Cathepsin Inhibitor

RKLLW-NH2 is a Cathepsin L inhibitor.

Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a K_i of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen.

CTSL/CAPN1-IN-2 (Compound 14b) is an orally active inhibitor of both CTSL and CAPN1, with IC₅₀ values of 6.88 nM and 347.6 nM, respectively. CTSL/CAPN1-IN-2 possesses anti-inflammatory properties and favorable pharmacokinetic characteristics. CTSL/CAPN1-IN-2 exhibits broad-spectrum antiviral activity against coronaviruses by blocking viral entry.

Ctsk Rat Pre-designed siRNA Set A contains three designed siRNAs for Ctsk gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Gardenin B (Standard) is the analytical standard of Gardenin B (HY-N6037). This product is intended for research and analytical applications. Gardenin B is a flavonoid isolated from Gardenia jasminoides. Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC₅₀: 6.24 μg/mL), and Cathepsin D (IC₅₀: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC₅₀ values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.

Ctsb Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ctsb gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Ctse Rat Pre-designed siRNA Set A contains three designed siRNAs for Ctse gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

SQ 32056 is a cathepsin E inhibitor. SQ 32056 can block the pressor response to endothelin.

FGA139 is a cysteine proteases inhibitor with IC₅₀ values of 4.98/3.14 μM for cathepsin B/L. FGA139 reduces LPS-induced NO production in RAW264.7 cells and tumor necrosis factor (TNFα) levels in microglia, and has anti-oxidative stress and anti-inflammatory activities. FGA139 promotes the secretion of neuroprotective metabolites purine and linoleic acid by LPS-stimulated microglia. FGA139 can be used in neuroinflammatory diseases research.

(Rac)-Neurodegenerative Disorder-Targeting Compound 1 is a calpain inhibitor (extracted from patent WO2010128102A1, compound 63) .

Z-Arg-Lys-AOMK diTFA is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK diTFA reduces cytosolic cathepsin B activity in homogenates of mouse cerebral cortex and hippocampal tissues, and alleviates motor dysfunction associated with CCI-TBI. Z-Arg-Lys-AOMK diTFA can be used in the research of traumatic brain injury.

Olgotrelvir (STI-1558) is an orally active dual inhibitor of coronavirus main protease (Mpro) and human cell cathepsin (Cathepsin L). Olgotrelvir is readily converted to its active form, AC1115, in full blood and/or plasma. Olgotrelvir can effectively inhibit both SARS-CoV-2 replication and entry into host cells.

Z-L(D-Val)G-CHN2 is the isoform of Z-LVG-CHN2 (HY-108137). Z-LVG-CHN2 is a cell-permeable and irreversible inhibitor of cysteine proteinase. Z-LVG-CHN2 is a tripeptide derivative and mimics part of the human cysteine proteinase-binding center. Z-LVG-CHN2 displays an inhibition on HSV whereas no significant effect on poliovirus replication. Z-LVG-CHN2 effectively blocks SARS-COV-2 replication (EC₅₀=190 nM) via inhibition of SARS-COV-2 3CL pro protease.

K777 tosylate is a potent, orally active and irreversible cysteine protease inhibitor. K777 tosylate is also a potent CYP3A4 inhibitor with an IC₅₀ of 60 nM. K777 tosylate irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 tosylate is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 tosylate inhibits SARS-CoV and EBOV pseudovirus entry with IC₅₀ values of 0.68 nM and 0.87 nM, respectively.

Ctsl Rat Pre-designed siRNA Set A contains three designed siRNAs for Ctsl gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Z-LVG is an irreversible cysteine proteinase inhibitor. Z-LVG is a tripeptide derivative from cystatin C which can inhibit viral replication. Z-LVG can be used for virus diseases research.

Z-Leu-Leu-Leu-fluoromethyl ketone (Z-LLL-FMK) is a cysteine protease inhibitor. Z-Leu-Leu-Leu-fluoromethyl ketone inhibits SARS infection. Z-Leu-Leu-Leu-fluoromethyl ketone also protects mice against a T. crassiceps challenge.

GB111-NH2 is a cysteine cathepsin inhibitor and can be used in cancer research.

Cathepsin K inhibitor 4 is a potent carbohydrazide Cathepsin K inhibitor with IC₅₀s of 13 nM, 269 nM, 296 nM for human, rat, mouse Cathepsin K, respectively.

Anti-osteoporosis agent-9 (compound 5b) is a N-cyclopropyl-4-((4-((4-(trifluoromethyl)phenyl)sulfonyl)piperazin-1-yl)methyl)benzamide derivative that shows anti-osteoclast activity.