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Gly-Phe-β-naphthylamide is a substrate of CathepsinC (HY-P2922) and belongs to the lysosomal agonist. Gly-Phe-β-naphthylamide can freely pass through the cell membrane and organelle membrane. Gly-Phe-β-naphthylamide will be specifically hydrolyzed by CathepsinC, ultimately leading to a permeability lysis when it enters the acidic compartment. Gly-Phe-β-naphthylamide can be used to study lysosomal hydrolysis, lysosomal membrane permeability, and the function of cathepsinC .
diABZI-V/C-DBCO is a STING agonist with an EC50 of 1.47 nM. diABZI-V/C-DBCO activates the STING pathway, induces the production of IFN-I, and stimulates the secretion of IFN-β. diABZI-V/C-DBCO serves as a substrate for cathepsin B, and releases active diABZI-amine via cathepsin B-mediated cleavage. In an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO increases serum IFN-β levels and the frequency of granzyme B + CD8 + T cells. diABZI-V/C-DBCO is applicable to research related to triple-negative breast cancer .
diABZI-V/C-Mal is a STING agonist (with a STINGEC50 of 314 nM in TH1 dual reporter cells) and a Cathepsin B substrate. diABZI-V/C-Mal activates STING, thereby triggering the IRF3 signaling pathway. diABZI-V/C-Mal is cleaved by Cathepsin B to regenerate diABZI-NH2 .
CathepsinC-IN-5 (compound SF38) is a potent, selective and orally active CathepsinC 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. CathepsinC-IN-5 inhibits the Cat C activity in bone marrow and blood. CathepsinC-IN-5 decreases the activation of NSPs (neutrophil serine proteases). CathepsinC-IN-5 shows anti-inflammatory activity .
Gly-Phe-AMC is a fluorogenic peptide substrate consisting of a peptide sequence composed of glycine and phenylalanine, linked to the fluorophore AMC. Gly-Phe-AMC also serves as a cathepsinC substrate. Gly-Phe-AMC is widely used to detect the activity of various proteases .
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsinC inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
Ciluprevir (BILN 2061; BILN 2061ZW) is an orally active macrocyclic peptide inhibitor of hepatitis C virus (HCV)NS3 protease, with an IC50 of 3 nM. Ciluprevir has Kᵢ values of 0.66 nM and 0.30 nM against genotypes 1b and 1a, respectively. Ciluprevir inhibits HCV RNA replication with an EC50 of 1.2 nM, and its EC50 values against genotypes 1b and 1a are 3 nM and 4 nM, respectively. Ciluprevir shows no significant inhibition against human leukocyte elastase and hepatic cathepsin B. Ciluprevir can be used for genotype 1 HCV infection .
Verducatib (BI 1291583) is an orally active inhibitor of cathepsinC (also known as DPP1). Verducatib restores the protease-inhibitor balance by inhibiting the activation of neutrophil serine proteases, thereby alleviating pulmonary inflammation and regulating infection responses. Verducatib significantly reduces the risk (including severe exacerbations) and frequency of acute exacerbations in bronchiectasis (BE). Verducatib also improves lung function and quality of life, and shortens the duration of antibiotic use. The overall incidence of adverse events of Verducatib is comparable to that of placebo, with only slightly more mild-to-moderate cutaneous adverse events observed in the high-dose group, demonstrating promising clinical application potential .
CathepsinC is a lysosomal cysteine protease essential for catalytic activation of many serine proteases, including proteinase 3 (PR3), neutrophil elastase (NE), cathepsin G (CTSG), granzyme A/B/C, and mast cell chymase .
Eglin c (41-49) is a peptide fragment related to eglin c. Eglin c (41-49) shows inhibitory effects to cathepsin G and α-chymotrypsin with Ki values of 42 and 20 μM, respectively .
GSK-2793660 (free base) is an oral, irreversible inhibitor of CathepsinC (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis .
