2. Signaling Pathways
  3. Immunology/Inflammation
  4. Kallikrein

Kallikrein

KLK; Kallikrein-related peptidase

Kallikrein is a serine protease that plays a crucial role in the kallikrein-kinin system. Plasma kallikrein, specifically expressed in hepatocytes, acts on high molecular weight kininogen to release bradykinin, which is involved in regulating vascular tone, inflammatory response, and endogenous blood coagulation and fibrinolysis. Tissue kallikrein, widely distributed in various tissues such as the lung, kidney, and brain, acts on low molecular weight kininogen to produce kinin, participating in processes like blood pressure regulation, electrolyte balance, and neuronal protection. Additionally, kallikrein can bind to LDLR, promoting its lysosomal degradation, and interact with ASICs to affect neuronal function in the central nervous system. Dysregulation of kallikrein activity is associated with various diseases including heart disease, kidney disease, and cancer[1][2].

Kallikrein Isoform Specific Products:

Kallikrein Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-11090
    DPC423 free base
    		Inhibitor
    DPC423 free base is a selective and orally active factor Xa inhibitor with a Kis of 0.15 (human) and 0.3 (rabbit) nM. DPC423 free base exhibits Kis of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 free base blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 free base can be used for the study of anticoagulation of arterial thrombosis.
    DPC423 free base
  • HY-139787D
    FAM labled Donidalorsen sodium
    FAM labled Donidalorsen sodiumis a FAM labled Donidalorsen sodium (HY-139787A).
    FAM labled Donidalorsen sodium
  • HY-167924
    Ono 3307 free base
    Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsin B leakage from lysosomes in a dose-dependent manner. Ono 3307 Free base is able to target trypsin (Ki=48 nM), thrombin (Ki=0.18 μM), plasma kallikrein (Ki=0.29 μM), plasmin (Ki=0.31 μM), pancreatic kallikrein (Ki=3.6 μM), and chymotrypsin (Ki=47 μM).
    Ono 3307 free base
  • HY-182600
    KLK6-IN-1
    		Inhibitor
    KLK6-IN-1 is a reversible small‑molecule inhibitor of KLK6, KLK1, and plasmin. KLK6-IN-1 shows IC50 values of 1.57 μM (KLK6), 5.1 μM (KLK1), 7.4 μM (plasmin), and Ki values of 0.8 μM (KLK6), 2.4 μM (KLK1), 1.3 μM (plasmin). KLK6-IN-1 is highly selective for KLK6 and its proteolytic network. KLK6-IN-1 induces oligodendrocyte differentiation by promoting oligodendrocyte precursor cell maturation. KLK6-IN-1 can be used for the research of multiple sclerosis.
    KLK6-IN-1
  • HY-19101
    ONO-3307
    		Inhibitor
    ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases.
    ONO-3307
  • HY-163464
    Plasma kallikrein-IN-5
    		Inhibitor
    Plasma kallikrein-IN-5 (Compound 20) is a potent covalent inhibitor of plasma potassium kinin peptide (Pka) with IC50 values of 66 nM and 70 pM at 1 minute and 24 hours, respectively. Plasma kallikrein-IN-5 can be used IN the study of hereditary angioedema (HAE).
    Plasma kallikrein-IN-5
  • HY-N16719
    Picrasidine J
    		Inhibitor
    Picrasidine J is a selective inhibitor targeting the KLK-10 protease and the ERK signaling pathway. Picrasidine J inhibits epithelial-mesenchymal transition (EMT) by upregulating E-Cadherin and ZO-1 and downregulating β-catenin and Snail, while simultaneously reducing KLK-10 expression and inhibiting ERK phosphorylation, thereby exhibiting significant anti-migratory and anti-invasive activity. Picrasidine J can inhibit the metastasis of head and neck squamous cell carcinoma (HNSCC) and is primarily used in anti-metastasis research for head and neck tumors.
    Picrasidine J
  • HY-139787
    Donidalorsen
    		Inhibitor
    Donidalorsen (ISIS-721744; IONIS-PKK-LRX free acid) is an antisense oligonucleotide targeting prekallikrein (PKK). Donidalorsen inhibits kallikrein activity and reduces the production of Bradykinin (HY-P0206) by specifically binding to and degrading PKK mRNA in the liver. Donidalorsen can be used in the research of hereditary angioedema.
    Donidalorsen
  • HY-126809
    Bz-Pro-Phe-Arg-pNA
    		Substrate
    Bz-Pro-Phe-Arg-pNA (Bz-PFR-pNA) is a chromogenic peptide substrate for plasma and glandular Kallikrein, cysteine proteinase (Cruzipain) and Trypsin. Bz-Pro-Phe-Arg-pNA can be used in Factor XII assay.
    Bz-Pro-Phe-Arg-pNA
  • HY-P5027
    Cbz-Lys-Arg-pNA
    		Substrate
    Cbz-Lys-Arg-pNA is a peptide substrate containing pNA as the chromogenic group. Cbz-Lys-Arg-pNA is widely used in enzymatic analysis, including thrombin, plasmin, factor Xa and Kallikrein.
    Cbz-Lys-Arg-pNA
  • HY-124714
    DKFZ-251
    		Inhibitor
    DKFZ-251 is a kininogenase-related peptidase KLK6 inhibitor (IC50=0.47 μM), and also exhibits certain inhibitory activity against KLK5 and KLK7 (IC50 values are 1.1 nM and 73 nM, respectively). DKFZ-251 transiently acylates the catalytic serine of KLK6 to form a long-lived acyl-enzyme complex that inhibits enzyme function. DKFZ-251 is a phenotypic modulator that alters cell proliferation capacity and regulates epithelial-mesenchymal transition (EMT). DKFZ-251 can be used in research related to head and neck cancer.
    DKFZ-251
  • HY-P0237
    KKI-5
    KKI-5 is a specific inhibitor of tissue kallikrein. KKI-5 can attenuate breast cancer cell invasion.
    KKI-5
Cat. No. Product Name / Synonyms Application Reactivity
Kallikrein Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.