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].

References:

[1]. Raspi G. Kallikrein and kallikrein-like proteinases: purification and determination by chromatographic and electrophoretic methods. J Chromatogr B Biomed Appl. 1996 Sep 20;684(1-2):265-87. [Content Brief]

[2]. Yousef GM, et al. The new human tissue kallikrein gene family: structure, function, and association to disease. Endocr Rev. 2001 Apr;22(2):184-204. [Content Brief]

Kallikrein Isoform Specific Products:

Kallikrein Isoform Comparison

Kallikrein Related Products (52)
Antibodies (4)
Kallikrein Isoform Comparison

By Effects:	Inhibitors (42) Substrates (2)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-148949A

Kallikrein 5-IN-2 TFA	Inhibitor	99.53%
Kallikrein 5-IN-2 TFA is the TFA salt form of Kallikrein 5-IN-2 (HY-148949). Kallikrein 5-IN-2 TFA is a selective inhibitor for kallikrein 5 (KLK5) with pIC₅₀ of 7.1. Kallikrein 5-IN-2 TFA is non-phototoxic (100 μg/mL) and non-irritant. Kallikrein 5-IN-2 is stable at pH 4-pH 8 under non-oxidative condition. Kallikrein 5-IN-2 is potent in ameliorating the Netherton syndrome.

HY-139787A

Donidalorsen sodium	Inhibitor
Donidalorsen (ISIS-721744; IONIS-PKK-LRX) sodium is an antisense oligonucleotide targeting prekallikrein (PKK). Donidalorsen sodium inhibits kallikrein activity and reduces the production of Bradykinin (HY-P0206) by specifically binding to and degrading PKK mRNA in the liver. Donidalorsen sodium can be used in the research of hereditary angioedema.

HY-P990459

Anti-KLK5/Kallikrein 5 Antibody	Inhibitor	98.49%
Anti-KLK5/Kallikrein 5 Antibody is a CHO-expressed human antibody that targets KLK5/Kallikrein 5. The Anti-KLK5/Kallikrein 5 Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for the Anti-KLK5/Kallikrein 5 Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).

HY-139888

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

HY-117478

FE-999024	Inhibitor
FE-999024 (CH-2856) is a specific tissue kallikrein inhibitor. FE-999024 can inhibit cancer cells invasion with a maximum of 39%. FE-999024 can reduce eosinophilia in a model of allergic inflammation. FE-999024 can be used for the researches of cancer, inflammation and immunology.

HY-139787C

Donidalorsen sodium scrambled negative control	Inhibitor
Donidalorsen sodium scrambled negative control is the sequence scrambled negative control of Donidalorsen sodium (HY-139787A).

HY-124610

DKFZ-633	Inhibitor
DKFZ-633 is a potent KLK6 inhibitor and KLK6-specific probe with an IC₅₀ of 250 nM against human KLK6. DKFZ-633 covalently labels active KLK6 in a specific manner, and successfully pulls down and captures endogenous active KLK6 from cell-conditioned media. DKFZ-633 serves as a critical tool for investigating the function of KLK6 and its regulatory mechanisms in head and neck cancer.

HY-181798

pKal-IN-1	Inhibitor
pKal-IN-1 (compound 13) is a plasma kallikrein (pKal) inhibitor. pKal-IN-1 can be used for the research of diabetic macular edema, diabetic retinopathy.

HY-11090A

DPC423	Inhibitor
DPC423 is a selective and orally active factor Xa inhibitor with a K_is of 0.15 (human) and 0.3 (rabbit) nM. DPC423 exhibits K_is of 60, 61 and 6000 nM against human trypsin, plasma kallikrein and thrombin. DPC423 blocks the formation of prothrombinase complex, reduces thrombin production, inhibits fibrin formation and platelet activation. DPC423 can be used for the study of anticoagulation of arterial thrombosis.

HY-108814

Ecallantide	Inhibitor
Ecallantide (DX-88) is a specific plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide can be used to prevent acute attacks of angioedema.

HY-122543A

PPACK II	Inhibitor
PPACK II is an irreversible and specific glandular and plasma kallikreins inhibitor.

HY-150085

GSK951	Inhibitor
GSK951 is a potent and selective Kallikrein-5 (KLK5) inhibitor amenable to epidermal delivery. GSK951 shows an IC₅₀ of 250 pM for KLK5 and greater than 100-fold selectivity over KLK7 and KLK14. GSK951 can reduce transepidermal water loss, and decrease proinflammatory cytokine expression. GSK951 can be used for the researches of inflammation and immunology, such as Netherton syndrome.

HY-177652A

Onvuzosiran sodium	Inhibitor
Onvuzosiran sodium, a siRNA, is a prekallikrein synthesis reducer.

HY-145568A

Feniralstat hydrochloride	Inhibitor
Feniralstat (compound 30) hydrochloride, a pyrazole derivative, is a potent kallikrein inhibitor with an IC₅₀ of 6.7 nM for Human plasma kallikrein (pKal). Feniralstat has no inhibition on Human KLKl, Human FXIa, Human Factor Xlla (all IC₅₀>40 μM).

HY-177652

Onvuzosiran	Inhibitor
Onvuzosiran, a siRNA, is a prekallikrein synthesis reducer.

HY-150519

FXIa/Plasma kallikrein-IN-1	Inhibitor
FXIa/Plasma kallikrein-IN-1 is an inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein with K_i values of 187.70 nM and 151.6 nM, respectively. FXIa/Plasma kallikrein-IN-1 can be used in the research of thromboembolic diseases.

HY-139787E

Cy3 labled Donidalorsen sodium
Cy3 labled Donidalorsen sodium is a Cy3 labled Donidalorsen sodium (HY-139787A).

HY-177652B

Onvuzosiran sodium scrambled negative control	Inhibitor
Onvuzosiran sodium scrambled negative control is the sequence scrambled negative control of Onvuzosiran sodium.

HY-143476

Plasma kallikrein-IN-2	Inhibitor
Plasma kallikrein-IN-2 (Compound 198) is a potent plasma kallikrein (PKal) inhibitor with an IC₅₀ of 0.1 nM. Plasma kallikrein-IN-2 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research.

HY-150052

Plasma kallikrein-IN-3	Inhibitor
Plasma kallikrein-IN-3 is a plasma kallikrein inhibitor (IC₅₀: 0.15 μM). Plasma kallikrein-IN-3 can be used for hereditary angioedema, diabetic macular edema, and diabetic retinopathy research.

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Kallikrein

Kallikrein Isoform Specific Products:

Kallikrein Isoform Specific Products:

Kallikrein Related Products (52)

Antibodies (4)

Kallikrein Isoform Comparison

Kallikrein Related Products (52):