CathepsinC-IN-4 (compound SF27) is a potent CathepsinC (Cat C) inhibitor, with an IC50 of 65.6 nM. CathepsinC-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively .
CathepsinC-IN-3 (compound SF11) is a potent CathepsinC (Cat C) inhibitor, with an IC50 of 61.79 nM. CathepsinC-IN-3 also inhibits THP-1 and U937 cell, with IC50 values of 101.5 and 86.5 nM, respectively .
DPP-1-IN-1 (Compound 14) is an orally active inhibitor of CathepsinC (also known as Dipeptidyl peptidase I) with an IC50 of 5.31 nM. DPP-1-IN-1 can inhibit the activity of CathepsinC downstream Neutrophil elastase in neutrophils. DPP-1-IN-1 can be used in the research of inflammatory diseases .
BI-9740 is an orally active and selective cathepsinC (CatC) inhibitor, with an IC50 of 0.6 nM in mice and 2.6 nM in rats. BI-9740 can inhibit the production of active neutrophil elastase. Additionally, BI-9740 is capable of reducing the activities of neutrophil elastase and cathepsin G in the bone marrow of rats, alleviating pathological damage to grafts after heart transplantation, shortening the reperfusion time, and improving left ventricular function. BI-9740 can be used in research related to organ transplantation .
CathepsinC-IN-6 (compound 2) is a E-64c-hydrazideas based inhibitor of cathepsinC with anti-inflammatory activity. CathepsinC-IN-6 inhibts activation of neutrophil elastase，exhibits potential efficacy in inflammatory diseases with high neutrophil load (e.g.，chronic obstructive pulmonary disease) .
CTSC-IN-1 (B22) is a CTSC inhibitor. CTSC-IN-1 inhibits CTSC activity by binding to S2 pocket and S1 site. CTSC-IN-1 can be used in the study inflammatory bowel disease .
hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with KI values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity .
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27), an agent-linker conjugate for ADC, consists the ADC linker Mal-N(Me)-C6-N(Me) and a potent ADC cytotoxin PNU-159682. Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) selectively delivers the payload to CD46-expressing cells, where the linker is cleaved by cathepsin B to release PNU-159682, inducing DNA damage and apoptosis. Mal-N(Me)-C6-N(Me)-PNU-159682 shows durable tumor regression in xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) .
Z-Arg-Lys-AOMK is a cathepsin B inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK 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 can be used in the research of traumatic brain injury .
Y1693 is an orally active RANKL inhibitor with a Kd of 5.03 μM for hRANKL. Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP, cathepsin K, c-fos and NFATc1. Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases .
NB-533 is an orally active and brain-penetrant BACE-1 inhibitor with a human IC50 of 0.002 μM. NB-533 also inhibits human cathepsin D with an IC50 of 0.001 μM. NB-533 inhibits amyloidogenic amyloid precursor protein (APP) processing and reduces Aβ40 release. NB-533 reduces brain levels of APP metabolite C99 and Aβ40 in transgenic mice. NB-533 can be used for the research of Alzheimer’s disease .
Gly-Phe-AMC is a fluorogenic peptide substrate consisting of a peptide sequence composed of glycine and phenylalanine, linked to the fluorophore AMC. Gly-Phe-AMC also serves as a cathepsinC substrate. Gly-Phe-AMC is widely used to detect the activity of various proteases .
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
Eglin c (41-49) is a peptide fragment related to eglin c. Eglin c (41-49) shows inhibitory effects to cathepsin G and α-chymotrypsin with Ki values of 42 and 20 μM, respectively .
Cathepsin C/DPPI Protein, a thiol protease, exhibits dipeptidylpeptidase activity with broad substrate specificity, excluding proline at the P1 position and arginine at the P2 position. Operating as both exopeptidase and endopeptidase, it displays catalytic versatility. Crucially, Cathepsin C/DPPI activates serine proteases like elastase, cathepsin G, and granzymes A and B. Cathepsin C/DPPI Protein, Human (HEK293, C-His) is the recombinant human-derived Cathepsin C/DPPI protein, expressed by HEK293, with C-10*His labeled tag.
