Proteases

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  1. proteasome β1i (LMP2) subunit inhibitor

    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
  2. HIV capsid inhibitor

    CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
  3. GAC inhibitor

    UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.
  4. PPP1R15B inhibitor

    Raphin1 is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B).
  5. Thrombin inhibitor

    Melagatran is a direct and orally active inhibitor of thrombin, without interacting with any other enzymes in the coagulation cascade or fibrinolytic enzymes aside from thrombin.
  6. HIV infection inhibitor

    HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
  7. Cysteine protease inhibitor

    LHVS is a potent, non-selective cysteine protease inhibitor. LHVS effectively blocks T. gondii microneme protein secretion (IC50=10 μM), gliding motility, and cell invasion.
  8. PME-1 inhibitor

    ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
  9. LMP2 inhibitor

    KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
  10. CDC25 phosphatase family inhibitor

    BN82002 is a potent, selective and irreversible inhibitor of CDC25 phosphatase family.
  11. ecto-ATPase inhibitor

    ARL67156 trisodium salt is an inhibitor of ecto-ATPase. ARL 67156 is a weak competitive inhibitor of NTPDase1 (CD39), NTPDase3 and NPP1, with Kis of 11, 18 and 12?μM, respectively.
  12. alpains 1 and 2 inhibitor

    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
  13. PTP/PTEN Inhibitor

    bpV(phen) is a potent inhibitor of protein tyrosine phosphatases (PTPs) and PTEN, exhibiting IC50 values of 38 nM, 343 nM, and 920 nM for PTEN, PTP-β, and PTP-1B, respectively. This compound demonstrates significant anti-proliferative effects on the protozoan parasite Leishmania in vitro. Additionally, bpV(phen) enhances the secretion of various chemokines and pro-inflammatory cytokines while promoting a Th1-type immune response characterized by IL-12 and IFNγ production. It also induces apoptosis and exhibits anti-angiogenic and anti-tumor properties, making it valuable for research in cancer and inflammation biology.
  14. Thrombin Inhibitor

    Hirudin is a potent thrombin inhibitor known for its anticoagulant properties. It exhibits significant anti-thrombotic activity and is implicated in therapeutic applications such as wound repair, anti-fibrosis, and anti-tumor responses. Additionally, Hirudin has been explored for its effects on diabetic complications and cerebral hemorrhage, making it a valuable reagent in various research contexts.
  15. Calpain Inhibitor

    Z-LLY-FMK is a potent calpain inhibitor that exhibits significant effects on apoptosis across various cell systems. By inhibiting calpain activity, Z-LLY-FMK has been shown to mitigate intestinal apoptosis following common bile duct ligation and reduce parasite burden in mouse models challenged with Taenia crassiceps cysts. This reagent serves as a valuable tool for research into cysticercosis and the role of calpain in cellular processes.
  16. Tyrosinase Inhibitor

    Aloesin is a potent tyrosinase inhibitor known for its diverse biological activities, including anti-inflammatory effects and ultraviolet protection. Additionally, it exhibits antibacterial properties and has been shown to induce apoptosis in various cancer cell lines, making it a valuable compound for research in ovarian cancer and related studies. Its multifunctional profile provides a broad spectrum of applications in both dermatological and oncology research.
  17. LonP1/ CT-L proteasome inhibitor

    BT317 is a selective inhibitor of mitochondrial Lon peptidase I (LonP1) and the caspase-like (CT-L) activity of the proteasome. This compound has been shown to increase the production of reactive oxygen species (ROS), leading to apoptosis in astrocytoma cells. BT317 exhibits significant antitumor activity, making it a valuable reagent for research in cancer biology and therapeutic applications targeting gliomas.
  18. Proteasome Inhibitor

    YSY01A is a potent proteasome inhibitor that promotes apoptosis in cancer cells, demonstrating IC50 values of 51.0 nM in HEK293T, 9.2 nM in A549, 5.2 nM in MCF-7, 8.9 nM in MGC-803, and 35.4 nM in PC-3M cell lines. This compound effectively disrupts constitutive STAT3 signaling by downregulating gp130 and JAK2 in human A549 lung cancer cells. YSY01A serves as a valuable tool for research in cancer therapy and apoptosis mechanisms.
  19. PTPN2/1 Dual Inhibitor

    PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research.
  20. Proteasome Inhibitor

