Kallikrein Inhibitor

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

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

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

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.

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

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.

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

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.

PKSI-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 is an irreversible and specific glandular and plasma kallikreins inhibitor.

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).

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.

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 (Example 153) is a plasma kallikrein inhibitor with an IC₅₀ of 0.016 μM against human plasma kallikrein.

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.

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

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.

Eflumenibep alfa is a Kallikrein 5 inhibitor with anti-inflammatory activity. Eflumenibep alfa is a fusion protein that combines human SPINK2 with the human IgG1 Fc fragment at the C-terminus.

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.

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.