The cathepsin C/DPPI protein is a thiol protease that acts as a dipeptidyl peptidase with multiple substrate specificities, excluding proline at the P1 position and arginine at the P2 position. It has both exopeptidase and endopeptidase functions and can activate serine proteases such as elastase, cathepsin G, and granzymes A and B. Cathepsin C/DPPI Protein, Mouse (Inactive, His-Myc) is the recombinant mouse-derived Cathepsin C/DPPI protein, expressed by E. coli , with N-10*His, C-Myc labeled tag. The accession of Cathepsin C/DPPI Protein, Mouse (Inactive, His-Myc) is P97821 (D25-W134).
The cathepsin C/DPPI protein is a thiol protease that acts as a dipeptidyl peptidase with multiple substrate specificities, excluding proline at the P1 position and arginine at the P2 position. It has both exopeptidase and endopeptidase functions and can activate serine proteases such as elastase, cathepsin G, and granzymes A and B. Cathepsin C/DPPI Protein, Mouse (Active, HEK293, His) is the recombinant mouse-derived Cathepsin C/DPPI protein, expressed by HEK293, with C-10*His labeled tag. The proform was activated by Recombinant Human Cathepsin L and further purified.
The cathepsin C/DPPI protein is a thiol protease that acts as a dipeptidyl peptidase with multiple substrate specificities, excluding proline at the P1 position and arginine at the P2 position. It has both exopeptidase and endopeptidase functions and can activate serine proteases such as elastase, cathepsin G, and granzymes A and B. Cathepsin C/DPPI Protein, Mouse (HEK293, His) is the recombinant mouse-derived Cathepsin C/DPPI protein, expressed by HEK293, with C-10*His labeled tag.
Cathepsin A protein is an important protective factor for β-galactosidase and neuraminidase, maintaining their stability and optimizing enzyme activity. Its carboxypeptidase activity expands its functional repertoire and can deamid tachykinins and participate in a variety of biochemical processes. Cathepsin A Protein, Human (HEK293, His) is the recombinant human-derived Cathepsin A, expressed by HEK293, with C-6*His labeled tag. The total length of Cathepsin A Protein, Human (HEK293, His) is 452 a.a..
Cathepsin A Protein, Human (HEK293, His, solution) is a 58-60 kDa human cathepsin A protein with a His-flag. Cathepsin A is a multicatalytic enzyme with carboxypeptidase activities.
diABZI-V/C-DBCO is a STING agonist with an EC50 of 1.47 nM. diABZI-V/C-DBCO activates the STING pathway, induces the production of IFN-I, and stimulates the secretion of IFN-β. diABZI-V/C-DBCO serves as a substrate for cathepsin B, and releases active diABZI-amine via cathepsin B-mediated cleavage. In an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO increases serum IFN-β levels and the frequency of granzyme B + CD8 + T cells. diABZI-V/C-DBCO is applicable to research related to triple-negative breast cancer .
hCAIX-IN-21 (compound 16c) is a potent hCAIX inhibitor with KI values of 5.2, 3.5, 12.6, 13600 nM for hCAIX, hCA II, hCA XII, hCA I, respectively. hCAIX-IN-21 inhibits cathepsin B enzyme activity .
Sgc8c-M is a PTK7-targeted aptamer-drug conjugate (ApDC). Sgc8c-M is composed of the classic PTK7-specific aptamer Sgc8c, a cathepsin B (CTSB)-cleavable valine-citrulline (VC)-based linker, and the potent antimitotic agent Monomethyl auristatin E (MMAE) (HY-15162) as the payload. Sgc8c-M inhibits the growth of PTK7-overexpressing cancer cells. Sgc8c-M can be used for the study of PTK7-expressing advanced solid tumors .
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Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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