649748-23-2 Usage
Uses
Potent and specific irreversible inhibitor of plasma and glandular kallikreins.
Biological Activity
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].
references
[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.
Check Digit Verification of cas no
The CAS Registry Mumber 649748-23-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 6,4,9,7,4 and 8 respectively; the second part has 2 digits, 2 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 649748-23:
(8*6)+(7*4)+(6*9)+(5*7)+(4*4)+(3*8)+(2*2)+(1*3)=212
212 % 10 = 2
So 649748-23-2 is a valid CAS Registry Number.
649748-23-2Relevant articles and documents
Targeted delivery of paclitaxel to tumor cells: Synthesis and in vitro evaluation
Ndungu, John M.,Lu, Yang J.,Zhu, Shijun,Yang, Chao,Wang, Xu,Chen, Georgia,Shin, Dong M.,Snyder, James P.,Shoji, Mamoru,Sun, Aiming
experimental part, p. 3127 - 3132 (2010/11/24)
We previously reported a novel drug delivery system, drug-linker-Phe-Phe- Arg-methylketone (FFR-mk)-factor VIIa (fVIIa). The method utilizes tissue factor (TF), which is aberrantly and abundantly expressed on many cancer cells. The advantage of this delivery system is its ability to furnish a potent anticancer drug specifically to the tumor vasculature and cancer cells. In this paper, we describe the synthesis of paclitaxel (PTX)-Phe-Phe-Arg-chloromethyl ketone (FFR-ck), followed by coupling with fVIIa to form PTX-FFR-mk-fVIIa. FFRck was separately linked to the OH groups at the C2′ or C7 positions of PTX (C2′- or C7-PTX-FFRck), the C2′ analogue exhibiting better activity against human head and neck squamous KB 3-1 cells. The activity order against PTX-sensitive KB 3-1 cells is C2′-PTX-FFRmk-fVIIa > PTX > C2′-PTX-FFRck. The C2′ complex shows an IC50 of 12 nM against the PTX-sensitive cell line and 130 nM against PTX-resistant cells.
