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The Kallikrein (KLK) Family: Emerging Targets in Oncology

The human kallikrein-related peptidase (KLK) family comprises 15 serine proteases (KLK1–KLK15) that regulate essential physiological networks, including skin desquamation, semen liquefaction, innate immunity, and neural function. Dysregulated expression of these enzymes is a hallmark of various pathologies, most notably prostate cancer.
While KLK3 (PSA) serves as the standard clinical biomarker, family members such as KLK2, KLK4, and KLK14 actively drive tumorigenesis by degrading the extracellular matrix and remodeling the tumor microenvironment. Consequently, these enzymes are increasingly recognized as high-value targets for next-generation diagnostics and therapeutics, paving the way for novel inhibitors (e.g., MDPK67b) and KLK-activated prodrugs.
Biological Functions of Key KLK Molecules
Molecule Key Biological Functions
KLK1 Regulates the kallikrein-kinin system; modulates blood pressure and inflammatory responses.
KLK4, KLK10, KLK11 Regulate epithelial cell dynamics (proliferation, differentiation, apoptosis); involved in carcinogenesis.
KLK6 Implicated in CNS inflammation and neurodegenerative disease progression.
KLK2, KLK3 Established prostate cancer biomarkers and therapeutic targets.
KLK5, KLK6, KLK7, KLK14 Core components of the skin barrier protease network; mediate desquamation and barrier homeostasis; linked to inflammatory dermatoses.
KLK8, KLK9, KLK12, KLK13, KLK15 Play emerging roles in inflammation and tumor progression (mechanisms under investigation).
To accelerate the development of these targeted therapies, we have launched a comprehensive range of high-quality Kallikrein family proteins. This portfolio includes KLK1, KLK2, KLK3, KLK5, KLK7, and KLK11, designed to support robust experimental outcomes.

>>>Explore PSMA – A High-Value Prostate Cancer Target

Key Features & Applications

Product Features

High Purity & Homogeneity: Verified by SDS-PAGE & SEC-MALS/HPLC.

High Enzymatic Activity: Verified by routine QC testing to ensure reliable data.

High Bioactivity: Validated by ELISA.

Lot-to-Lot Consistency: Strict standards ensure stability to support long-term drug development.

Applications

Antibody Development: Immunization, antibody Screening, and functional studies.

Drug Hit-Lead Discovery: Screening of lead compounds and inhibitors.

Assay Development: Utilization of specific cleavage activity for substrate-based detection assays.

Product List

Verification Data

High Purity Verification (SDS-PAGE)
High Purity Verification (SDS-PAGE)

Human Kallikrein 2 Protein, Tag Free (Cat.No. KA2-H5214) on SDS-PAGE under reducing (R) condition. The gel was stained with Coomassie Blue. The purity of the protein is greater than 95% (With Star Ribbon Pre-stained Protein Marker).

High Purity Verification (SDS-PAGE)

Biotinylated Human Kallikrein 3 Protein, His,Avitag (Cat.No. KA3-H82E4)on SDS-PAGE under reducing (R) condition. The gel was stained with Coomassie Blue. The purity of the protein is greater than 90% (With Star Ribbon Pre-stained Protein Marker).

High Purity & Homogeneity Verification (SEC-MALS/HPLC)
High Purity & Homogeneity Verification (SEC-MALS/HPLC)

The purity of Human Kallikrein 3 Protein, His Tag (Cat. No. KL3-H52H3) is more than 95% and the molecular weight of this protein is around 25-40 kDa verified by SEC-MALS.

Protocol

High Purity & Homogeneity Verification (SEC-MALS/HPLC)

The purity of Human Kallikrein 1 (25-262) Protein, His Tag (Cat. No. KL1-H52H4) was greater than 95% as determined by SEC-HPLC.

Protocol

Enzyme Activity Data
Cat. No. Human Kallikrein 2 Protein, Tag Free (active enzyme)
(Cat.No.KA2-H5214) 		Human Kallikrein 2 Protein, His Tag (active enzyme)
(Cat.No.KA2-H52H3)
Substrate Pro-Phe-Arg-7-amido-4-methylcoumarin (PFR-AMC)
Enzyme Activity
（pmol/min/μg） 		>450 >150
Cat. No. Biotinylated Human Kallikrein 3 Protein, His,Avitag™
(active enzyme, MALS verified)
(Cat.No.KA3-H82E4) 		Human Kallikrein 3 Protein, His Tag (Pro-form, MALS verified)
(Cat.No.KL3-H52H3)
Substrate Succinyl-Arg-Pro-Tyr-p-Nitroanilide (SucRPYpNA)
Enzyme Activity
（pmol/min/μg） 		>160 >150
Cat. No. Human Kallikrein 5 Protein, Tag Free (active enzyme)
(Cat.No.KA5-H5213) 		Human Kallikrein 7 Protein, Tag Free (active enzyme)
(Cat.No.KA7-H5213)
Substrate BOC-Val-Pro-Arg-AMC Mca-RPKPVE-Nval-WRK(Dnp)-NH2
Enzyme Activity
（pmol/min/μg） 		>350 ＞150
Binding activity to antibodies has been validated by ELISA
Binding activity to antibodies has been validated by ELISA

Immobilized Human Kallikrein 2 Protein, Tag Free (Cat. No. KA2-H5214) at 1 μg/mL (100 μL/well) can bind Human KLK2 Antibody with a linear range of 0.1-8 ng/mL (Routinely tested).

Protocol

Binding activity to antibodies has been validated by ELISA

Immobilized Human Kallikrein 2 Protein, His Tag (Cat. No. KA2-H52H3) at 1 μg/mL (100 μL/well) can bind Human KLK2 Antibody, IgG with a linear range of 0.06-2 ng/mL (Routinely tested).

Protocol

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  • Background
  • Key Features & Applications
  • Product List
  • Verification Data
  • Related Products