    Ub4ix is a potent proteasome inhibitor that selectively protects K48-linked ubiquitin chains from deubiquitinating enzymes (DUBs), thereby preventing the degradation of ubiquitin-tagged proteins. This compound has demonstrated significant biological activity, including the reduction of cell viability and induction of apoptosis in HeLa cells, with an IC50 value of 1.6 μM. Ub4ix is a valuable tool for research applications focused on understanding protein homeostasis and the role of the proteasome in cellular processes.
  21. uPA Inhibitor

    UCD38B hydrochloride is a competitive inhibitor of urokinase-type plasminogen activator (uPA) with an IC50 value of 7 μM. This compound exhibits cell permeability and specifically targets intracellular uPA, leading to its mistrafficking into perinuclear mitochondria. This mistrafficking results in a reduction of mitochondrial membrane potential and ultimately promotes the release of apoptotic inducible factor (AIF), thereby inducing apoptosis. UCD38B hydrochloride is useful in research applications focused on cancer biology and therapeutic strategies targeting apoptosis.
  22. Proteasome Inhibitor

    Baceridin is a proteasome inhibitor characterized as a cyclic hexapeptide. Isolated from the culture medium of Epiphytic Bacillus, it disrupts proteasome function, leading to inhibition of cell cycle progression and induction of apoptosis in tumor cells via a p53-independent mechanism. This compound is valuable for cancer research applications, particularly in studies exploring proteasome inhibition and its effects on tumor biology.
  23. Tubulin/MMP Inhibitor

    Tubulin/MMP-IN-2 is a dual inhibitor targeting both tubulin and matrix metalloproteinases (MMPs). It effectively inhibits tubulin polymerization, leading to induced apoptosis in cancer cells. Additionally, Tubulin/MMP-IN-2 demonstrates inhibitory activity against MMP-2, MMP-3, and MMP-9, with IC50 values of 24.95 μM, 31.60 μM, and 22.37 μM, respectively. This compound is valuable for research focused on cancer biology and therapeutic development.
  24. γ-secretase Inhibitor

    Nirogacestat dihydrobromide is a selective, noncompetitive inhibitor of γ-secretase, with a reported IC50 of 6.2 nM. This compound effectively inhibits Notch signaling, making it a valuable tool for studying Notch receptor-dependent cancers while minimizing gastrointestinal toxicity. It is particularly useful in research focused on the role of γ-secretase in cancer biology and therapeutic development.
  25. DHODH Inhibitor

    JNJ-74856665 is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 of 0.396 nM for human DHODH. This compound disrupts pyrimidine synthesis, making it a valuable tool for studying the role of DHODH in various biological processes, including cell proliferation and immune response modulation. JNJ-74856665 has potential applications in research related to autoimmune diseases and cancer therapeutic strategies.
  26. DHODH Inhibitor

    Lapachol is a potent inhibitor of dihydroorotate dehydrogenase (DHODH), demonstrating significant immunosuppressive effects on lymphocytes by disrupting pyrimidine synthesis. This natural naphthoquinone exhibits antitumor properties, inhibiting DNA and RNA synthesis in neoplastic cells. Additionally, Lapachol has shown efficacy against Leishmania, suggesting its potential in parasitological research and therapeutic applications.
  27. DHODH Inhibitor

    AG-636 is a selective and reversible inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 17 nM. This compound demonstrates significant anticancer activity, making it a valuable tool in cancer research and pharmacological studies targeting the de novo pyrimidine synthesis pathway. Its oral bioavailability further enhances its utility in preclinical and clinical studies.
  28. Immunomodulator/DHODH Inhibitor

    Laflunimus is an immunomodulator that primarily functions as an inhibitor of dihydroorotate dehydrogenase (DHODH). This compound effectively suppresses the secretion of immunoglobulins, demonstrating IC50 values of 2.5 µM for IgM and 2 µM for IgG. Additionally, Laflunimus serves as an inhibitor of prostaglandin endoperoxide H synthases (PGHS-1 and PGHS-2), making it valuable for research applications focused on immunosuppression and inflammatory pathways.
  29. Potent DHODH Inhibitor

    DHODH-IN-1 is a potent inhibitor of Dihydroorotate Dehydrogenase (DHODH), exhibiting an IC50 of 25 nM. By targeting the DHODH enzyme, this compound effectively disrupts the pyrimidine biosynthesis pathway, making it a valuable tool for researchers investigating cellular proliferation and metabolic regulation. Its application spans the study of autoimmune diseases, cancer research, and other conditions where modulation of pyrimidine synthesis is critical.
  30. DHODH Inhibitor

    hDHODH-IN-5 is a potent inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 value of 0.91 μM. This compound has been demonstrated to induce differentiation in acute myeloid leukemia cells, highlighting its potential utility in cancer research. hDHODH-IN-5 serves as a valuable tool for investigating the role of DHODH in cellular differentiation and proliferation pathways.
  31. DHODH Inhibitor

