Proteases

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  1. dual-specificity phosphatase 6 (DUSP6) inhibitor

    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  2. proteasome-associated deubiquitinating enzymes inhibitor

    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity.
  3. anticancer agent

    5,7,4'-Trimethoxyflavone is isolated from Kaempferia parviflora (KP) that is a famous medicinal plant from Thailand. 5,7,4'-Trimethoxyflavone induces apoptosis, as evidenced by increments of sub-G1 phase, DNA fragmentation, annexin-V/PI staining, the Bax/Bcl-xL ratio, proteolytic activation of caspase-3, and degradation of poly (ADP-ribose) polymerase (PARP) protein.5,7,4'-Trimethoxyflavone is significantly effective at inhibiting proliferation of SNU-16 human gastric cancer cells in a concentration dependent manner.
  4. antioxidant agent

    Rosamultin is a 19 α-hydroxyursane-type triterpenoid isolated from Potentilla anserina L. Rosamultin has inhibitory effects against HIV-1 protease. Rosamultin has the potential for treating H2O2-induced oxidative stress injury through its antioxidant and antiapoptosis effects.
  5. human cathepsin L inhibitor

    Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L.
  6. CNS penetrant Aldose Reductase inhibitor

    AT-007 is an orally active central nervous system (CNS) penetrant Aldose Reductase inhibitor for treatment of Galactosemia with an IC50 value of 100 pM. AT-007 reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.
  7. uPA inhibitor

    ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
  8. tyrosine kinase signal transduction modulator

    SU 4942 is a tyrosine kinase signal transduction modulator, targeting VEGF and ECGF.
  9. type 1 (SR-BI) inhibitor

    BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor.
  10. 6-Diazo-5-oxo-L-nor-Leucine is a glutamine antagonist that shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 

  11. Pep2-8 is a PCSK9 inhibitor with a binding KD of 0.7 μM and an IC50 of 1.4 μM.
  12. D-3
    D-3, a phosphorpeptide, is an efficient, simple, and specific iPSC-eliminating agent.
  13. Z-Gly-Pro-Arg-AMC hydrochloride a fluorescent trypsin and cathepsin K substrate. Z-Gly-Pro-Arg-AMC hydrochloride can be used to determine trypsin and cathepsin K activity.
  14. γ-Glu-Tyr, a competitive inhibitor of dipeptidyl peptidase-IV (DPP-IV) (IC50=6.77 mM), is a potentially functional component of the type 2 diabetes diet.
  15. Opiorphin, an opioid peptide, is a potent enkephalin-inactivating zinc ectopeptidases in human inhibitor. Opiorphin inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11) with an IC50 value of 11 μM, and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity by activating endogenous opioid-dependent transmission.
  16. HAEGT is the first N-terminal 1-5 residues of glucagon like peptide-1 (GLP-1) peptide, and the sequence is His-Ala-Glu-Gly-Thr. HAEGT acts as a competitive substrate for probing prime substrate binding sites of human dipeptidyl peptidase-IV (DPP-IV) 1, in which the N-terminal His-Ala is catalyzed cleavage by DPP-IV. HAEGT can be used in the research of diabetes, obesity.
  17. Caspase-1 substrate

    Ac-YVAD-pNA is a specific Caspase-1 substrate. Ac-YVAD-pNA can be used to detect Caspase-1 activity. Caspase-1 is a key mediator of inflammatory processes.
  18. Tetrapeptide-30 is a skin-brightening peptide consisting of four amino acids. Tetrapeptide-30 can act as a tyrosinase inhibitor, lightening hyperpigmentation and evening out skin tone by reducing the amount of tyrosinase and inhibiting melanocyte activation.
  19. Irucalantide is kallikrein inhibitor.
  20. MMP-7-IN-2 (comp 16) is a selective MMP7 inhibitor, with an IC50 of 16 nM.
  21. MMP-7-IN-3 is a potent and selective inhibitor of MMP-7. MMP-7-IN-3 suppresses kidney fibrosis progression in a mouse model with unilateral ureteral obstruction.
  22. Pre-mRNA Splicing Activity Modulator

    Hinokiflavone is a naturally occurring biflavonoid isolated from plants, recognized as a novel modulator of pre-mRNA splicing. It exhibits diverse biological activities, including anti-inflammatory, antitumor, and antiviral effects. Mechanistically, Hinokiflavone acts as a potent inhibitor of matrix metalloproteinases (MMPs) and suppresses the virulence of methicillin-resistant Staphylococcus aureus (MRSA) by targeting caseinolytic protease P (ClpP) with an IC₅₀ of 34.36 µg/mL. In cancer models, Hinokiflavone triggers apoptosis through a reactive oxygen species (ROS)-dependent, mitochondria-mediated pathway and suppresses tumor cell migration and invasion. Additionally, it functions as a SUMO protease inhibitor, effectively blocking sentrin-specific protease 1 (SENP1) activity.
  23. CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane compound that exhibits antitumor activity in pancreatic cancer models by inhibiting Ras activation and downstream ERK1/2 signaling. It is also a potent inhibitor of zinc-dependent matrix metalloproteinases (MMPs), with IC₅₀ values ranging from 2.0 to 69 μM. Additionally, CMC2.24 has therapeutic potential in osteoarthritis, where it restores cartilage homeostasis and reduces chondrocyte apoptosis through modulation of the NF-κB/HIF-2α pathway.
  24. COX-2/MMP-7/TLR4 Inhibitor

