2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. Ser/Thr Protease

Ser/Thr Protease

Serine proteases; Serine endopeptidases; Threonine proteases

Ser/Thr Protease

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Serine (Ser) proteases catalyse the hydrolysis of specific peptide bonds in their substrates and this activity depends on a set of amino acids in the active site of the enzyme, one of which is always a serine. There are two families especially well studied, the trypsin family and the subtilisin family. Serine proteases play crucial roles in a wide variety of cellular as well as extracellular functions, including the process of blood clotting, protein digestion, cell signaling, inflammation, and protein processing. Threonine (Thr) proteases are a family of proteolytic enzymes harbouring a threonine residue within the active site. The prototype members of this class of enzymes are the catalytic subunits of the proteasome, however the acyltransferases convergently evolved the same active site geometry and mechanism.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-147404
    Tilpisertib fosmecarbil
    		Inhibitor
    Tilpisertib fosmecarbil is a potent serine/threonine kinase inhibitor. Tilpisertib fosmecarbil has anti-inflammatory activity.
    Tilpisertib fosmecarbil
  • HY-W231513
    MASTL/Aurora A-IN-1
    		Inhibitor 99.47%
    MASTL/Aurora A-IN-1 (Compound MA4) is a dual inhibitor of MASTL and Aurora A kinases with IC50 values of 0.56 μM and 0.16 μM, respectively. MASTL/Aurora A-IN-1 has broad-spectrum anticancer activity and has potent anticancer activity against SR (leukemia), K-562 (leukemia), MDA-MB-435 (melanoma), MOLT-4 (leukemia), and SK-MEL-2 (melanoma) cell lines in NCI-60 cancer cell lines with GI50 values of 0.023, 0.032, 0.037, 0.044, and 0.051 μM, respectively. MASTL/Aurora A-IN-1 inhibits Aurora A and MASTL kinases, inducing cell cycle G2/M arrest, thereby inhibiting cancer cell proliferation. MASTL/Aurora A-IN-1 can be used in cancer research, especially for tumors with dysregulated mitosis.
    MASTL/Aurora A-IN-1
  • HY-P2990
    Enteropeptidase
    Enteropeptidase (TMPRSS15), a type II transmembrane serine protease and a physiological activator of trypsinogen. Enteropeptidase is associated with the brush border membrane (BBM) of the enterocytes in the upper small intestine. Trypsinogen is the primary substrate for Enteropeptidase. Enteropeptidase is involved in digestion in humans and animals.
    Enteropeptidase
  • HY-P990464
    Anti-Matriptase Antibody
    		Inhibitor
    Anti-Matriptase Antibody is a human-derived antibody expressed in CHO, targeting Matriptase. The Anti-Matriptase Antibody has a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. The isotype control for Anti-Matriptase Antibody can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-Matriptase Antibody
  • HY-130136A
    TMPRSS6-IN-1 TFA
    		Inhibitor
    TMPRSS6-IN-1 (TFA) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice.
    TMPRSS6-IN-1 TFA
  • HY-19727
    FOY 251 free base
    		Inhibitor
    FOY 251 free base, an anti-proteolytic active metabolite of Camostate (HY-13512), acts as a proteinase inhibitor. FOY 25 free base inhibits SARS-CoV-2 infection in cells assay.
    FOY 251 free base
  • HY-112143
    STOCK2S-26016
    		Inhibitor 98.7%
    STOCK2S-26016 is a WNK signalling inhibitors. STOCK2S-26016 inhibits WNK4 and WNK1 with IC50s of 16 μM and 34.4 μM, respectively. STOCK2S-26016 has potential for antihypertensive research.
    STOCK2S-26016
  • HY-19303
    CRA-2059
    		Inhibitor
    CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
    CRA-2059
  • HY-130136
    TMPRSS6-IN-1
    		Inhibitor
    TMPRSS6-IN-1 (compound 8) is a potent inhibitor of TMPRSS6 (Matriptase-2), belonging to TTSPs (transmembrane serine protease). TMPRSS6, is a type II TTSP, the genetic reduction of which will improve symptoms of hemochromatosis and beta thalassemia in mice.
    TMPRSS6-IN-1
  • HY-137495
    GGACK
    		Inhibitor
    GGACK (H-Glu-Gly-Arg-CMK) is an irreversible substrate-like serine protease urokinase-type plasminogen activator (uPA) inhibitor.
    GGACK
  • HY-P10095A
    D-Val-Phe-Lys-CMK diTFA
    		Inhibitor
    D-Val-Phe-Lys-CMK (D-Val-Phe-Lys Chloromethyl ketone) diTFA can inhibit plasmin activity.
    D-Val-Phe-Lys-CMK diTFA
  • HY-P4310
    Boc-Val-Leu-Lys-AMC
    		98.93%
    Boc-Val-Leu-Lys-AMC is a sensitive, fluorogenic, and specific substrate of plasmin, as well as acrosin from the ascidian Halocynthia roretzi, porcine calpain isozymes I and II, and papain.
    Boc-Val-Leu-Lys-AMC
  • HY-126361
    ZK824190
    		Inhibitor
    ZK824190 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.
    ZK824190
  • HY-E70226
    Cathepsin S, human
    Cathepsin S, human, is a potent cysteine protease that promotes the degradation of damaged or harmful proteins in the endolysosomal pathway. Cathepsin S, human, is involved in multiple pathological processes, including arthritis, cancer, and cardiovascular disease.
    Cathepsin S, human
  • HY-E70192
    Acetyltrypsin, Bovine pancreas
    Acetyltrypsin, Bovine pancreas is a stable trypsin derivative that can catalyze the hydrolysis of alpha-N-benzoyl-L-argininamide.
    Acetyltrypsin, Bovine pancreas
  • HY-153752
    TAO Kinase inhibitor 2
    		Inhibitor
    TAO Kinase inhibitor 2 (Example 49) is a TAO Kinase inhibitor (IC50=between 50 and 500 nM). TAO Kinase inhibitor 2 also inhibits KIAA1361 and JIK with IC50s of 50-500 nM.
    TAO Kinase inhibitor 2
  • HY-144820
    JO146
    		Inhibitor 98.49%
    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.
    JO146
  • HY-129263
    L-Isoleucyl-L-valine
    L-Isoleucyl-L-valine (Ile-Val) is a dipeptide that induces the bovine trypsinogen-trypsin transition.
    L-Isoleucyl-L-valine
  • HY-P2942
    Chymotrypsinogen
    Chymotrypsinogen is an inactive precursor of Chymotrypsin (HY-108910). Chymotrypsin is a serine protease produced by the pancreas.
    Chymotrypsinogen
  • HY-161847
    HZ1
    		Inhibitor 99.20%
    Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor.
    HZ1
Cat. No. Product Name / Synonyms Application Reactivity