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-16735

Avoralstat	Inhibitor	98.0%
Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.

HY-148949

Kallikrein 5-IN-2		99.46%
Kallikrein 5-IN-2 (compound 21) is a selective Kallikrein KLK5 inhibitor (pIC₅₀=7.1). KLK5 inhibition may normalise epidermal shedding and reduce the associated inflammation and itching.

HY-P4245

D-Pro-Phe-Arg-Chloromethylketone	Inhibitor	99.51%
D-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation.

HY-P99110

Lanadelumab	Inhibitor	99.74%
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an K_i value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema.

HY-132830

Sebetralstat	Inhibitor	99.58%
Sebetralstat (KVD900) is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases.

HY-W662576

KVD-001	Inhibitor	99.73%
KVD-001 is a potent plasma kallikrein inhibitor. KVD-001 can be used for diabetic macular edema research.

HY-183667

JNJ-pan-AR	Inhibitor
JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC₅₀ of 19 nM and a K_i of 8.4 nM against human wild-type AR. JNJ-pan-AR abolishes androgen-induced KLK2 and KLK3 mRNA expression and reduces androgen-dependent colony formation in prostate cancer cells. JNJ-pan-AR blocks AR nuclear translocation, inhibits PSA protein expression, and represses the growth of AR-dependent tumor cells and ARF877L-driven tumor xenografts. JNJ-pan-AR blocks transactivation and signaling of wild-type AR and various mutant AR variants. JNJ-pan-AR is applicable for research on castration-resistant prostate cancer.

HY-P992250

Anti-KLK7 Antibody
Anti-KLK7 Antibody is a monoclonal antibody targeting KLK7. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-KLK7 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).

HY-109127

Berotralstat	Inhibitor	99.70%
Berotralstat (BCX7353) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.

HY-108814A

Ecallantide TFA	Inhibitor	99.54%
Ecallantide (DX-88) TFA is a specific recombinant plasma kallikrein inhibitor. Ecallantide inhibits the production of bradykinin. Ecallantide may be used to prevent acute attacks of angioedema.

HY-114150D

D-Val-Leu-Arg-pNA acetate		98.89%
D-Val-Leu-Arg-pNA (acetate) is the acetate form of D-Pro-Phe-Arg-p-nitroanilide (pNa). D-Pro-Phe-Arg-p-nitroanilide (pNa) is the substrate for kallikrein and can be used to assay the activity of kallikrein.

HY-123133

PKSI-527	Inhibitor	98.04%
PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system.

HY-122543

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

HY-P0237A

KKI-5 TFA		99.29%
KKI-5 (TFA) is a specific inhibitor of tissue kallikrein. KKI-5 (TFA) can attenuate breast cancer cell invasion.

HY-145568

Feniralstat	Inhibitor	99.12%
Feniralstat (compound 30), 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-109127A

Berotralstat dihydrochloride	Inhibitor	98.67%
Berotralstat dihydrochloride (BCX7353 dihydrochloride) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.

HY-153115

Plasma kallikrein-IN-4	Inhibitor	98.61%
Plasma kallikrein-IN-4 (Example 153) is a plasma kallikrein inhibitor with an IC₅₀ of 0.016 μM against human plasma kallikrein.

HY-126378

LSP-249	Inhibitor	99.05%
LSP-249 (example 35), extracted from patent WO2016011209A1, is a plasma kallikrein inhibitor under the study for angioedema, with an EC₅₀ less than 100 nM in cell.

HY-P4669

LM-030	Inhibitor
LM-030 (BPR277), cyclic depsipeptide, is a potent kallikrein-related peptidase 7 (KLK7) and human neutrophil elastase inhibitor with IC₅₀ values of 1 and 10 nM. LM-030 can be used for the study of Netherton syndrome.

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.

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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):