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MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsinB and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
K777 is a potent, orally active and irreversible cysteine protease inhibitor. K777 is also a potent CYP3A4 inhibitor with an IC50 of 60 nM. K777 irreversibly inhibits Cruzain, the major cysteine protease of Trypansoma cruzi, and cathepsinsB 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 .
Z-Arg-Arg-AMC hydrochloride is a highly selective fluorescent CathepsinB substrate. Z-Arg-Arg-AMC hydrochloride can be hydrolyzed by CathepsinB to produce a fluorescent product for enzyme activity detection .
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis .
CA-074 methyl ester is a specific inhibitor of CathepsinB, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
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 cathepsinB, and releases active diABZI-amine via cathepsinB-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 .
CathepsinB, Bovine spleen is a cysteine protease and is involved in multiple kinds of programmed cell death (including apoptosis, pyroptosis, ferroptosis, necroptosis, and autophagic cell death) .
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsinB, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis .
Alloc-Val-Ala-PAB is a peptide cleavable linker used in the synthesis of antibody-drug conjugates (ADCs). The Val-Ala will specifically be cleaved by CathepsinB. The Alloc group is stable to treatment with piperidine and TFA, but can be easily removed under mild conditions by palladium catalyzed allyl transfer.
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, cathepsin K, 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-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsinB activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
diABZI-V/C-Mal is a STING agonist (with a STINGEC50 of 314 nM in TH1 dual reporter cells) and a CathepsinB substrate. diABZI-V/C-Mal activates STING, thereby triggering the IRF3 signaling pathway. diABZI-V/C-Mal is cleaved by CathepsinB to regenerate diABZI-NH2 .
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsinB, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
L-Arginine-7-amido-4-methylcoumarin (Arginine 4-methyl-7-coumarylamide) hydrochloride is a specific substrate of cathepsin H but not for cathepsins L and B .
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 .
PD 151746 is a selective calpain-1 inhibitor with an IC50 of 260 nM. PD 151746 binds μ-calpain Ca 2+-binding sites, and shows selectivity over cathepsinB, papain, trypsin, thermolysin, and basal calcineurin. PD 151746 reduces Oxidized low-density lipoprotein (oxLDL)-induced cytotoxicity, apoptotic DNA fragmentation, and blocks IL-1α maturation. PD 151746 can be used for the research of atherosclerosis and psoriasis .
PSMA-Val-Cit-PAB-MMAE is a small-molecule conjugate targeting PSMA, with Monomethyl auristatin E (MMAE) (HY-15162) as its cytotoxic payload. PSMA-Val-Cit-PAB-MMAE binds to PSMA, thereby being delivered into PSMA-expressing prostate cancer cells. Subsequently, the Val-Cit linker is cleaved under the mediation of cathepsinB, releasing active MMAE. PSMA-Val-Cit-PAB-MMAE inhibits CYP3A4 activity (IC50 = 11.2 μM), induces intracellular ROS production and oxidative stress, disrupts the cytoskeleton through microtubule destabilization, and induces prostate cancer cell death. PSMA-Val-Cit-PAB-MMAE can be used in research related to prostate cancer .
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsinB .
VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsinB, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects .
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 .
JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
Poly-L-Glutamic acid (MW 700000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-Glutamic acid is an ideal tumor-targeting polymer carrier. Poly-L-Glutamic acid can be hydrolyzed by cathepsinB during metabolic decomposition .
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 cathepsinB. Ciluprevir can be used for genotype 1 HCV infection .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsinB and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
Arg-Arg-AMC acetate is the acetate salt form of Arg-Arg-AMC (HY-P4340). Arg-Arg-AMC acetate is a fluorescent substrate for cathepsinB and used in the cathepsinB activity assay .
Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Cathepsin C 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 .
Poly-L-glutamic acid sodium salt (MW 30000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
DBCO-PEG4-Val-Cit-PAB-PNP is a cleavable ADC linker. The Val-Cit will specifically be cleaved by CathepsinB. PNP can be substituted by amine-containing payload. DBCO enable click chemistry with azide molecules.
DBCO-PEG4-Val-Ala-PAB-PNP is a cleavable ADC linker. The Val-Ala linkers can be cleaved by CathepsinB. The DBCO groups is commonly used for Click Chemistry reactions. PEG spacer improves the compound's aqueous solubility. PNP is a good leaving group.
