Serine Protease
In human, serine proteases exert their activities at various cellular levels and are responsible for the coordination of many physiological functions including digestion, cell cycle, coagulation, immunity, and reproduction. Furthermore, serine proteases are key elements of the inflammation response due to their release from activated leukocytes and mast cells or generation through the coagulation cascade. The dysregulation of serine proteases is thus involved in a wide range of pathologies: thrombin and plasmin in coagulopathies and bleeding disorders, granzymes and neutrophil elastases (NEs) in immune deficiencies, and plasma kallikreins levels in blood pressure disorders like angioedema. In the epidermis, serine proteases, including some kallikrein-related peptidases that we will detail hereafter and matriptase, are involved in various skin disorders. Serine proteases which possess similar structures and catalytic properties are grouped into clans. The four main clans are clan PA represented by chymotrypsin, clan SB by subtilisin, and clans SC and SF which encompass various proteases.
References
1.Soualmia F, El Amri C. Expert Opin Ther Pat. 2018;28(2):93–110.
References
1.Soualmia F, El Amri C. Expert Opin Ther Pat. 2018;28(2):93–110.
Proteasome/Ubiquitin
Serine Protease
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Patamostat HCl
catalog no : M37650
cas no: 3031765-17-7
Patamostat HCl is a highly potent and selective small molecule protease (protease) inhibitor that inhibits trypsin, fibrinolytic enzymes, and thrombin with IC50 values of 39 nM, 950 nM, and 1.9 μM, respectively. -
TS-24
catalog no : M37553
cas no: 1563260-97-8
TS-24 is an inhibitor of the cysteine protease histatin S (CTSS).TS-24 promotes BRCA1-mediated apoptosis and shows radiosensitization in a TNBC xenograft mouse model. -
TR-107
catalog no : M37552
cas no: 2485052-87-5
TR-107 (Anticancer agent 230) is a selective and potent activator of the mitochondrial protease ClpP that inhibits tumor growth in the MDA-MB-231 xenograft model. -
SLK/STK10-IN-1
catalog no : M35494
cas no: 264210-49-3
SLK/STK10-IN-1 is a selective and potent inhibitor of SLK and STK10 with potential antitumor activity. -
4-Aminobenzamidine dihydrochloride
catalog no : M35392
cas no: 2498-50-2
4-Aminobenzamidine dihydrochloride (p-Aminobenzamidine dihydrochloride) is a strong trypsin inhibitor and a relatively weak inhibitor of urokinase type plasminogen activator (uPA) (K i =82 μM).