71142-71-7
Chemical Structure
PPACK
- CAS No.: 71142-71-7
- Formula:C21H31ClN6O3
- Molecular Weight:450.96
IUPAC Name: (S)-1-(D-phenylalanyl)-N-((S)-1-chloro-6-guanidino-2-oxohexan-3-yl)pyrrolidine-2-carboxamide
InChIKey: KWPACVJPAFGBEQ-IKGGRYGDSA-N
SMILES: O=C(N1[C@@H](CCC1)C(N[C@@H](CCCNC(N)=N)C(CCl)=O)=O)[C@@H](CC2=CC=CC=C2)N
Biological Activity:
PPACK is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases[1][2][3][4].
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PPACK | PPACK is a potent, peptidic inhibitor targeting thrombin and granzyme GZMK. PPACK specifically blocks the activities of thrombin and GZMK, thereby inhibiting thrombin-mediated PAR-1 cleavage, as well as downstream inflammatory and procoagulant signaling pathways. Through stabilizing IκB proteins, blocking NF-κB activation and reducing systemic levels of proinflammatory/procoagulant biomarkers, PPACK exerts multiple effects including anti-inflammatory, antithrombotic, barrier repair, and inhibition of atherosclerotic plaque progression. PPACK binds to platelets without interference from kininogen, effectively limiting acute thrombus growth and reducing eosinophil infiltration and goblet cell hyperplasia in asthma models. PPACK is an important tool molecule for investigating the mechanisms of atherosclerosis, asthma and related thromboinflammatory diseases. |
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- [1]. Palekar RU, et al. Inhibition of Thrombin With PPACK-Nanoparticles Restores Disrupted Endothelial Barriers and Attenuates Thrombotic Risk in Experimental Atherosclerosis. Arterioscler Thromb Vasc Biol. 2016;36(3):446-455. [Content Brief]
- [2]. Wu Y, et al. The inhibitory effect of antiplatelet drugs on spontaneous platelet aggregation on glass surfaces: an analysis based on microscopic three-dimensional topography. J Thromb Thrombolysis. Published online September 9, 2025. [Content Brief]
- [3]. Lan F, et al. GZMK-expressing CD8+ T cells promote recurrent airway inflammatory diseases. Nature. 2025;638(8050):490-498. [Content Brief]
- [4]. Schmaier AH, et al. PPACK-thrombin is a noncompetitive inhibitor of alpha-thrombin binding to human platelets. Thromb Res. 1992;67(5):479-489. [Content Brief]
Keywords