Hepcidin-1 (mouse) is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) upregulates mRNA levels of TRAP, cathepsin K, 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 .
DBCO-PEG3-Glu-VC-PABC-MMAF (compound s19b) is a drug-linker conjugate for ADC by using the tubulin inhibitor, MMAF (HY-15579), linked via cathepsin cleavable DBCO-PEG3-Glu-VC-PABC. DBCO-PEG3-Glu-VC-PABC-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs) .
Dibenzyl trisulfide (DTS) is an active ingredient that can be isolated from Petiveria alliacea L.. Dibenzyl trisulfide inhibits cell proliferation and migration. Dibenzyl trisulfide decreased the mRNA and protein expression of BAK-1 and LTA. Dibenzyl trisulfide induces lysosomal membrane permeabilization and cathepsinB release .
Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease CathepsinB and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-CathepsinB type proteins .
Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC50 of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC50s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively .
Poly-L-glutamic acid sodium salt (MW 15000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 7500) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsinB 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 .
TB-9, a Tasiamide B (HY-N15154) derivative, is a potent cathepsin D, cathepsin E, and BACE1 inhibitor with IC50s of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively .
Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsinB, respectively . L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption .
NM-001 is a theranostic prodrug that targets ανβ3 integrin. NM-001 consists of cRGD and GFLG peptides, a DCM fluorophore and Chlorambucil (HY-13593). NM-001 internalizes into lysosomes of tumor cells via the cRGD peptide, and generates NM-002 (HY-178820) and Chlorambucil through intracellular cleavage at the GFLG peptide by overexpressed CathepsinB (CTSB). NM-001 exhibits green fluorescence under physiological conditions, and converts to NIR fluorescence by CTSB activation. NM-001 has significant antitumor activity with low toxicity in HeLa cell xenografts mouse models. NM-001 can be used for real-time drug release monitoring research .
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 .
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 cathepsinsB 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 .
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 .
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 cathepsinsB, F, K, and L, and caspase 3 .
Ac-RR-AFC TFA is a CathepsinB fluorogenic substrate (Ex=400 nm, Em=505 nm). CathepsinB activity in cells lysates is determined by measuring cleavage of Ac-RR-AFC TFA and its cleavage occurs at the RR-AFC amide bond. Ac-RR-AFC TFA can be used for activity assays and mechanistic studies on cathepsinB .
Arg-Arg-AMC is a highly selective substrate of CathepsinB. Arg-Arg-AMC can be used to cathepsinB activity assay in cancer cells, while cathepsinB is assocaited with cell invasive and metastatic phenotype in numerous types of cancer .
JNJ 10329670 is a potent and selective noncovalent cathepsin S inhibitor with a Ki value of 34 nM for human cathepsin S. JNJ 10329670 blocks invariant chain proteolysis in B cells and dendritic cells, as well as antigen-induced T cell proliferation .
Abz-HPGGPQ-EDDnp (Cathepsin K 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. Cathepsin K 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 cathepsin K 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 cathepsin K. This peptide is resistant to hydrolysis by cathepsinsB, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
SmCB1-IN-1 (Compound 2h) is an inhibitor for S. mansonicathepsinB1 (SmCB1) with an Ki of 0.05 μM . SmCB1-IN-1 exhibits selectivity toward human off-target cathepsins (29% and 37% inhibition for CatB and CatL at 20 μM). SmCB1-IN-1 inhibits 68% Schistosoma mansoni at 1 μM .
Poly-L-glutamic acid sodium salt (MW 60000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
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 .
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsinB and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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 .
MC-Val-Ala-NHS ester is a cleavable ADC linker with a malimide group and an NHS ester group. The Val-Ala linkers can be cleaved by CathepsinB. Maleimide group is reactive toward thiol groups. MC is reactive with thiol moieties. The NHS ester is able to react specifically and efficiently with amines (e.g. the side chain of lysine residues or aminosilane-coated surfaces) at neutral or slightly basic condition to form a covalent bond.
HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC50 of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsinB (CTSB) in the lysosomes, with a DC50 of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8 .
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 cathepsinB enzyme activity .
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsinB, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
Abz-GIVRAK(Dnp) is the most efficient substrate for cathepsinB and is highly selective for this enzyme among lysosomal cysteine proteases. After Abz-GIVRAK(Dnp) is hydrolyzed, aminoacylbenziminosulfosuccinic acid (Abz-SAS) is released, and dinitrobenzoyl (Dnp) is also released. The product of this hydrolysis reaction, Abz-SAS, is fluorescent under ultraviolet light and can emit a fluorescent signal .
Poly-L-Glutamic acid (MW 100000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-Glutamic acid is an ideal tumor-targeting polymer carrier. Poly-L-Glutamic acid can be hydrolyzed by cathepsinB during metabolic decomposition .
AM4299B is an inhibitor for thiol protease. AM4299B inhibits bovine spleen cathepsinB, human kidney cathepsin L and papain with IC50s of 0.7, 0.5 and 20 μM, respectively. AM4299B can be used in research in osteoporosis, and has potential to be used as an antiparasitic agent .
Oxocarbazate is an inhibitor of human cathepsin L with the IC50 values of 6.9 nM (human Cathepsin L,0 h) 0.4 nM ((human Cathepsin L,4 h) and 5.07 μM (human cathepsinB), respectively. Oxocarbazate blockes both SARS-CoV (IC50 = 273 nM) and Ebola virus (IC50 = 193 nM) entry into 293T cells .
(S,R,R)-VBY-825 is the isomer of VBY-825 (HY-15958), and can be used as an experimental control. VBY-825 is a novel reversible inhibitor of cathepsin with high inhibition of cathepsinB, L, S and V.
L-006235 (Standard) is the analytical standard of L-006235. This product is intended for research and analytical applications. L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsinB, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
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 cathepsinB, K, and S, respectively.NC 2300 can be used for study of diseases involving bone mineral disorders .
Tetromycin B is a cysteine protease inhibitor with Ki values of 0.62, 1.42, 32.5, and 1.59 μM for rhodesain, falcipain-2, cathepsin L, and cathepsinB, respectively. It inhibits the growth of T. brucei in vitro (IC50=30.87 μM). Tetromycin B is also cytotoxic to HEK293T kidney cells and J774.1 macrophages (IC50s=71.77 and 20.2 μM, respectively).
SARS-CoV-2 Mpro-IN-31 (Compound 18) is an inhibitor of SARS-CoV-2 M Pro with an IC50 value of 11 nM. Additionally, SARS-CoV-2 Mpro-IN-31 effectively inhibits the enzymatic activity of the cysteine proteases cathepsinB and cathepsin L, with IC50 values of 24 nM and 1.8 nM, respectively .
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 .
Poly-L-glutamic acid sodium salt (MW 120000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 3000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 45000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
DBCO-PEG4-Val-Ala-PAB is a cleavable ADC linker. The Val-Ala linkers can be cleaved by CathepsinB. The DBCO groups is commonly used for Click Chemistry reactions. PEG spacer improves the compound's aqueous solubility.
Alloc-Val-Ala-OH (((Allyloxy)carbonyl)-L-valyl-L-alanine) is a building block in the synthesis of Tesirine, a clinical antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. The Val-Ala will specifically be cleaved by CathepsinB. The Alloc group is stable to treatment with piperidine and TFA, but can be easily removed under mild conditions by palladium catalyzed allyl transfer.
Azido-PEG8-Amido-Val-Cit-PAB is a cleavable ADC linker. The Val-Cit will specifically be cleaved by CathepsinB. As this enzyme is only present in the lysosome, the ADC payload will be released only in the cell. Azido will react with DBCO, BCN or other alkyne groups through click chemistry. PEG spacer increases aqueous solubility. Reagent grade, for research purpose.
HDAC3-IN-7 (Compound 8ae) is a selective HDAC3 inhibitor with an IC50 value of 311 nM. HDAC3-IN-7 degrades PD-L1 through the lysosome pathway mediated by CathepsinB, exerting activities such as inhibiting tumor cell proliferation, migration, and invasion. HDAC3-IN-7 is promising for research of cancers .
Cathepsin L-IN-7 is an inhibitor of cathepsin L, cathepsinB and cathepsin S. Cathepsin L-IN-7 has an IC50 of 0.011 μM against cathepsin L and an IC50 of 0.062 μM against cathepsin S, while it shows weak inhibitory activity against cathepsinB. Cathepsin L-IN-7 binds to the active site of cysteine proteases and blocks their proteolytic function. Cathepsin L-IN-7 can be used in research on viral infections and cancer .
