Ser/Thr Protease
Serine proteases are enzymes that cleave peptide bonds in proteins, in which serine serves as the nucleophilic amino acidat the active site. They are found ubiquitously in both eukaryotes and prokaryotes. Serine proteases fall into two broad categories based on their structure: chymotrypsin-like or subtilisin-like. In humans, serine proteases are responsible for co-ordinating various physiological functions, including digestion, immune response, blood coagulation and reproduction. Threnonine proteases are a family of proteolytic enzymes harbouring a threonine (Thr) 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 andmechanism.
Targets for Ser/Thr Protease
Products for Ser/Thr Protease
- Cat.No. Product Name Information
- GC65044 Alirocumab (anti-PCSK9) Alirocumab (anti-PCSK9) is a human monoclonal antibody inhibiting proprotein convertase subtilisin/kexin type 9 (PCSK9).
- GC40032 Antipain (hydrochloride) Antipain (hydrochloride) is a protease inhibitor isolated from Actinomycetes.
- GC68302 AS-Inclisiran
- GC42915 Benzamidine (hydrochloride) Benzamidine is a reversible inhibitor of serine proteases, including trypsin, plasmin, and thrombin (Kis = 35, 350, and 220 μM, respectively).
- GC67751 Berotralstat dihydrochloride
- GC62175 Cetraxate hydrochloride Cetraxate hydrochloride (DV-1006), an orally active anti-ulcer agent with mucosal protective effects, can be used for gastric ulcers research.
- GC66092 Chymotrypsin Chymotrypsin (Chymotrypsin A) is a serine protease produced by the pancreas. Chymotrypsin cleaves protein chains at the carboxyl side of aromatic amino acids.
- GC62408 CRA-2059 hydrochloride CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
- GC62910 CRA-2059 TFA CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).
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GC64281
Evolocumab
Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9.
- GC60856 FOY 251 FOY 251, an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor.
- GC63423 Inclisiran Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9.
- GC17676 Nafamostat Broad spectrum serine protease inhibitor, kallikrein inhibitor
- GC16290 Nafamostat hydrochloride Synthetic serine protease inhibitor
- GC10613 Nafamostat Mesylate(FUT-175) A serine protease inhibitor
- GC62306 Patamostat Patamostat (E-3123) is a potent protease inhibitor.
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GC69670
PCSK9-IN-10
PCSK9-IN-10 is an effective, orally active PCSK9 inhibitor with an IC50 value of 6.4 µM. It increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 can slow down the progression of atherosclerosis. It has potential for researching hyperlipidemia.
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GC69671
PCSK9-IN-11
PCSK9-IN-11 (compound 5r) is an orally effective PCSK9 inhibitor. PCSK9-IN-11 exhibits transcriptional inhibition activity of PCSK9 in HepG2 cells with an IC50 of 5.7 μM. PCSK9-IN-11 increases the protein level of LDL receptor (LDLR). PCSK9-IN-11 can be used for atherosclerosis research.
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GC69672
PCSK9-IN-12
PCSK9-IN-12 is a heteroaromatic compound. It has binding affinity to PCSK9 with a Kd value of <200 nM. PCSK9-IN-12 can be used for research on cholesterol metabolism.
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GC50447
Pep 2-8
Potent PCSK9 inhibitor
- GC38028 PF-06446846 hydrochloride PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9).
- GC40998 Pinostrobin Pinostrobin is a flavonoid with diverse biological activities, including antioxidant, anti-inflammatory, and anticancer properties.
- GC64483 PKR-IN-C51 PKR-IN-C51(compound 51) is an ATP-competitive double-stranded RNA-activated protein kinase (PKR) inhibitor with an IC50 of 9 μM.
- GC32456 R-IMPP A cell-permeable inhibitor of PCSK9 secretion
- GC18424 SBC-110736 A PCSK9 inhibitor
- GC17417 SBC-115076 Anti-PCSK9 compound
- GC62303 SBC-115337 SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM.
- GC65958 Sebetralstat Sebetralstat (KVD900) is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases.
- GC31716 UK-371804 A uPA inhibitor
- GC63693 UK122 UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion.
- GC32882 Upamostat (WX-671) Upamostat (WX-671) (WX-671) is a serine protease inhibitor. Upamostat (WX-671) is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
- GC62662 WNK-IN-11 D3 WNK-IN-11 D3 is an orally active, selective and potent With-No-Lysine (WNK) kinase inhibitor.
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GC70147
WNK1-IN-1
WNK1-IN-1 is a selective inhibitor of WNK1 with an IC50 value of 1.6 μM. It inhibits the phosphorylation of OSR1 with an IC50 value of 4.3 μM. WNK1-IN-1 can be used for research on blood pressure regulation and cancer treatment.
- GC19383 WNK463 WNK463 is an orally bioavailable pan-WNK-kinase inhibitor with IC50s of 5, 1, 6, and 9 nM for WNK1, WNK 2, WNK 3, and WNK 4, respectively.
- GC64686 ZK824190 hydrochloride ZK824190 hydrochloride is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis.