PPACKII (trifluoroacetate salt)

- Overview
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    Background
    
    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.
- Properties
  - Alternative Name
    
    H-D-Phe-Phe-Arg-Chloromethyl Ketone; D-phenylalanyl-N-[(1S)-4-[(aminoiminomethyl)amino]-1-(chloroacetyl)butyl]-L-phenylalaninamide, bis(trifluoroacetate)
    
    CAS Number
    
    649748-23-2
    
    Molecular Formula
    
    C25H33ClN6O3·2CF3COOH
    
    Molecular Weight
    
    729.1
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥95.00%
    
    Solubility
    
    ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

PPACKII (trifluoroacetate salt)

Background

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