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PPACKII (trifluoroacetate salt) Sale

(Synonyms: H-D-Phe-Phe-Arg-Chloromethyl Ketone) 目录号 : GC17711

An irreversible inhibitor of kallikreins

PPACKII (trifluoroacetate salt) Chemical Structure

Cas No.:649748-23-2

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1mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

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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.

Chemical Properties

Cas No. 649748-23-2 SDF
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 SMILES O=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 C25H33ClN6O3 • 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°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.3716 mL 6.8578 mL 13.7155 mL
5 mM 0.2743 mL 1.3716 mL 2.7431 mL
10 mM 0.1372 mL 0.6858 mL 1.3716 mL
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