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CathepsinK inhibitor 6 (compound 19) is an inhibitor of cathepsinK (Cat K) with an IC50 of 17 nM. CathepsinK inhibitor 6 also has inhibitory effects on other isoforms, with IC50s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively .
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsinK substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsinK activity .
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsinK, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsinK (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
Gü2602 is a potent, reversible cathepsinK (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsinK zymogen .
CathepsinK inhibitor 3 (compound 23) is a highly selective cathepsinK inhibitor with an IC50 value of 0.5 nM. CathepsinK inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies .
CathepsinK inhibitor 4 is a potent carbohydrazide CathepsinK inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse CathepsinK, respectively .
CathepsinK inhibitor 7 (compound 7) is a CathepsinK inhibitor with the pKi of 7.3 aganist CatK. CathepsinK inhibitor 7 can be used for study of osteoporosis .
CathepsinK inhibitor 2 is a potent inhibitor of cathepsinK. CathepsinK, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. CathepsinK inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78) .
Gü1303 is a potent, reversible, slow-binding cathepsinK (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsinK zymogen .
2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsinK inhibitor with an IC50 of 170 nM. 2-Cyanopyrimidine is used for osteoporos .
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsinK inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsinK, cathepsin S, cathepsin L, cathepsin B, respectively . L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsinK. L-873724 inhibits bone resorption .
Balicatib (AAE581) is a potent, orally active and selective cathepsinK inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsinK, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis .
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsinK, with an IC50 of 0.2 nM for human cathepsinK .
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsins B and L. K777 is a broad-spectrum antiviral by targeting cathepsin-mediated cell entry. K777 inhibits SARS-CoV and EBOV pseudovirus entry with IC50 values of 0.68 nM and 0.87 nM, respectively .
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 and a selective CCR4 antagonist featuring the potent chemotaxis inhibition. 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 .
Cathepsin C-IN-5 (compound SF38) is a potent, selective and orally active Cathepsin C inhibitor with IC50s of 59.9 nM, 4.26 µM, >5 µM, >5 µM, >5 µM for Cat C, Cat L, Cat S, Cat B, Cat K, respectively. Cathepsin C-IN-5 inhibits the Cat C activity in bone marrow and blood. Cathepsin C-IN-5 decreases the activation of NSPs (neutrophil serine proteases). Cathepsin C-IN-5 shows anti-inflammatory activity .
ONO-5334 is a potent, selective and orally active cathepsinK inhibitor with Ki values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsinK, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC50 value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease .
NC 2300 (VEL-0230)is a selective and orally active cysteine cathepsin inhibitor with the IC50 values of 284, 34.5, and 186 nM for cathepsin B, K, and S, respectively.NC 2300 can be used for study of diseases involving bone mineral disorders .
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsinsK, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsinK in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets . Calpeptin is also an inhibitor of cathepsinK .
MK-0674 is a potent, orally bioavailable and selective cathepsinK 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 .
SARS-CoV-2 Mpro-IN-6 is a covalent, irreversible and selective SARS-CoV-2 M pro inhibitor with an IC50 of 0.18 μM. SARS-CoV-2 Mpro-IN-6 does not inhibit human cathepsins B, F, K, and L, and caspase 3 .
Hepcidin-1 (mouse) is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) upregulates mRNA levels of TRAP, cathepsinK, and MMP-9 and increases TRAP-5b protein secretion. Hepcidin-1 (mouse) downregulates the level of FPN1 protein and increases intracellular iron. Hepcidin-1 (mouse) facilitates osteoclast differentiation .
Hepcidin-1 (mouse) TFA is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) TFA upregulates mRNA levels of TRAP, cathepsinK, and MMP-9 and increases TRAP-5b protein secretion. Hepcidin-1 (mouse) TFA downregulates the level of FPN1 protein and increases intracellular iron. Hepcidin-1 (mouse) TFA facilitates osteoclast differentiation .
Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsinK substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsinK activity .
Hepcidin-1 (mouse) TFA is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) TFA upregulates mRNA levels of TRAP, cathepsinK, and MMP-9 and increases TRAP-5b protein secretion. Hepcidin-1 (mouse) TFA downregulates the level of FPN1 protein and increases intracellular iron. Hepcidin-1 (mouse) TFA facilitates osteoclast differentiation .
CathepsinK inhibitor 4 is a potent carbohydrazide CathepsinK inhibitor with IC50s of 13 nM, 269 nM, 296 nM for human, rat, mouse CathepsinK, respectively .
Abz-HPGGPQ-EDDnp (CathepsinK substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. CathepsinK is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsinK activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsinK. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
Hepcidin-1 (mouse) is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) upregulates mRNA levels of TRAP, cathepsinK, and MMP-9 and increases TRAP-5b protein secretion. Hepcidin-1 (mouse) downregulates the level of FPN1 protein and increases intracellular iron. Hepcidin-1 (mouse) facilitates osteoclast differentiation .
Cathepsin K protein is a thiol protease that is critical in osteoclastic bone resorption and exhibits potent endoprotease activity against fibrinogen under acidic conditions. Its potential role in extracellular matrix degradation is noteworthy. Cathepsin K Protein, Mouse (His) is the recombinant mouse-derived Cathepsin K protein, expressed by E. coli , with N-6*His labeled tag. The total length of Cathepsin K Protein, Mouse (His) is 215 a.a., with molecular weight of ~31 kDa.
Cathepsin K protein is a thiol protease that plays a crucial role in osteoclastic bone resorption and contributes to bone remodeling. Working under acidic conditions, it exhibits potent endoprotease activity, particularly against fibrinogen, suggesting involvement in extracellular matrix degradation. Cathepsin K Protein, Human (P.pastoris, His) is the recombinant human-derived Cathepsin K, expressed by P. pastoris , with N-6*His labeled tag. The total length of Cathepsin K Protein, Human (P.pastoris, His) is 215 a.a.,
Cathepsin K protein is a thiol protease that is essential for osteoclastic bone resorption and regulation of bone remodeling. It exhibits potent endoprotease activity against fibrinogen under acidic conditions, suggesting its role in extracellular matrix degradation. Cathepsin K Protein, Rat (His) is the recombinant rat-derived Cathepsin K protein, expressed by E. coli , with N-6*His labeled tag. The total length of Cathepsin K Protein, Rat (His) is 215 a.a., with molecular weight of ~27.5 kDa.
Odanacatib-d4 is the deuterium labeled Odanacatib (HY-10042). Odanacatib is a potent and selective inhibitor of cathepsinK, with an IC50 of 0.2 nM for human cathepsinK .
Cathepsin K Antibody is an unconjugated, approximately 36 kDa, rabbit-derived, anti-Cathepsin K polyclonal antibody. Cathepsin K Antibody can be used for: WB, ELISA, IHC-P, IHC-F, IF expriments in rat, and predicted: human, mouse, dog, pig, cow, horse, guinea pig background without labeling.
Cathepsin L/V/K/H Antibody (YA2547) is a rabbit-derived non-conjugated IgG antibody (Clone NO.: YA2547), targeting Cathepsin L/V/K/H, with a predicted molecular weight of 38 kDa (observed band size: 38 kDa). Cathepsin L/V/K/H Antibody (YA2547) can be used for WB, IHC-P, ICC/IF, FC experiment in human, mouse, rat background.
Cathepsin Inhibitor 3 (Compound 53k) is a non-radioactive intermediate in compound [ 18F] 2k radioactive synthesis, which has selectivity for cathepsin S. Cathepsin Inhibitor 3 can undergo radioactive fluorination and can be used for fluorine-18 labeling research . Cathepsin Inhibitor 3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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