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
All Product Categories
-
Kallikrein Related Products (63)
Related Products (63)
-
Antibodies (4)
-
Kallikrein Isoform Comparison
-
Avoralstat
0 ImagesCat. No.: HY-16735CAS No.: 918407-35-9Synonyms: BCX4161Avoralstat (BCX4161), a potent and orally active plasma kallikrein (PKK) inhibitor, is used for hereditary angioedema research.
-
Kallikrein 5-IN-2
0 ImagesKallikrein 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.
-
Pro-Phe-Arg-AMC acetate
0 ImagesPro-Phe-Arg-AMC acetate is a substrate for human glandular kallikrein 2. Pro-Phe-Arg-AMC acetate can be used for the quantitative detection of enzyme activity.
-
Sebetralstat
0 ImagesSynonyms: KVD900Sebetralstat (KVD900) is an orally active and selective plasma kallikrein inhibitor, with an IC50 of 6.0 nM and a Ki of 3.0 nM against the human target. Sebetralstat binds to the active site of plasma kallikrein, inducing a conformational flip of Trp215 to form a U-shaped conformation; its P1 group interacts with the S1 pocket through hydrophobic interactions and displacement of high-energy water molecules, independent of the Asp189 ionic bond. Sebetralstat inhibits plasma kallikrein-kinin system activation in whole plasma, rapidly relieves laryngeal and abdominal attack symptoms of hereditary angioedema (HAE-C1INH), and reduces attack severity. Sebetralstat can be used in research related to hereditary angioedema (HAE).
-
D-Pro-Phe-Arg-Chloromethylketone
0 ImagesD-Pro-Phe-Arg-Chloromethylketone, a inhibitor of coagulation factor XII and plasma kallikrein, plays an important role in thrombosis and inflammation.
-
XYD113
0 ImagesCat. No.: HY-184896CAS No.: 3032314-99-8XYD113 is an orally active, selective GSPT1 Molecular glue degrader. XYD113 promotes the formation of the CRBN-GSPT1 ternary complex and mediates GSPT1 degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. XYD113 downregulates genes associated with the occurrence and progression of prostate cancer (c-Myc, AR, AR-V7, KLK3, KLK2, TMPRSS2). XYD113 exhibits anticancer activity against prostate cancer. XYD113 can be used in the research of prostate cancer.
-
JNJ-pan-AR
0 ImagesCat. No.: HY-183667CAS No.: 1332390-06-3JNJ-pan-AR is an orally active androgen receptor (AR) inhibitor with an IC50 of 19 nM and a Ki 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.
-
Lanadelumab
0 ImagesSynonyms: SHP643; DX-2930; X124-G01Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki 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.
-
Berotralstat
0 ImagesSynonyms: BCX7353Berotralstat (BCX7353) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.
-
Pro-Phe-Arg-AMC
0 ImagesPro-Phe-Arg-AMC is a substrate for human glandular kallikrein 2. Pro-Phe-Arg-AMC can be used for the quantitative detection of enzyme activity.
-
Ecallantide TFA
0 ImagesCat. No.: HY-108814APurity: 99.54%Synonyms: DX-88 TFAEcallantide (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.
-
D-Val-Leu-Arg-pNA acetate
0 ImagesD-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.
-
PKSI-527
0 ImagesPKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system.
-
PPACK II diTFA
0 ImagesCat. No.: HY-122543CAS No.: 649748-23-2PPACK II diTFA is an irreversible and specific glandular and plasma kallikreins inhibitor.
-
KKI-5 TFA
0 ImagesCat. No.: HY-P0237APurity: 99.29%KKI-5 (TFA) is a specific inhibitor of tissue kallikrein. KKI-5 (TFA) can attenuate breast cancer cell invasion.
-
Feniralstat
0 ImagesSynonyms: KVD-824Feniralstat (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).
-
Berotralstat dihydrochloride
0 ImagesSynonyms: BCX7353 dihydrochlorideBerotralstat dihydrochloride (BCX7353 dihydrochloride) is an orally active plasma kallikrein inhibitor. Berotralstat can reduce brain edema and is being studied for glioblastoma and hereditary angioedema.
-
Kallikrein 5-IN-2 TFA
0 ImagesCat. No.: HY-148949APurity: 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.
-
Plasma kallikrein-IN-4
0 ImagesPlasma kallikrein-IN-4 (Example 153) is a plasma kallikrein inhibitor with an IC50 of 0.016 μM against human plasma kallikrein.
-
LSP-249
0 ImagesLSP-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.