Z-Arg-Lys-AOMK is a cathepsinB inhibitor that can cross the blood-brain barrier. Z-Arg-Lys-AOMK reduces cytosolic cathepsinB 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 .
Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on CathepsinB or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .
PI3K-001 is a cathepsinB-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsinB-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis .
TML-2Cl is a dichloro-modified trimethyl lock adapter for antibody-drug conjugates and payload releaser.TML-2Cl undergoes 1,6-elimination followed by rapid self-cyclization to facilitate release of the payload Exatecan after cathepsinB cleavage of the associated linker.TML-2Cl exhibits high stability when conjugated to a drug and high intrinsic hydrophobicity.TML-2Cl can be used for the research of gastric carcinoma .
Cathepsin K-IN-9 is a selective, potent and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. Cathepsin K-IN-9 has IC50 > 10000 nM for cathepsinB, L, and S, showing over 1600-fold selectivity. Cathepsin K-IN-9 has excellent safety and metabolic stability.Cathepsin K-IN-9 can be used for the research of osteoporosis .
JPM-OEt (Standard) is the analytical standard of JPM-OEt (HY-102087). This product is intended for research and analytical applications. JPM-OEt is a broad spectrum cysteine cathepsin inhibitor. JPM-OEt binds covalently in the active site, and irreversibly inhibits the cysteine cathepsin family. Antitumor activity .
CA-074 (Standard) is the analytical standard of CA-074 (HY-103350). This product is intended for research and analytical applications. CA-074 is a potent inhibitor of cathepsinB with a Ki of 2 to 5 nM.
CA-074 methyl ester (Standard) is the analytical standard of CA-074 methyl ester (HY-100350). This product is intended for research and analytical applications. CA-074 methyl ester is a specific inhibitor of CathepsinB, which has potent bioactivities such as neuroprotective, anti-cancer, and anti-inflamatory effects.
GK730 is a potent and selective SARS-CoV-2 main protease inhibitor with an IC50 of 5.75 nM. GK730 does not inhibit cathepsinB, while exhibits weak inhibition of cathepsin L (IC50 = 11 μM). GK730 can simultaneously block the replication of the virus and the entry pathways for variants such as Omicron into cells. GK730 demonstrates an EC50 value of 5.70 μM against a wild-type SARS-CoV-2 strain in Vero E6 cells and CC50 value greater than 100 μM. GK730 can be used for the research of COVID-19 .
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsinB 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 .
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsinB (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury .
NM-002 is a metabolite of prodrug NM-001 (HY-178819), with NIR emission. NM-002 generates through activates the prodrug NM-001 by overexpressed CathepsinB (CTSB) within tumor cells. NM-002 has no toxicity towards tumor cells and can escape from the lysosomes into the cytoplasm. NM-002 can be used for real-time drug release monitoring research .
NCO-700 is a dual cathepsinB and calcium-activated neutral protease (CANP) inhibitor with IC50 values of 0.8 and 46 μM, respectively. NCO-700 reduces the degradation of myocardial fibrin by inhibiting protease activity. NCO-700 also has inhibitory effects on hormone-independent tumor cells, such as prostate cancer cells, and induces apoptosis. NCO-700 can be used to study myocardial ischemia and refractory hormone-independent tumors .
FGA139 is a cysteine proteases inhibitor with IC50 values of 4.98/3.14 μM for cathepsinB/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 .
Z-FA-FMK ((1S)-Z-FA-FMK) is a potent CathepsinB and L inhibitor. Z-FA-FMK blocks the induction of DEVDase activity, DNA fragmentation, and externalization of phosphatidylserine by selective synthetic retinoid-related molecules (RRMs). Z-FA-FMK inhibits apoptosis. Z-FA-FMK inhibits caspase activity and selectively inhibits recombinant effector caspases 2, -3, -6, and -7. Z-FA-FMK is a viral inhibitor. Z-FA-FMK inhibits reovirus replication in a susceptible host .
Mal-VC-PAB-seco-CBI-PBD dimer is a highly active drug-linker conjugate. Mal-VC-PAB-seco-CBI-PBD dimer integrates the DNA-damaging effects of two distinct types of compounds: seco-cyclopropabenzindoline (seco-CBI) and pyrrolobenzodiazepine (PBD). Mal-VC-PAB-seco-CBI-PBD dimer is linked via a valine-alanine (VC) linker cleavable by cathepsinB and achieves targeted delivery relying on monoclonal antibodies. Mal-VC-PAB-seco-CBI-PBD dimer is applicable for cancer research .
NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsinB. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsinB with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages .
Anti-inflammatory agent 113 (compound B5) is a Cathepsin L (CTSL) inhibitor and anti-inflammatory agent with a CTSL IC50 of 5.52 μM. Anti-inflammatory agent 113 suppresses CTSL maturation, attenuates NF-κB and p38 MAPK signaling pathway activation, and binds stably in CTSL’s active site via noncovalent interactions with Asp162, Cys25, and Glu63. Anti-inflammatory agent 113 inhibits pro-inflammatory cytokine (IL-6, IL-8) production, reduces inflammatory cell lung infiltration, and alleviates lung tissue injury. Anti-inflammatory agent 113 can be used for the research of acute lung injury .
Ono 3307 Free base is a novel synthetic protease inhibitor that exhibits protective effects against acute pancreatitis by preventing hyperamylasemia and pancreatic edema. Ono 3307 Free base also inhibits the redistribution of lysosomal enzymes in acinar cells and mitigates lactic dehydrogenase discharge. Ono 3307 Free base effectively reduces cathepsinB leakage from lysosomes in a dose-dependent manner. Ono 3307 Free base is able to target trypsin (Ki=48 nM), thrombin (Ki=0.18 μM), plasma kallikrein (Ki=0.29 μM), plasmin (Ki=0.31 μM), pancreatic kallikrein (Ki=3.6 μM), and chymotrypsin (Ki=47 μM).
CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer .
Ac-RKAA-PABC-MMAE is a Drug-Linker Conjugates for ADC. Ac-RKAA-PABC-MMAE consists of the ADC Cytotoxin MMAE (HY-15162) and a linker. Ac-RKAA-PABC-MMAE can be used for synthesis of ADCs .
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 cathepsinB 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) .
MPD-1 (Maleimide-KGDEVD-doxorubicin) is a peptide drug conjugate (PDC). MPD-1 releases Doxorubicin (HY-15142) via radiation-activated caspase-3 cleavage, triggering a cytotoxic amplification cascade at the tumor site. MPD-1 enhances CD8 + T cell tumor infiltration, and activates antigen-presenting cells. MPD-1 enables dual-trigger payload release, amplifies cytotoxicity via in situ feedback, and selectively delivers payload to tumor microenvironments via enhanced albumin metabolism and macropinocytosis. MPD-1 exhibits antitumor efficacy in mouse colorectal cancer models. MPD-1 can be used for the research of colorectal cancer .
Ac-RKAA-PABC-MMAE TFA is a Drug-Linker Conjugates for ADC. Ac-RKAA-PABC-MMAE TFA consists of the ADC Cytotoxin MMAE (HY-15162) and a linker. Ac-RKAA-PABC-MMAE TFA can be used for synthesis of ADCs .
SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL pro protease (b. SARS-CoV-2 3CL pro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL pro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection .
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsinB and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
L-Arginine-7-amido-4-methylcoumarin (Arginine 4-methyl-7-coumarylamide) hydrochloride is a specific substrate of cathepsin H but not for cathepsins L and B .
Poly-L-glutamic acid sodium salt (MW 30000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 15000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 7500) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 60000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsinB and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
Poly-L-Glutamic acid (MW 100000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-Glutamic acid is an ideal tumor-targeting polymer carrier. Poly-L-Glutamic acid can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 120000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 3000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Poly-L-glutamic acid sodium salt (MW 45000) is a synthetic polypeptide with biocompatibility, biodegradability and non-immunogenicity. Poly-L-glutamic acid sodium salt is an ideal tumor-targeting polymer carrier. Poly-L-glutamic acid sodium salt can be hydrolyzed by cathepsinB during metabolic decomposition .
Z-Arg-Arg-AMC hydrochloride is a highly selective fluorescent CathepsinB substrate. Z-Arg-Arg-AMC hydrochloride can be hydrolyzed by CathepsinB to produce a fluorescent product for enzyme activity detection .
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, cathepsin K, 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-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsinB activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsinB and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
Arg-Arg-AMC acetate is the acetate salt form of Arg-Arg-AMC (HY-P4340). Arg-Arg-AMC acetate is a fluorescent substrate for cathepsinB and used in the cathepsinB activity assay .
Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
Hepcidin-1 (mouse) is an endogenous peptide hormone involved in the regulation of iron homeostasis. Hepcidin-1 (mouse) upregulates mRNA levels of TRAP, cathepsin K, 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 .
CBP-1018 is a PDC (peptide-drug conjugate) formed by conjugating Monomethyl auristatin E (HY-15162) to a dual-targeting ligand of FLOR1/PSMA (prostate-specific membrane antigen) via a linker (HY-78738). CBP-1018 binds to FLOR1 and prostate-specific membrane antigen (PSMA). CBP-1018 is applicable to the research of solid tumors and metastatic castration-resistant prostate cancer .
Z-Arg-Arg-βNA acetate is a sensitive dipeptide substrate of the protease CathepsinB and resistant to proteases H and L. Z-Arg-Arg-βNA acetate can serve as an important tool for distinguishing non-CathepsinB type proteins .
Ac-Leu-Val-Lys-Aldehyde is a potent cathepsinB 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 .
Cathepsin D and E FRET Substrate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D .
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 .
Ac-RR-AFC TFA is a CathepsinB fluorogenic substrate (Ex=400 nm, Em=505 nm). CathepsinB activity in cells lysates is determined by measuring cleavage of Ac-RR-AFC TFA and its cleavage occurs at the RR-AFC amide bond. Ac-RR-AFC TFA can be used for activity assays and mechanistic studies on cathepsinB .
Arg-Arg-AMC is a highly selective substrate of CathepsinB. Arg-Arg-AMC can be used to cathepsinB activity assay in cancer cells, while cathepsinB is assocaited with cell invasive and metastatic phenotype in numerous types of cancer .
Abz-HPGGPQ-EDDnp (Cathepsin K 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. Cathepsin K 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 cathepsin K 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 cathepsin K. This peptide is resistant to hydrolysis by cathepsinsB, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
Abz-GIVRAK(Dnp) is the most efficient substrate for cathepsinB and is highly selective for this enzyme among lysosomal cysteine proteases. After Abz-GIVRAK(Dnp) is hydrolyzed, aminoacylbenziminosulfosuccinic acid (Abz-SAS) is released, and dinitrobenzoyl (Dnp) is also released. The product of this hydrolysis reaction, Abz-SAS, is fluorescent under ultraviolet light and can emit a fluorescent signal .
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsinB 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 .
NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsinB. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM) .
Ac-RKAA-PABC-MMAE is a Drug-Linker Conjugates for ADC. Ac-RKAA-PABC-MMAE consists of the ADC Cytotoxin MMAE (HY-15162) and a linker. Ac-RKAA-PABC-MMAE can be used for synthesis of ADCs .
Ac-RKAA-PABC-MMAE TFA is a Drug-Linker Conjugates for ADC. Ac-RKAA-PABC-MMAE TFA consists of the ADC Cytotoxin MMAE (HY-15162) and a linker. Ac-RKAA-PABC-MMAE TFA can be used for synthesis of ADCs .
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 .
3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC50, 6.5 μM; Ki, 19.5 μM), with no obvious effect on cathepsinB .
Dibenzyl trisulfide (DTS) is an active ingredient that can be isolated from Petiveria alliacea L.. Dibenzyl trisulfide inhibits cell proliferation and migration. Dibenzyl trisulfide decreased the mRNA and protein expression of BAK-1 and LTA. Dibenzyl trisulfide induces lysosomal membrane permeabilization and cathepsinB release .
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 .
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 .
Cathepsin B Protein, Mouse (HEK293, His) is an approximately 32-50 kDa Cathepsin B protein with a His-flag. Cathepsin B is an enzymatic protein belonging to the peptidase C1 family.
Cathepsin B is a lysosomal cysteine protease that plays a role in intracellular protein catabolism. Cathepsin B mediates JNK signaling pathway to regulate the migration of glioma initiation cells. Cathepsin B is involved in the pathology of chronic inflammatory diseases of the airway and joints, as well as cancer and pancreatitis. Cathepsin B Protein, Rat (HEK293, His) is the recombinant rat-derived Cathepsin B protein, expressed by HEK293 , with C-His labeled tag.