    DHODH-IN-14 is a selective inhibitor of dihydroorotate dehydrogenase (DHODH), exhibiting an IC50 of 0.49 μM against rat liver DHODH. This hydroxyfurazan analog of A771726 demonstrates significant potential in the treatment of rheumatoid arthritis. Its inhibitory capacity on DHODH suggests applications in modulating pyrimidine synthesis, providing a valuable tool for research in autoimmune disorders and related therapeutic development.
  32. DHODH Inhibitor

    hDHODH-IN-4 is a selective inhibitor of human dihydroorotate dehydrogenase (DHODH), exhibiting a pIC50 of 7.8 against human recombinant DHODH. This compound effectively inhibits measles virus replication, demonstrated by a pMIC50 of 8.8. As a DHODH inhibitor, hDHODH-IN-4 is valuable for research into viral infections and the modulation of pyrimidine metabolism.
  33. HsDHODH Inhibitor

    hDHODH-IN-3 is a potent inhibitor of human dihydroorotate dehydrogenase (HsDHODH), which plays a critical role in the de novo pyrimidine synthesis pathway. This compound has demonstrated significant antiviral activity, particularly inhibiting measles virus replication with a pMIC50 value of 8.6. hDHODH-IN-3 is particularly valuable for research in virology and metabolic diseases.
  34. hDHODH Inhibitor

    hDHODH-IN-1 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH), an enzyme essential for de novo pyrimidine synthesis. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research in autoimmune diseases and inflammatory conditions. Its mechanism of action allows for exploration in therapeutic applications aimed at modulating immune responses and cellular proliferation.
  35. PfDHODH Inhibitor

    PfDHODH-IN-1 is an inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH). This compound exhibits significant antimalarial activity by disrupting the pyrimidine biosynthesis pathway in the malaria parasite. PfDHODH-IN-1 serves as a valuable tool for research focused on malaria treatment and the exploration of novel therapeutic strategies against Plasmodium falciparum infections.
  36. Rat DHODH Inhibitor

    DHODH-IN-11 is a Leflunomide derivative that functions primarily as a dihydroorotate dehydrogenase (DHODH) inhibitor. This compound demonstrates weak inhibitory activity against DHODH, an essential enzyme in the de novo pyrimidine synthesis pathway. It is particularly relevant for research in cellular metabolism and immunology, providing insights into therapeutic strategies for autoimmune disorders and certain cancers.
  37. Caspase-3/Caspase-7 Inhibitor

    Ac-ESMD-CHO is an inhibitor of caspase-3 and caspase-7, targeting the proteolytic cleavage of the caspase-3 precursor peptide (CPP32) at the Glu-Ser-Met-Asp (ESMD) site. This compound is crucial for studying apoptosis and cellular signaling mechanisms by selectively modulating caspase activity. Its application extends to research areas involving cell death regulation and disease models where caspase-mediated pathways play a pivotal role.
  38. Tyrosinase Inhibitor

    Dalbergioidin is a potent tyrosinase inhibitor that demonstrates significant activity through its ability to modulate enzymatic processes related to melanin biosynthesis. This compound has been shown to ameliorate renal fibrosis induced by doxorubicin by suppressing the TGF-β signaling pathway. Dalbergioidin's potential applications include studies focused on skin disorders and the regulation of pigmentation.
  39. Calpain/Apoptosis Inhibitor

    AK 295 is a selective calpain inhibitor that modulates apoptosis via a calpain-dependent mechanism. This compound exhibits potent neuroprotective effects and is effective in decreasing myocardial injury by inhibiting calpain activity. AK 295 is suitable for research applications related to infection, inflammation, and a variety of diseases, including cardiovascular conditions and neurological disorders such as stroke and viral myocarditis.
  40. γ-Secretase Inhibitor I

    Z-LLNle-CHO is a γ-secretase inhibitor that effectively disrupts the Akt-mediated pro-survival signaling pathway, leading to caspase activation and ROS-dependent apoptosis. This compound is instrumental in cancer research, particularly in the studies of breast cancer and leukemia, where inhibiting γ-secretase activity may provide insights into therapeutic strategies.
  41. Aldose Reductase Inhibitor