    Isofraxidin is a coumarin compound derived from *Acanthopanax senticosus* that exhibits anti-invasive and anti-inflammatory properties. It inhibits MMP-7 expression and suppresses cell invasion in human hepatoma cells by reducing ERK1/2 phosphorylation. Isofraxidin also downregulates the expression of iNOS and COX-2 and inhibits the formation of the TLR4/myeloid differentiation protein-2 (MD-2) complex.
  25. NF-kB inhibitor

    SM-7368 is a potent NF-κB inhibitor that acts downstream of MAPK p38 activation. It suppresses TNF-α-induced upregulation of MMP-9 and is suitable for research on chemotherapeutic strategies targeting TNF-α-mediated tumor invasion and metastasis.
  26. MMP-9 inhibitor

    MMP-9-IN-1 is a selective inhibitor of matrix metalloproteinase-9 (MMP-9) that specifically targets the hemopexin (PEX) domain of MMP-9, without affecting other MMP family members.
  27. MMP Inhibitor/PPARα Agonists

    Auraptene is an orally active geranyloxycoumarin compound naturally found in plants of the *Brassicaceae* family. It exhibits a wide range of biological activities, including antibacterial, anti-pathogenic, antioxidant, anti-tumor, and neuroprotective effects. Auraptene has shown therapeutic potential in the management of various chronic conditions such as hypertension and cystic fibrosis, making it a valuable compound for pharmacological and nutraceutical research.
  28. Triolein is a symmetric triacylglycerol composed of three oleic acid molecules esterified to glycerol. It exhibits strong antioxidant and anti-inflammatory properties and has been shown to reduce the upregulation of matrix metalloproteinase-1 (MMP-1), a key enzyme involved in tissue remodeling and inflammation. These activities make triolein a compound of interest in research related to inflammatory diseases and oxidative stress.
  29. Caspase-1 inhibitor

    Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective, irreversible inhibitor of caspase-1 (also known as IL-1β converting enzyme, ICE). It exhibits potent neuroprotective and anti-inflammatory effects by suppressing the expression of proinflammatory cytokines IL-1β and IL-18. Ac-YVAD-cmk also inhibits pyroptosis, a form of inflammatory cell death, making it a valuable tool for studying inflammation-related diseases and neurodegenerative disorders.
  30. Papain is a cysteine protease belonging to the peptidase C1 family, derived from the latex of the papaya (*Carica papaya*). It is widely used across various industries, including food processing (as a meat tenderizer), pharmaceuticals (for wound debridement and anti-inflammatory formulations), textiles (for fabric treatment), and cosmetics (for exfoliation and skin care products).
  31. Hydrangenol is an orally active antiphotoaging compound isolated from *Hydrangea serrata* leaves. It prevents wrinkle formation by downregulating matrix metalloproteinases (MMPs) and inflammatory cytokines, while upregulating moisturizing factors and antioxidant gene expression, making it a promising agent for skin health and anti-aging research.
  32. Cathepsin L inhibitor

    Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific inhibitor of cathepsin L (CTSL), a lysosomal cysteine protease involved in protein degradation and various pathological processes. It is commonly used as a tool compound in studies of CTSL-related functions and diseases.
  33. SHP2 inhibitor

    Migoprotafib (GDC-1971; compound 199) is a selective SHP2 inhibitor that suppresses the MAPK/ERK signaling pathway. It exhibits antitumor activity and is under investigation for its potential in targeting SHP2-driven cancers.
  34. PGAM1 inhibitor

    HKB99 is an allosteric inhibitor of phosphoglycerate mutase 1 (PGAM1) that induces apoptosis and suppresses cell migration by inhibiting the formation of invasive pseudopodia. It increases oxidative stress, activates the JNK/c-Jun pathway, and downregulates AKT and ERK signaling. HKB99 is a promising compound for the study of non-small cell lung cancer (NSCLC).
  35. α-Amyrin is an orally active pentacyclic triterpenoid that activates the ERK and GSK-3β signaling pathways. It is studied for its potential in treating metabolic syndrome induced by a high-fructose diet and cognitive dysfunction associated with reduced cholinergic neurotransmission.
  36. Endoplasmic Reticulum Stress Inhibitor

    Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects.
  37. ADAM17 inhibitor

