plasma kallikrein-in-1

Plasma kallikrein-IN-1 is a PKK inhibitor with an IC50 value of 0.5 nM.

Lanadelumab (SHP643) is a humanized IgG1 monoclonal antibody targeting plasma kallikrein (pKal) with a Ki value of 0.12 nM. Lanadelumab effectively inhibits both free pKal and its interaction with high molecular weight kininogen (HMWK)-bound pKal. Lanadelumab has demonstrated potential in hereditary angioedema research and represents a promising therapeutic antibody for studying kallikrein-kinin system regulation.

Berotralstat (BCX7353) is a second-generation, synthetic, and orally active plasma kallikrein inhibitor with low toxicity. It is highly specific and effectively used in the research of hereditary angioedema (HAE) attacks. Berotralstat functions by inhibiting the enzymatic activity of plasma kallikrein, which is responsible for the release of bradykinin. This blocking mechanism targets the major biologic peptide involved in the promotion of swelling and pain associated with HAE attacks[1][2].

Plasma kallikrein-IN-3, a potent inhibitor ( IC 50 : 0.15 μM) of plasma kallikrein, finds application in research related to hereditary angioedema, diabetic macular edema, and diabetic retinopathy [1].

Kallikrein is capable of forming the kallikrenase kalinin system (KKS) in plasma and tissues, producing bradykinin and kalin peptides , respectively [1] .

D-Pro-Phe-Arg-Chloromethylketone, an inhibitor of coagulation factor XII and plasma kallikrein, is significant in the regulation of thrombosis and inflammation [1].