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PPACKII(trifluoroacetate salt)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PPACKII(trifluoroacetate salt)图片
CAS NO:649748-23-2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
glandular and plasma kallikreins inhibitor
Cas No.649748-23-2
别名H-D-Phe-Phe-Arg-Chloromethyl Ketone
化学名D-phenylalanyl-N-[(1S)-4-[(aminoiminomethyl)amino]-1-(chloroacetyl)butyl]-L-phenylalaninamide,bis(trifluoroacetate)
Canonical SMILESO=C([C@@H](CC1=CC=CC=C1)N)N[C@@H](CC2=CC=CC=C2)C(N[C@H](C(CCl)=O)CCCNC(N)=N)=O.FC(F)(C(O)=O)F.FC(F)(C(O)=O)F
分子式C25H33ClN6O3o 2CF3COOH
分子量729.1
溶解度≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.