    JG26 is a potent ADAM inhibitor with IC50 values of 12 nM for ADAM8, 1.9 nM for ADAM17, and 150 nM for ADAM10. It also inhibits MMP-12 with an IC50 of 9.4 nM. JG26 suppresses AngII-induced EGFR transactivation and ERK activation, upregulates ACE2 expression, inhibits CD23 shedding, and reduces SARS-CoV-2 infection. Additionally, JG26 demonstrates anti-metastatic effects in colorectal cancer and holds research potential in Hodgkin lymphoma and vascular diseases.
  38. mGluR5 allosteric modulator

    CDPPB is a selective, orally active allosteric modulator of the metabotropic glutamate receptor 5 (mGluR5). It enhances AKT and ERK1/2 signaling and upregulates BDNF mRNA expression. CDPPB also inhibits caspase-3 activation and mitigates mitochondrial dysfunction, demonstrating therapeutic potential in improving cognitive impairment, depression, and Huntington’s disease.
  39. HIV-1 protease/PTP1B inhibitor

    Isosinensetin is a bioactive flavonoid compound with diverse pharmacological properties. It acts as a dual inhibitor of HIV-1 protease and protein tyrosine phosphatase 1B (PTP1B), with an IC₅₀ of 2.61 µM and a Kᵢ of 0.92 µM for PTP1B, indicating its potential in antiviral and metabolic disease research. Additionally, isosinensetin inhibits P-glycoprotein (P-gp) activity in MDR1-MDCKII cells, suggesting its utility in overcoming multidrug resistance. Isosinensetin exhibits multiple therapeutic effects, including anti-tumor, anti-viral, anti-inflammatory, and antioxidant activities. These properties support its application in the research of various conditions such as cancer, chronic inflammation, osteoporosis, diabetes, and infectious diseases.
  40. Phosphatase inhibitor

    β-Glycerophosphate disodium salt pentahydrate is a bioactive endogenous metabolite and a widely used phosphatase inhibitor. It plays a critical role in promoting and sustaining osteoblast differentiation, supporting mineral metabolism, and modulating cellular signal transduction pathways. In tissue engineering and drug delivery, it is commonly utilized as a component in the formation of heat-sensitive hydrogels due to its thermoresponsive properties. Additionally, β-glycerophosphate disodium salt accelerates calcification in vascular smooth muscle cells, making it a valuable tool for studying vascular calcification and related pathologies.
  41. COX-1/HDAC/Tyrosinase Inhibitor

    Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders.
  42. Tyrosinase Inhibitor

    Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells.
  43. PTPN2 Degrader

    PROTAC PTPN2 degrader-1 is an effective degrader of the protein tyrosine phosphatase PTPN2. This compound facilitates target protein degradation through the proteasome pathway, enabling the modulation of cellular signaling related to cancer and metabolic diseases. Its application in research may provide insights into the therapeutic potential of targeting PTPN2 in various disease contexts.
  44. Tumor Promoter

    Nodularin is a potent hepatotoxin, tumor promoter, and protein phosphatase inhibitor.
  45. HIV Protease Inhibitor

    Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
  46. PTPN1/PTPN2 Inhibitor

    Osunprotafib (ABBV-CLS-484) is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.
  47. Cysteine Residues Modifier

    N-Ethylmaleimide (NEM) is a potent chemical reagent that irreversibly alkylates free sulfhydryl groups, specifically targeting cysteine residues. This compound serves as an effective inhibitor of cysteine proteases and significantly affects phosphate transport in mitochondria. With an IC50 value of 6.3 μM, N-Ethylmaleimide is valuable for modifying cysteine residues in proteins and peptides, making it an essential tool in biochemical research and studies involving protein functionality and structure.
  48. MMP Inhibitor

    o-Phenanthroline monohydrate is a potent MMP inhibitor that acts by chelating divalent metal ions, particularly iron (Fe2+), forming a stable red complex that absorbs light maximally at 510 nm. This compound has demonstrated the ability to prevent chromosomal aberrations in cells exposed to streptozotocin, thereby highlighting its significance in cellular and molecular biology research. It is widely utilized in studies investigating metalloproteinases and their role in various biological processes and disease states.
  49. Glycosaminoglycan

    Hyaluronic acid sodium, also known as sodium hyaluronate, is a glycosaminoglycan that plays a crucial role in the extracellular matrix (ECM). This biopolymer is involved in key biological activities such as cell proliferation, tissue remodeling, and angiogenesis, particularly in the context of digestive cancers. Hyaluronic acid sodium is implicated in tumor cell growth and migration, and it activates the PI3K-Akt signaling pathway. This reagent can also be utilized in research related to joint diseases, wound healing, and as a drug delivery system to enhance the efficacy of therapeutics in cancer research.
  50. Caspase Inhibitor

    Z-VA-DL-D-FMK is an irreversible caspase inhibitor that targets and binds to caspases, modulating their activity. This compound enhances the sensitivity of TNF-α, thereby influencing apoptotic pathways. Additionally, Z-VA-DL-D-FMK has been shown to activate HIV replication in infected T cells, such as ACH-2, making it valuable for studies in cell signaling and viral reactivation.

Items 501-550 of 1361

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