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  1. γ-Secretase Inhibitor

    BMS 433796 is a γ-secretase inhibitor with Aβ lowering activity in a transgenic mouse model of Alzheimer's disease.
  2. HCV NS3 protease Inhibitor

    Ciluprevir is a specific and potent peptidomimetic inhibitor of the HCV NS3 protease.
  3. NS3 protease inhibitor

    Narlaprevir is a potent, selective, orally bioavailable NS3 protease inhibitor(Ki=6 nM; EC90=40 nM)
  4. HCV replication inhibitor

    R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).
  5. HCV NS3/4A protease inhibitor

    Voxilaprevir (GS-9857) is a fluorinated macrocyclic hepatitis C virus (HCV) nonstructural protein (NS) 3/4A protease inhibitor with potent in vitro antiviral activity against genotypes 1-6 HCV and broad coverage of NS3/4A protease polymorphisms. GS-9857 improves coverage against commonly encountered NS3 resistance-associated variants (RAVs).
  6. transglutaminase 2 (TG2) inhibitor

    ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, which can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD).
  7. proteasome inhibitor

    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
  8. Nek2 inhibitor

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

    MBM-55 (compound 42g) is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM.
  10. 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
  11. alpha-glucosidase I inhibitor

    Celgosivir is an alpha-glucosidase I inhibitor for the potential treatment of HCV infection.
  12. MTP inhibitor

    Implitapide (AEGR 427) is a microsomal triglyceride transfer protein (MTP) inhibitor.
  13. 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.
  14. KHK inhibitor

    KHK-IN-2 is a potent and selective ketohexokinase (KHK) inhibitor with an IC50 of 0.45 μM.
  15. HCV NS5B polymerase inhibitor

    BI 207127 was a non-nucleoside hepatitis C virus NS5B polymerase inhibitor for the treatment of hepatitis C
  16. SPPL2a inhibitor

    SPL-707 is a potent, selective and orally available signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 80 nM.
  17. HCV NS3/4a inhibitor

    MK-5172 is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants.
  18. HCV NS5A inhibitor

    MK 8742, also known as Elbasvir, is a HCV NS5A inhibitor, which is an all-oral, interferon-free regimen for the treatment of HCV infection.
  19. HCV NS3/4A protease inhibitor

    GS-9451, a novel hepatitis C virus (HCV) nonstructural 3/4a (NS3/4a) protease inhibitor, is highly active in patients infected with HCV genotype 1 (GT 1).
  20. HCV Protease Inhibitor

    Faldaprevir is a hepatitis C virus protease inhibitor.
  21. CPG2 inhibitor

    Carboxypeptidase G2 (CPG2) Inhibitor is a novel Carboxypeptidase G2 (CPG2) Inhibitor, Antitumor agents.
  22. gamma-secretase modulator

    gamma-secretase modulator 3 is a gamma-secretase modulator.
  23. HIV protease inhibitor

    Tipranavir, a nonpeptidic HIV protease inhibitor (NPPI), inhibits the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates.
  24. MMP Inhibitor

    20(R)-Ginsenoside Rh2 is a matrix metalloproteinase (MMP) inhibitor that acts as a cell antiproliferator.
  25. Allosteric IN inhibitor

    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
  26. Atox1/CCS inhibitor

    DC_AC50 is an inhibitor of copper trafficking proteins Atox1 and CCS, resulting in a disruption of cellular copper transport.
  27. γ-Secretase inhibitor

    Z-Ile-Leu-aldehyde is a potent gamma-Secretase inhibitor; Notch signaling inhibitor.
  28. MTP inhibitor

    Lomitapide mesylate(AEGR-733; BMS-201038) is an inhibitor of microsomal triglyceride-transfer protein (MTP) wtih in vitro IC50 of 8 nM.
  29. NAE inhibitor

    ZM223 is a non-sulfamide NEDD8 activating enzyme (NAE) inhibitor that inhibits HCT116 colon cancer cells with an IC50 value of 100 nM.
  30. HIV-1 maturation inhibitor

    GSK3532795, also known as BMS-955176, is a potent, orally active, second-generation HIV-1 maturation inhibitor. CAS: 1392312-45-6 (free base) 2023808-13-9 (HCl) 2023798-97-0 (HCl hydrate) 2097784-79-5 (oxalate)
  31. NEK2 kinase inhibitor

    CMP3a is a NEK2 kinase inhibitor. CMP3a efficiently attenuated GBM growth in a mouse model and exhibited a synergistic effect with radiotherapy. Targeting NEK2 attenuates glioblastoma growth and radioresistance by destabilizing histone methyltransferase EZH2.
  32. insecticidal and anticancer

    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells.
  33. ALP activator

    DIPQUO is an activator of the bone marker alkaline phosphatase (ALP), with an EC50 of 6.27 μM in C2C12 cells. DIPQUO promotes mouse and human osteoblast differentiation via activation of p38 MAPK-β.
  34. NAE inhibitor

    TAS4464 is a highly potent and selective inhibitor of NEDD8 activating enzyme (NAE), with an IC50 of 0.955 nM.
  35. MMP-13 inhibitor

    DB04760 (compound 4) is a potent, highly selective, non-zinc-chelating MMP-13 inhibitor with an IC50 of 8 nM. DB04760 significantly reduces paclitaxel neurotoxicity and has anticancer activity.
  36. MMP inhibitor

    BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  37. Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity. Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation.
  38. γ-secretase modulator

    BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively.
  39. PP2A activator

    SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A.
  40. proteasome β1i (LMP2) subunit inhibitor

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

    CA inhibitor 1 (GS-6207 analog) is a potent HIV capsid inhibitor for HIV inhibition.
  42. 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.
  43. 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.
  44. HIV infection inhibitor

    HIV-1 inhibitor-3 is a HIV infection inhibitor extracted from patent US2018360927.
  45. 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.
  46. 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.
  47. 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).
  48. ADAM17 inhibitor

    KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively.
  49. γ secretase modulator

    BI-1408 is a potent γ secretase modulator with an IC50 of 0.04 μM for Aβ42.
  50. SHIP2 inhibitor

    SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 ?M. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer??s disease.

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