VHR-IN-3 (Compound 1) is a selective vaccinia H1-related (VHR) phosphatase inhibitor with a Ki of 0.81 μM. VHR-IN-3 mimics the phosphate group through the sulfonic acid group and competitively binds to the catalytic active center of VHR. VHR-IN-3 can be used for the research of cervical cancer.

SM-122 is a monovalent Smac mimetic targeting cellular inhibitor of apoptosis protein (cIAP)-1/2. SM-122 can induce cIAP-1/2 degradation and weakly induce apoptosis in tumor cells. SM-122 can be used for the research of cancer, such as breast cancer.

PI3Kα-IN-28 (Compound 23) is an efficient dual targeted PI3K/BRD4 inhibitor. PI3Kα-IN-28 can inhibit the proliferation of various cells, such as KYSE180 and KYSE450 cells. PI3Kα-IN-28 can concentration dependently inhibit migration and colony formation, induce G0/G1 phase arrest, significantly inhibit DNA synthesis, and significantly increase the proportion of senescent cells. PI3Kα-IN-28 can inhibit the expression of p-AKT and c-Myc and activate the AMPK-p27 pathway. PI3Kα-IN-28 can be used for research on cancers such as esophageal cancer.

Fmoc-Lys[Octa(OtBu)-Glu-OtBu]-OH is an Fmoc-protected amino acid derivative.

DRP1 Allosteric-IN-3 (Compound 2b) is an allosteric inhibitor of DRP1. Its IC50 value for the DRP1:MiD49 protein-protein interaction is 11 μM. DRP1 Allosteric-IN-3 can be used to study various diseases related to mitochondrial division disorders.

AMG-126737 is an orally active and highly selective human mast cell tryptase inhibitor with a Ki of 90 nM. AMG-126737 suppresses early/late-phase bronchoconstriction in sheep models. AMG-126737 is promising for research of asthma and allergic diseases.

UK-356202 is a urokinase-type plasminogen activator (uPA) with a Ki value of 0.037 μM. UK-356202 can be used in research related to the topical treatment of chronic ulcerous wounds.

MOL-6131 is a highly selective, reversible tryptase inhibitor, with a Ki of 45 nM. MOL-6131 significantly reduces the following features of allergic airway inflammation: eosinophil infiltration in lung tissue, goblet cell hyperplasia and mucus occlusion of airways.

BMS-354326 is a tryptase inhibitor with an IC50 of 1.8 nM. BMS-354326 exhibits excellent selectivity against trypsin and most other related serine proteases. BMS-354326 can be used in the research of asthma and inflammatory diseases.

JNJ-27390467 is a potent, orally active, and selective tryptase inhibitor (human β-tryptase IC50 = 3.6 nM, Ki = 3.7 nM). JNJ-27390467 exhibits excellent selectivity over trypsin of ~5000-fold. JNJ-27390467 shows effects in animal models of airway inflammation. JNJ-27390467 can be used for allergic asthma research.

2-thioacetyl MAGE is a colorimetric substrate of a serine hydrolase enzyme KIAA1363.

RWJ-58643 hydrochloride is a β-trypsin inhibitor that inhibits allergic inflammation. RWJ-58643 hydrochloride (1 g) significantly reduces nasal allergy symptoms, eosinophil infiltration, and IL-5 levels at low doses. RWJ-58643 hydrochloride causes late eosinophilia and elevated IL-5 levels at high doses (300 mg and 600 mg). RWJ-58643 hydrochloride modulates allergic reactions by inhibiting the release of β-trypsin from mast cells.

L-Isoleucyl-L-valine (Ile-Val) is a dipeptide that induces the bovine trypsinogen-trypsin transition.

Benzamidine is a reversible competitive trypsin inhibitor with a Ki of 19 μM. Benzamidine shows inhibitory activity against homogeneous boar sperm acrosin with a Ki of 4 μM.

Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab binds to the circulating PCSK9 protein, inhibiting it from binding to the LDLR. Evolocumab can be used for the research of hypercholesterolemia and atherosclerotic cardiovascular diseases.

SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.

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

AAF-CMK is a TPPII (tripeptidylpeptidase II) inhibitor, shows anti-tumor activity and induces apoptosis. AAF-CMK can be used in leukemia research.

Cyclotheonamide A is a serine protease inhibitor (cyclic polypeptide), which can be obtained from marine sponges of the genus Theonella. Cyclotheonamide A shows potent inhibitory activity against trypsin (Ki=0.023 µM) and streptokinase (Ki=0.035 µM) and moderate inhibitory activity against human α-thrombin (Ki=0.18 µM). Cyclotheonamide A can be used in study of antithrombotic.

UAMC-00050 is a potent trypsin-like serine protease inhibitor. UAMC-00050 can be used in research of dry eye syndrome and ocular inflammation.

Tilpisertib fosmecarbil is a potent serine/threonine kinase inhibitor. Tilpisertib fosmecarbil has anti-inflammatory activity.

Bezeparsen is a PCSK9 synthesis inhibitor.

Chymotrypsin (Chymotrypsin A) is a serine protease produced by the pancreas. Chymotrypsin cleaves protein chains at the carboxyl side of aromatic amino acids.

JO146 is a Chlamydia trachomatis high temperature requirement A (CtHtrA) protease inhibitor with IC50s of 21.86 and 1.15 μM for CtHtrA and human neutrophil elastase (HNE), respectively. JO146 can be used to inhibits bacterial infections.

Manusiran is a potent TMPRSS6 (transmembrane protease serine 6) synthesis reducer.

ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.

VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer.

APC 366 is a selective inhibitor of mast cell tryptase (Ki=7.1 μM). APC 366 inhibits antigen-induced early asthmatic response (EAR), late asthmatic response (LAR), and bronchial hyperresponsiveness (BHR) in a sheep model of allergic asthma.

Upamostat (WX-671), a novel serine protease urokinase (uPA) inhibitor by inhibiting the urokinase-type plasminogen activator (uPA) system.

APC-6860 is a trypsin-like serine proteases inhibitor with ki values of 0.21, 0.44, 1.5, 16.8, 20, 30 μM for uPA, trypsin, tryptase, tPA, thrombin and factor Xa, respectively. APC-6860 has a selectivity ratio for tPA versus uPA of 80. APC-6860 has ki values of 0.1, 0.082 μM for human and murine urokinases, respectively. APC-6860 can be used for the research of cancer.