Proteases

Items 501-550 of 1366

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  1. PP2A activator

    (1S,2S,3R)-DT-061 is an enantiomer of DT-061. DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis.
  2. NAE inhibitor

    TAS4464 (hydrochloride) is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  3. HCV NS5B polymerase inhibitor

    NM107 (2'-C-Methylcytidine) is an nucleoside inhibitor of the hepatitis C virus (HCV) NS5B polymerase, the EC50 of NM107 in the wild-type replicon cells is 1.85 μM.
  4. HCV NS5B polymerase inhibitor

    PSI-6206 13CD3 is the deuterium labeled PSI-6206. PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase.
  5. transglutaminase 2 (TGase) inhibitor

    GK921 is a transglutaminase 2 (TGase) inhibitor with an IC50 of 7.71 μM for human recombinant TGase 2.
  6. dual specificity phosphatase inhibitor

    BCI hydrochloride ((E)-BCI hydrochloride) is an allosteric inhibitor of dual specificity phosphatase (DUSP).
  7. thrombin inhibitor

    Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity.
  8. DPP4 inhibitor

    DBPR108 is a potent, selective, and orally bioavailable dipeptide-derived inhibitor of DPP4 with IC50 of 15 nM; no inhibition on DDP8 and DPP9.
  9. DPP4 inhibitor

    Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).
  10. PTB1B inhibitor

    MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTB1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
  11. proteasome inhibitor

    (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
  12. FBPase inhibitor

    MB07803 is an orally available prodrug of a potent, noncompetitive inhibitor (MB07729) of fructose 1,6-bisphosphatase (FBPase), with EC50 of 140 nM and t1/2 of 7.6±2.9 h.
  13. FBPase inhibitor

    MB-07729 is a potent fructose 1,6-bisphosphatase (FBPase) noncompetitive inhibitor with IC50 values of 31, 121, and 189 nM for human, monkey, and rat, respectively.
  14. HNE inhibitor

    GW-311616 is a potent, orally bioavailable, long duration and selective human neutrophil elastase (HNE) inhibitor with IC50 value of 22 nM and Ki value of 0.31 nM.
  15. substrate for aminopeptidase

    H-β-Ala-AMC TFA is a substrate for aminopeptidase.
  16. ADAM17 inhibitor

    GW280264X is an ADAM17 inhibitor.
  17. PLD1/PLD2 dual inhibitor

    ML299 (VU0463568) is a dual inhibitor of PLD1 and PLD2 with IC50 of 6 nM and 20 nM, respectively.
  18. depalmitoylase inhibitor

    JCP174 is a depalmitoylase inhibitor that enhances Toxoplasma host-cell invasion by targeting TgPPT1.
  19. pan-PHLPP inhibitor

    NSC-45586 is a pan-PHLPP inhibitor selective for PHLPP1 and PHLPP2.
  20. CP4H1 inhibitor

    PythiDC is a selective inhibitor of collagen prolyl 4-hydroxylase.
  21. aldose reductase inhibitor

    Ponalrestat, also known as MK-538, is an aldose reductase inhibitor.
  22. inhibitor of hepatitis C virus (HCV)

    HZ-1157 is an inhibitor of hepatitis C virus (HCV) with inhibitory activities toward HCV NS3/4A protease.
  23. Dihydroorotate Dehydrogenase (DHODH) inhibitor

    ASLAN003 is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme.
  24. DDHD2 inhibitor

    KLH45 is a potent and selective DDHD2 inhibitor, with an IC50 of 1.3 nM.
  25. Anti-ulcer agent

    Cetraxate (DV-1006) Hydrochloride (HCl) is a mucosal protective agent and an anti-ulcer drug candidate. Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma.
  26. proteinase inhibitor

    FOY 251, an anti-proteolytic active metabolite Camostate, acts as a proteinase inhibitor. FOY 251 inhibits SARS-CoV-2 infection in cells assay.

  27. LMPTP inhibitor

    LMPTP INHIBITOR 1 (dihydrochloride) is a selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP), with an IC50 of 0.8 μM LMPTP-A.
  28. DD1

    proteasome inhibitor

    DD1 is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.
  29. activator of SHIP-1

    AQX-016A is a potent activator of SHIP-1 that induces apoptosis of the cancer cell lines in vitro in both a time and dose dependant manner.
  30. ketohexokinase (KHK) inhibitor

    PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor.
  31. Tomatine is an glycoalkaloid that occurs in the extract of leaves of wild tomato plants. It has been found to inhibit the growth of various fungi and bacteria. It is used as a precipitating agent for steroids.
  32. antioxidant

    2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.
  33. serine proteases inhibitor

    Benzamidine hydrochloride is an reversible competitive inhibitor of trypsin-like serine proteases, with Kis of 97 ?M, 21 ?M, 20 ?M and 110 ?M for uPA, trypsin, tryptase and factor Xa, respectively.
  34. uPA inhibitor

    UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin).
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. human cathepsin L inhibitor

    Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L.
  40. human neutrophil elastase inhibitor

    Lodelaben is a human neutrophil elastase inhibitor with an IC50 and Ki of 0.5 and 1.5 μM, respectively.
  41. uPA system inhibitor

    UKI-1 is a novel synthetic inhibitor of the urokinase-type plasminogen activator system.
  42. PGAM1 inhibitor

    PGMI-004A is a potent phosphoglycerate mutase 1 (PGAM1) inhibitor with an IC50 of 13.1 μM.
  43. Aldose reductase inhibitor

    Sorbinil, is an Aldose reductase inhibitor (ARI).
  44. HCV polymerase inhibitor

    JTK-853 is a novel, non-nucleoside Hepatitis C Virus (HCV) polymerase inhibitor which shows effective antiviral activity in HCV replicon cells with EC50s of 0.38 and 0.035 ?M in genotype 1a H77 and 1b Con1 strains, respectively.
  45. HNE inhibitor

    BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
  46. MMP inhibitor

    BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  47. anti-secretagogue of PCSK9

    R-IMPP is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
  48. NEP inhibitor

    Candoxatril is a neutral endopeptidase (NEP) inhibitor.
  49. NS4A antagonist

    ACH-806 is an NS4A antagonist which can inhibit Hepatitis C Virus (HCV) replication with an EC50 of 14 nM.
  50. MMP inhibitor

    XL-784 is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1, MMP-2, MMP-3, MMP-8, MMP-9, MMP-13 respectively.

Items 501-550 of 1366

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