649748-23-2

Potent and specific irreversible inhibitor of plasma and glandular kallikreins.

ppackii is a specific and irreversible inhibitor of glandular and plasma kallikreins [1].human tissue kallikreins (hks) are a class of secreted serine proteases that involved in the release of vasodepressor peptides or kinins from a plasma substrate. kallikrein has diverse expression patterns and physiological roles. kallikrein has been primarily known as cancer biomarkers. kallikrein has been implicated in many cancer-related processes, such as cell-growth regulation, angiogenesis, invasion and metastasis. kallikrein could promote or inhibit neoplastic progression individually and/or with the interaction in cascades with other hks and proteases [2].ppackii prevented apolipoprotein proteolysis in dextran sulfate-precipitated human plasma ldl and inhibited serum atrial natriuretic peptide cleavage at micromolar concentrations [1]. it has been reported that ppackii inactivated the amidolytic activity of native human hageman factor (factor xii) at 5.3 μm [3].

[1]. byrne r e, scanu a m. apolipoprotein b-100 of plasma low density lipoproteins undergoes proteolysis by contact activation factors when plasma is treated with dextran sulfate-500-mgcl2[j]. journal of lipid research, 1989, 30(1): 109-120.
[2]. borgoo c a, diamandis e p. the emerging roles of human tissue kallikreins in cancer[j]. nature reviews cancer, 2004, 4(11): 876-890.
[3]. silverberg m, kaplan a p. enzymatic activities of activated and zymogen forms of human hageman factor (factor xii)[j]. blood, 1982, 60(1): 64-70.