Papain

Papain, a cysteine protease of the peptidase C1 family, is utilized in the food, pharmaceutical, textile, and cosmetic industries.

Papain Inhibitor acetate (Gly-Gly-Tyr-Arg) is an affinity Ligand for Papain.

PLpro inhibitor is a potent papain-like protease (PLpro) inhibitor(IC50 of 2.6 uM)

4'-O-Methylbavachalcone (O-Methylbroussochalcone B) is isolated from Psoralea corylifolia, inhibits severe acute respiratory syndrome coronavirus (SARS-CoV) papain-like protease (PLpro) activity (IC50: 10.1 μM).

TC-067533 is a Papain-like protease inhibitor with an IC50 of 8.7 μM.

Z-Lys-OH is a competitive inhibitor of papain, a lysine derivative.

Calpeptin is a cell-permeable Calpain inhibitor (IC50 = 5 nM), and its ID50 value for human platelet Calpain I is 40 nM. Calpeptin is also an effective inhibitor of Cathepsin K (IC50 = 0.11 nM).

L-Cystine (Cystine Acid) is not considered one of the 20 amino acids, L-Cystine (Cystine Acid) is a sulfur-containing derivative obtained from oxidation of cysteine amino acid thiol side chains. It functions as an antioxidant and protects tissues against radiation and pollution, slowing the aging process. It also aids protein synthesis. L-Cystine (Cystine Acid) is abundant in many proteins of skeletal tissues and skin, and found in insulin and digestive enzymes chromotrypsinogen A, papain, and trypsinogen.

PLpro-IN-6 (compound 6) serves as an inhibitor for the papain-like protease (PLpro), demonstrating potent activity with an IC 50 of 0.019 μM against the SARS-CoV-2 PLpro enzyme.

PF-07957472 (Compound 4) is an orally effective inhibitor of the SARS-CoV-2 papain-like protease (PLpro). In NHBE cells infected with SARS-CoV-2, it demonstrated cytopathic effects with an EC50 of 13.9 nM. Additionally, PF-07957472 exhibited antiviral activity in a mouse-adapted COVID-19 infection model.

PLpro-IN-8 (compound 1) serves as an inhibitor of the SARS-CoV papain-like protease (PLpro), exhibiting IC50 values of 5.9 μM for SARS-CoV-2 PLpro and 0.46 μM for SARS-CoV-1 PLpro. Additionally, it hinders the Wuhan SARS-CoV-2 strain WK-521 with an EC50 of 2.7 μM.

PLpro-IN-7 (compound 83) is a novel papain-like protease (PLpro) inhibitor with an IC50 of 3 nM.

SARS-CoV-2-IN-102 (example 58) is an inhibitor of the SARS-CoV papain-like protease (SARS-CoVPLpro), demonstrating an IC50 of less than 100 nM.

SARS-CoV-2-IN-106 (compound 19) is a SARS-CoV-2 papain-like protease inhibitor, displaying IC50 values of 0.44 μM for papain-like proteases and 0.18 μM for viral replication.

SARS-CoV-2-IN-108 (Compound 29) is an inhibitor of SARSCoV-2 papain-like protease, with an IC50 of 0.14 µM. It can inhibit viral replication, displaying an EC50 of 0.21 µM.

Jun13728 is a potent and covalent inhibitor of the SARS-CoV-2 papain-like protease, with an IC50 value of 0.1 μM. This compound is applicable for antiviral research related to SARS-CoV-2.

ZHAWOC25153 (Compound 17o) is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 7 μM. It demonstrates antiviral properties and is applicable for research in the field of anti-infective studies.

9-AMN is an inhibitor of the SARS-CoV-2 papain-like protease (SARS-CoV-2 PLpro), effectively reducing its deubiquitinating (DUB) activity and protease activity, with IC50 values of 4.55 µM and 4.15 µM, respectively. Additionally, 9-AMN suppresses the replication of the SARS-CoV variants Delta and Omicron in Calu-3 cells, with IC50 values of 1.04 µM and 2.35 µM, respectively.

Jun13296 is an orally active quinoline SARS-CoV-2 papain-like protease inhibitor (IC50 = 0.13 µM, Ki = 8.8 nM). It demonstrates potent inhibitory effects against SARS-CoV-2 variants and Nirmatrelvir-resistant mutants. Jun13296 reduces lung viral titers and prevents lung tissue damage in SARS-CoV-2 infection models.

Mpro/PLPro-IN-2 (Compound 22l) is a non-covalent competitive dual inhibitor of SARS-CoV-2's papain-like protease and main protease, exhibiting a Ki of 0.2 μM for the papain-like protease and 1.1 μM for the main protease. Mpro/PLPro-IN-2 is applicable in research related to anti-SARS-CoV-2 efforts.

WEHI-P8 is an orally active inhibitor targeting the coronavirus papain-like protease (PLpro). It inhibits SARS-CoV-2 PLpro with an IC50 of 12 nM and demonstrates excellent cellular activity with an EC50 of 298 nM. Additionally, WEHI-P8 has protective effects in mice against prolonged lung and brain symptoms caused by SARS-CoV-2. This compound is applicable for research on post-COVID-19 syndrome.

PLpro-IN-2 (Compound 16) is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro), with an IC50 value of 0.25 μM.

SARS-CoV-2-IN-72 (compound 12) is a potent allosteric inhibitor of the SARS-CoV-2 papain-like protease domain, capable of inducing degradation of NSP3.

Jun12682 is an inhibitor of the SARS-CoV-2 papain-like protease (PLpro). It has a Ki value of 37.7 nM against PLpro and an EC50 value of 1.1 μM in the FlipGFP PLpro assay. Jun12682 is also orally active.