tryptase

Benzamidine hydrochloride (Benzamidine HCl) is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Ki of 35, 350, and 220 μM, respectively).

R112 is an ATP-competitive inhibitor of Syk kinase. Ki=6 nM,IC50=226 nM.

Alkaline tryptase-IN-1 (compound H-13) is an insecticide that targets alkaline trypsin-like enzymes. It has lethal concentration (LC50) values of 8.72, 13.77, 14.17, 12.96, and 12.35 μg/mL against Schizaphis graminum, Sitobion avenae, Brevicoryne brassicae, Aphis gossypii, Aphis spiraecola, and Myzus persicae, respectively.

FD-IN-1 is a factor D (FD) inhibitor with an IC50 of 12 nM.FD-IN-1 also inhibits factor XIa (FXIa) and Tryptase β2 with IC50s of 7.7 and 6.5μM, respectively. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system.

APC 366 is a selective tryptase inhibitor (Ki = 7.1 μM). Tryptase is a serine protease released during mast cell degranulation, which reduces acute airway responses to allergens and can be used for asthma allergy treatment.

BMS-262084 is a potent selective β-lactam trypsin inhibitor with therapeutic potential in the treatment of asthma.

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, exhibiting a Ki of 620 pM for recombinant human tryptase-β (rHTβ)[1][2].

CRA-2059 is a highly specific and selective tryptase inhibitor with a Ki of 620 pM for recombinant human tryptase-β (rHTβ) [1][2].

APC-6860 is a trypsin-like serine protease inhibitor with \( k_i \) values of 0.21, 0.44, 1.5, 16.8, 20, and 30 μM for uPA, trypsin, tryptase, tPA, thrombin, and factor Xa, respectively. It exhibits a selectivity ratio for tPA versus uPA of 80 and has \( k_i \) values of 0.1 and 0.082 μM for human and murine urokinases, respectively. APC-6860 can be utilized for cancer research.

APC 366 (TFA) is a potent irreversible inhibitor of mast cell tryptase. It is particularly useful in studies related to allergic diseases.

CRA-2059 is a selective and reversible inhibitor of human tryptase beta, exhibiting a Ki value of 620 pM against recombinant human tryptase beta (rHTβ).

RWJ 58643 is a reversible beta-tryptase and trypsin inhibitor. Low-dose RWJ-58643 (100 microg) and budesonide (200 microg) significantly reduced symptoms, eosinophils and levels of IL-5 following NAC. However, higher doses of RWJ-58643 (300 and 600 microg) caused a late eosinophilia and preceding increases in IL-5 compared with placebo.

APC-366 is a selective inhibitor of the mast cell tryptase that inhibits tryptase-induced histamine release from human tonsil and lung cells.

DB03417 is a compound listed in web page: https://go.drugbank.com/drugs/DB03417. DB03417 is a potential tryptase inhibitor.

Benzenecarboximidamide, hydrochloride, hydrate (1:1:x) (Benzamidine hydrochloride hydrate) is a reversible competitive trypsin-like serine proteases inhibitor with K i s of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa , Thrombin and tPA, respectively [1] [2] .