Cathepsin Inhibitor

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.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC₅₀ of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.

Cathepsin L-IN-3 (Compound cat L inh. 7) is selective a noncovalent cathepsin L inhibitor with a K_i of 4.3 nM.

ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.

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

Leupeptin Ac-LL is a broad-spectrum protease inhibitor. By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin Ac-LL significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin Ac-LL inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin Ac-LL can be used in research on chronic inflammatory diseases and skin tumorigenesis.

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-IN-5 is a cathepsin inhibitor with IC₅₀ values of 6.2 μM and 81 nM for cathepsin L and cathepsin S. Cathepsin-IN-5 inhibits cancer cells proliferation, induces apoptosis, reduces growth of hepatocellular tumors in mouse models, and modulates expression of genes linked to cell death, cell proliferation, and cellular processes. Cathepsin-IN-5 can be used for the research of hepatocellular carcinoma.

Ac-VLPE-FMK, a tetrapeptidyl mono-fluoromethyl ketone (m-FMK), is a Cat-B and Cat-L inhibitor. Ac-VLPE-FMK can be used for the research of cancer aggressiveness.

Tasiamide B is a Cathepsin D inhibitor, which is a linear peptide found in the marine cyanobacteria Symploca sp.. Tasiamide B is proved as a good template for the development of aspartic proteases inhibitors. Tasiamide B is effective against skin cancer by strongly interacting with the target protein HSP90.