    WJ-39 is a potent orally active inhibitor of aldose reductase (AR), demonstrating significant therapeutic potential. This compound has been shown to mitigate tubular damage in diabetic nephropathy models by activating the PINK1/Parkin signaling pathway, thereby promoting mitophagy and reducing apoptosis. WJ-39 serves as a valuable tool for studying diabetic complications and the underlying mechanisms of kidney injury.
  42. Granzyme B/Caspase-8 Inhibitor

    Ac-IETD-CHO is a potent, reversible inhibitor of granzyme B and caspase-8. By blocking these proteases, Ac-IETD-CHO effectively inhibits Fas-mediated apoptotic cell death, as well as preventing hemorrhage and liver failure. This compound is valuable for research in apoptosis, immune response, and the modulation of cytotoxic T lymphocyte-induced cell death.
  43. Tyrosinase Inhibitor

    AP736 is a potent inhibitor of tyrosinase, exhibiting an IC50 value of 0.9 μM, and demonstrates significant anti-melanogenesis activity in normal human melanocytes with an IC50 of 0.11 μM. By inhibiting the cAMP-PKA-CREB signaling pathway, AP736 effectively reduces the expression of tyrosinase and TRP-1/2, leading to a decrease in microphthalmia-associated transcription factor (MITF) transcripts and proteins. This compound is suitable for investigations into melanogenesis and the underlying mechanisms of hyperpigmentation.
  44. γ-Secretase Inhibitor

    EVP-0015962 is a potent γ-secretase inhibitor that effectively penetrates the blood-brain barrier, exhibiting an IC50 value of 3.9 μM. By modulating the γ-secretase-mediated cleavage of amyloid precursor protein, EVP-0015962 decreases the production of Aβ42 while increasing Aβ38 levels. This compound has demonstrated efficacy in reducing amyloid aggregates, mitigating amyloid plaque formation, and lowering inflammatory markers in mouse models, thereby enhancing cognitive function. EVP-0015962 serves as a valuable tool in Alzheimer's disease research.
  45. γ-secretase Inhibitor

    JNJ-40418677 is a potent orally active inhibitor of γ-secretase, capable of crossing the blood-brain barrier. It effectively inhibits the production of Aβ42 and the activity of NS2B-NS3 protease, with IC50 values of 200 nM and 3.9 μM, respectively. This compound exhibits favorable biological tolerance and is suitable for research applications related to Alzheimer's disease.
  46. γ-secretase Inhibitor

    Sulindac sulfide is a noncompetitive inhibitor of γ-secretase, exhibiting an IC50 of 20.2 μM for γ42-secretase activity. This compound plays a crucial role in research involving Alzheimer's disease and other neurodegenerative conditions by modulating the processing of amyloid precursor protein. Its ability to inhibit γ-secretase makes it a valuable tool for studies focused on reducing amyloid-beta peptide formation and investigating related signaling pathways.
  47. γ-secretase Inhibitor

    ELND 006 is a selective γ-secretase inhibitor that effectively reduces amyloid beta (Aβ) generation while preserving Notch signaling pathways. Developed with a focus on metabolic stability, this compound has shown significant efficacy in lowering Aβ levels both in vitro and in vivo during preclinical studies. ELND 006, alongside its structural analog ELND 007, has advanced into human clinical trials, indicating its potential therapeutic applications in Alzheimer's disease research and treatment.
  48. gamma-Secretase Inhibitor

    Gamma-secretase modulator 6 is a gamma-secretase inhibitor that effectively reduces the secretion of Aβ42 in HEK cells stably expressing amyloid precursor protein (APP), with a pIC50 value of 8.1. This compound plays a crucial role in the study of Alzheimer's disease by modulating gamma-secretase activity, thereby influencing amyloid plaque formation. It is a valuable tool for researchers exploring therapeutic strategies targeting amyloid pathology in neurodegenerative disorders.
  49. γ-secretase/Aβ42 Inhibitor

    Amyloid-β-IN-2 is a selective γ-secretase inhibitor that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 226 nM. This compound demonstrates potential for research applications in Alzheimer's disease and other conditions associated with Aβ deposition. Its ability to modulate γ-secretase activity makes it a valuable tool for studying the mechanisms underlying amyloid-related pathologies.
  50. γ-secretase/Aβ42 Inhibitor

    Amyloid-β-IN-3 is a selective inhibitor of γ-secretase that effectively reduces the secretion of Aβ42 in H4 cells, exhibiting an EC50 value of 148 nM. By modulating γ-secretase catalytic activity, it decreases Aβ42 production and helps mitigate the neurotoxicity associated with amyloid deposition. This compound shows potential for research applications in Alzheimer's disease (AD) studies.

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