the amelioration of collagen-induced arthritis. Clin Exp Immunol. 2017 May;188(2):263-274. doi: 10.1111/cei.12932. Epub 2017 Mar 9. PubMed PMID: 28128853; PubMed Central PMCID: PMC5383440.

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