Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].
Cathepsin L-IN-3 is a tripeptide-sized cathepsin L inhibitor.
Arg-Arg-AMC is a highly selective substrate of Cathepsin B. Arg-Arg-AMC can be used to cathepsin B activity assay in cancer cells, while cathepsin B is assocaited with cell invasive and metastatic phenotype in numerous types of cancer[1].
KGP-94 is a potent, selective cathepsin L inhibitor with IC50 of 189 nM, shows no significant inhibitory effect on cathepsin B (IC50>10 uM); significantly decreases the activity of cathepsin L toward human type I collagen, and impeds both migration and invasion of MDA-MB-231 human breast cancer cells; shows tumor growth retardation in a C3H mouse mammary carcinoma model.
A potent, selective, orally active inhibitor of cathepsin K with Ki of 0.1 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively; shows less or no potentcy for human cathepsin S/L/B/C (Ki=0.83/1.7/32/2500 nM); inhibits human osteoclasts bone resorption in vitro at a concentration more than 100 fold lower than that of alendronate; reduces plasma calcium level increased by PTHrP in thyroparathyroidectomized rats, decreases serum and urine C-telopeptide of type I collagen level. Osteoporosis Phase 2 Discontinued
Chymostatin is a potent cathepsin G inhibitor. Chymostatin inhibits fungal growth when combined with other pepsin inhibitors. Chymostatin can be used for acute lung injury and pancreatitis research[1].
Calpain-1 (pig) (μ-Calpain) is an intracellular Ca2+-regulated cysteine protease. Calpain-1 (pig) exhibits neuroprotective effect[1][2].
MK-0674 is a potent, orally bioavailable and selective cathepsin K inhibitor, with an IC50 of 0.4 nM, shows 1156, 1465, 11857 and 243 fold selectivity over Cat B, Cat F, Cat L and Cat S. MK-0674 exhibits long half-lives in rats, rabbits and rhesus monkeys[1].
3-Epiursolic Acid is a triterpenoid isolated from Myrtaceae, acts as a competitive inhibitor of cathepsin L (ICIC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsin B[1].
Z-Phe-Tyr(tBu)-diazomethylketone is a potent cathepsin L inhibitor. Z-Phe-Tyr(tBu)-diazomethylketone mediates reovirus disassembly. Z-Phe-Tyr(tBu)-diazomethylketone decreases viral detection[1][2].
Cathepsin X-IN-1 (compound 25) is a potent Cathepsin X inhibitor with an IC50 of 7.13 µM. Cathepsin X-IN-1 decreases PC-3 cell migration with low cytotoxic[1].
Z-Arg-Arg-4MβNA triacetate is a cathepsin B-specific substrate and can produce fluorescent end product 4MβNA (λex = 355 nm, λem = 430 nm)[1][2].
E-64 is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
LHVS is a potent, non-selective cysteine protease inhibitor[1]. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion[2].
H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH is a water-soluble polypeptide that can serve as a substrate for cathepsin D, pepsin and pepsinogen. H-Pro-Thr-Glu-Phe-p-nitro-Phe-Arg-Leu-OH has potential applications in biochemical analysis[1][2].
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI)[1][2].
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen[1].
Z-Phe-Ala-diazomethylketone binds directly to Aβ42 monomers and small oligomers. Z-Phe-Ala-diazomethylketone inhibits the formation of Aβ42 dodecamers and inhibits Aβ42 fibril formation in the solution. Z-Phe-Ala-diazomethylketone has the potential for neurodegenerative disorders research[1].
Cathepsin K inhibitor 5 is a potent Cathepsin K inhibitor[1].
Z-Arg-Arg-AMC hydrochloride is a selective substrate of cathepsin B[1].
Z-DEVD-CMK is an irreversible inhibitor of most of the cathepsins in vitro[1].
Z-FG-NHO-BzOME is a cysteine protease inhibitor that selectively inhibits cathepsin B, cathepsin L, cathepsin S, and papain[1].
RKLLW-NH2 is a Cathepsin L inhibitor[1].
SSAA09E1 is a cathepsin L blocker (IC50: 5.33 μM).SSAA09E1 inhibits stages of viral entry. SSAA09E1 can be used for SARS-CoV infection research[1]
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position[1][2].
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[3].
2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos[1].
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsin B inhibitor with IC50s of 4 nM. Ac-Leu-Val-Lys-Aldehyde significantly reduces quinolinic acid (HY-100807)-induced striatal cell death and causes accumulation of LC3-II[1].
Cathepsin L-IN-2 (Z-Phe-Phe-FMK) is a potent and irreversible cathepsin L and cathepsin B inhibitor[1][2].
Aurantiamide acetate (TMC-58A) is a selective and orally active cathepsin inhibitor isolated from Portulaca oleracea L. Aurantiamide acetate has anti-inflammatory activities and can be used for the study of inflammatory diseases[1][2].