Cathepsin B Protein, Human (HEK293, His) functions in intracellular protein catabolism and in certain situations may also be involved in other physiological processes, such as processing of antigens in the immune response, hormone activation and bone turnover.
Cathepsin H Protein, Mouse (HEK293, His) is an approximately 36-40 kDa cathepsin H protein with a His-flag. Cathepsin H is a lysosomal cysteine protease of the papain family.
Cathepsin B Protein, a thiol protease, is crucial for intracellular protein degradation, cleaving matrix extracellular phosphoglycoprotein MEPE. It's implicated in solubilizing cross-linked TG/thyroglobulin in the thyroid follicle lumen. Associated with tumor invasion and metastasis, Cathepsin B signifies potential relevance in cancer-related pathways. Cathepsin B Protein, Human (L26V, HEK293) is the recombinant human-derived Cathepsin B protein, expressed by HEK293 , with L26V mutation.
Cathepsin B Protein, a thiol protease, is crucial for intracellular protein degradation, cleaving matrix extracellular phosphoglycoprotein MEPE. It's implicated in solubilizing cross-linked TG/thyroglobulin in the thyroid follicle lumen. Associated with tumor invasion and metastasis, Cathepsin B signifies potential relevance in cancer-related pathways. Cathepsin B Protein, Human (L26V, HEK293, His) is the recombinant human-derived Cathepsin B protein, expressed by HEK293 , with C-His labeled tag and L26V mutation.
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 cathepsinB, and releases active diABZI-amine via cathepsinB-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 .
DBCO-PEG4-Val-Cit-PAB-PNP is a cleavable ADC linker. The Val-Cit will specifically be cleaved by CathepsinB. PNP can be substituted by amine-containing payload. DBCO enable click chemistry with azide molecules.
DBCO-PEG4-Val-Ala-PAB-PNP is a cleavable ADC linker. The Val-Ala linkers can be cleaved by CathepsinB. The DBCO groups is commonly used for Click Chemistry reactions. PEG spacer improves the compound's aqueous solubility. PNP is a good leaving group.
DBCO-PEG3-Glu-VC-PABC-MMAF (compound s19b) is a drug-linker conjugate for ADC by using the tubulin inhibitor, MMAF (HY-15579), linked via cathepsin cleavable DBCO-PEG3-Glu-VC-PABC. DBCO-PEG3-Glu-VC-PABC-MMAF can be used in the synthesis of antibody-drug conjugates (ADCs) .
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 cathepsinB enzyme activity .
hCAXII-IN-10 (Compound 18b) is a dual inhibitor of human carbonic anhydrase isoform XII (hCAXII) and cathepsinB, with a Ki value of 2.2 nM. hCAXII-IN-10 can inhibit the role of hCAXII in providing tumors with a pH microenvironment conducive to tumor growth, and is expected to be used in the study of tumor diseases .
DBCO-PEG4-Val-Ala-PAB is a cleavable ADC linker. The Val-Ala linkers can be cleaved by CathepsinB. The DBCO groups is commonly used for Click Chemistry reactions. PEG spacer improves the compound's aqueous solubility.
Azido-PEG8-Amido-Val-Cit-PAB is a cleavable ADC linker. The Val-Cit will specifically be cleaved by CathepsinB. As this enzyme is only present in the lysosome, the ADC payload will be released only in the cell. Azido will react with DBCO, BCN or other alkyne groups through click chemistry. PEG spacer increases aqueous solubility. Reagent grade, for research purpose.
TML-2Cl is a dichloro-modified trimethyl lock adapter for antibody-drug conjugates and payload releaser.TML-2Cl undergoes 1,6-elimination followed by rapid self-cyclization to facilitate release of the payload Exatecan after cathepsinB cleavage of the associated linker.TML-2Cl exhibits high stability when conjugated to a drug and high intrinsic hydrophobicity.TML-2Cl can be used for the research of gastric carcinoma .
Sgc8c-M is a PTK7-targeted aptamer-drug conjugate (ApDC). Sgc8c-M is composed of the classic PTK7-specific aptamer Sgc8c, a cathepsinB (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 .
MG-101 (GMP) (Calpain inhibitor I (GMP)) is MG-101 (HY-18964) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsinB and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer .
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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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