PIK-93是第一個報道的PI 4-激酶抑制劑，能夠在低納摩爾范圍內抑制PI 4 KIII 2（IC 50 =19 nM）。此外，該化合物在體外是PI 3 K β 3的有效抑制劑（IC 50 =16 nM）。該化合物抑制p110 β ± p110 β 2 p110 β ′，IC 50分別為0.039 0.59 0.12 μM。PIK-93與Val 882的骨架酰胺和羰基以及其磺酰胺和Asp 964之間形成氫鍵。PI 4KIII 2對許多惡性瘧原蟲病毒的復制至關重要。抑制瘧原蟲的PI 4KIIIII 2被認為是一種抗瘧疾的治療方法。參考資料由Bioz提供技術支持更多詳情請訪問BiozJ. E. Burke et al.“Structures of PI4KIIIb complex show simultaneous recruitment of Rab11 and its effectors”Science 344 1035（2014）; DOI：10.1126/science.1253397
產品描述
PIK-93 is the first reported PI4-kinase inhibitor which is able to inhibit PI4KIII?2 at low-nanomolar range (IC50=19 nM). In addition this compound is a potent inhibitor of PI3K?3 in vitro (IC50=16 nM). This compound inhibits p110?± p110?2 p110?′ with IC50's of 0.039 0.59 0.12 ?μM respectively. PIK-93 hydrogen bonds to the backbone amide and carbonyl of Val882 and between its sulphonamide and Asp964. PI4KIII?2 is essential for replication of numerous viruses P. falciparum. Inhibition of plasmodial PI4KIII?2 has been proposed as an anti-malaria treatment.References Powered by Bioz See more details on BiozJ.E. Burke et al. "Structures of PI4KIIIb complexes show simultaneous recruitment of Rab11 and its effectors" Science 344 1035 (2014); DOI: 10.1126/science.1253397
