Proteases

Items 451-500 of 1366

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  1. 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.
  2. 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.
  3. 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.
  4. p32-kinase activator

    D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
  5. HCV NS5B polymerase inhibitor

    VCH-916 is a novel nonnucleoside HCV NS5B polymerase inhibitor.
  6. gamma-secretase modulator

    Flurizan is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits γ-secretase activity.
  7. Cathepsin K inhibitor

    L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor.
  8. Nek2 inhibitor

    MBM-17 (compound 42c) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 3 nM.
  9. Thrombin inhibitor

    Ximelagatran is an anticoagulant that has been investigated extensively as a replacement for warfarin that would overcome the problematic dietary, drug interaction, and monitoring issues associated with warfarin therapy.
  10. Nek2 inhibitor

    MBM-55 (compound 42g) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM.
  11. HIV protease inhibitor

    Fosamprenavir is a prodrug of amprenavir, an inhibitor of human immunodeficiency virus (HIV) protease.
  12. Caspase-6 inhibitor

    Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability.
  13. Caspase-2 inhibitor

    Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes.
  14. PPP1R15A inhibitor

    Sephin1 is a selective inhibitor of stress-induced PPP1R15A and targets disease associated with accumulation of misfolded protein.
  15. GCP-II inhibitor

    2-MPPA is a selective glutamate carboxypeptidase II (GCP-II) inhibitor used in the treatment of neurological disorders associated with excessive activation of glutamatergic systems. Attenuates glutamate transmission resulting in the relief of neuropathic pain.
  16. SHIP1 Inhibitor

    3AC is a cell-permeable, selective inhibitor of SHIP1 polyphosphatase activity toward PIP3 (IC50 = 10 μM), but has no effect on SHIP2 or PTEN activity on PIP3.
  17. MMP inhibitor

    4-epi-Chlortetracycline Hydrochloride is a tetracycline derivative that acts as a metalloproteinase (MMP) inhibitor, used in treating tissue destructive diseases and cancer
  18. matrix metalloproteinase-13 (MMP-13) inhibitor

    T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes.
  19. HIV-1 Vif inhibitor

    RN-18 is a HIV-1 viral infectivity factor (HIV-1 Vif) inhibitor with an IC50 of 6 μM in nonpermissive H9 cells.
  20. DHODH inhibitor

    Vidofludimus is a novel orally active and potent DHODH inhibitor.
  21. Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
  22. PP1 inhibitor

    Tautomycetin induces apoptosis by inactivating Akt through a PP1-independent signaling pathway in human breast cancer cells.
  23. aldose reductase inhibitor

    Tolrestat is an aldose reductase inhibitor[1] which was approved for the control of certain diabetic complications.
  24. HCV Polymerase Inhibitor

    Setrobuvir (ANA-598) is a direct-acting antiviral or DAA, is a non-nucleoside inhibitor of the HCV RNA polymerase
  25. alpha-glucosidase I inhibitor

    Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection.
  26. Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.
  27. MMP-3 inhibitor

    MMP3 inhibitor 1 is a potent and highly selective MMP-3 inhibitor with an IC50 of 1 nM.
  28. HIV-1 RT inhibitor

    Trovirdine inhibits HIV-1 RT with an IC50 of 7 nM when employing heteropolymeric primer/template (oligo-DNA/ribosomal RNA)and dGTP as substrate.
  29. Gamma-secretase modulator

    TC-E 5006 is a gamma-secretase modulator. Reduces Aβ42 levels in vitro (EC50 = 390 nM) and in vivo.
  30. Cysteine Protease inhibitor

    E-64 is an irreversible and selective cysteine protease inhibitor with IC50 of 9 nM for papain.
  31. Cysteine Protease inhibitor

    Loxistatin Acid, a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
  32. MTP inhibitor

    Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.
  33. Neutrophil elastase inhibitor

    ZD-0892 is a selective and potent inhibitor of a neutrophil elastase with Kis of 6.7 and 200 nM for human neutrophil elastase and porcine pancreatic elastase, respectively.
  34. DPP-4 inhibitor

    Omarigliptin (MK-3102) is a competitive, reversible inhibitor of DPP-4 (IC50 = 1.6 nM, Ki = 0.8 nM). It is highly selective over all proteases tested (IC50 > 67 μM), including QPP, FAP, PEP, DPP8, and DPP9 and has weak ion channel activity (IC50 > 30 μM at IKr, Caγ1.2, and Naγ1.5).
  35. DPP-4 inhibitor

    Alogliptin Benzoate is a dipeptidyl-peptidase-4 (DPP 4) inhibitor
  36. DPP-4 inhibitor

    Trelagliptin is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed for the treatment of type 2 diabetes (T2D).
  37. MMP inhibitor

    GM 6001 is a potent, reversible broad spectrum inhibitor of zinc-containing proteases, including matrix metalloproteinases (MMPs).
  38. dual TACE/MMPs inhibitor

    Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) .
  39. KHK inhibitor

    KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
  40. synthetic thrombin inhibitor

    Inogatran (H-314-27) is a synthetic thrombin inhibitor, developed for the possible treatment and prophylaxis of arterial and venous thrombotic diseases.
  41. caspase 1 inhibitor

    ML132 (NCGC 00185682) is a potent and selective caspase 1 inhibitor with an IC50 of 0.316 nM.
  42. cathepsin K inhibitor

    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.
  43. DPP-IV inhibitor

    Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV).
  44. DPP4 inhibitor

    Dutogliptin (PHX-1149 free base) is an orally available, potent, and selective dipeptidyl peptidase-4 (DPP4) inhibitor for the treatment of type 2 diabetes mellitus.
  45. indirect thrombin inhibitor

    Odiparcil (SB-424323) is indirect thrombin inhibitor that exerts its anticoagulant effect through activation of antithrombin II (heparin cofactor II) .
  46. HCV RNA replication inhibitor

    PSI-7976 is the isomer of PSI-7977. PSI-7977 is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
  47. HCV RNA replication inhibitor

    Sofosbuvir impurity C is the less active impurity of Sofosbuvir, Sofosbuvir is an active inhibitor of HCV RNA replication in the HCV replicon assay, demonstrates potent anti-hepatitis C virus (HCV) activity.
  48. HCV RNA replication inhibitor

    Sofosbuvir impurity A, an diastereoisomer of sofosbuvir, is the impurity of sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
  49. ACDase inhibitor

    LCL521 dihydrochloride (1,3DMG-B13 dihydrochloride) is an acid ceramidase (ACDase) inhibitor.
  50. ketohexokinase (KHK) inhibitor

    KHK-IN-1 hydrochloride is a potent ketohexokinase (KHK) inhibitor with IC50 of 12 nM, interacts with Asp-27B in the ATP-binding region of KHK.

Items 451-500 of 1366

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