Proteases

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  1. DPP-IV inhibitor

    Talabostat (Val-boroPro; PT100) is an orally active and nonselective dipeptidyl peptidase IV (DPP-IV) inhibitor (IC50 < 4 nM; Ki = 0.18 nM) and the first clinical inhibitor of fibroblast activation protein (FAP) (IC50 = 560 nM).
  2. DPP-4 inhibitor

    Talabostat mesylate is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM.
  3. HCV Protease Inhibitor

    Faldaprevir is a hepatitis C virus protease inhibitor.
  4. Cysteine Protease inhibitor

    Leupeptin hemisulfate is a reversible inhibitor of trypsin-like and cysteine proteases such as calpain.
  5. reversible proteasome inhibitor

    PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.
  6. HIV-1 attachment inhibitor

    BMS-626529 is a potent HIV-1 attachment inhibitor. BMS-663068 is also the phosphonooxymethyl prodrug of BMS-626529 that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells.
  7. Proteasome inhibitor

    ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies.
  8. Neutrophil elastase inhibitor

    Sivelestat is a cell-permeable sulfanilide compound that acts as a potent, substrate-competitive, and highly specific inhibitor of neutrophil elastase (IC50 = 19-49 nM in rat, rabbit, hamster, human, and mouse leukocyte elastase).
  9. Hec1 Inhibitor

    INH6 is a potent Hec1 inhibitor, which specifically disrupts the Hec1/Nek2 interaction and causes chromosome mis-alignment.
  10. angiotensin receptor-neprilysin inhibitor

    LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure.
  11. Cysteine Protease inhibitor

    MG-101 (ALLN) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
  12. metalloendopeptidase inhibitor

    Phosphoramidon Disodium Salt is a metalloendopeptidase inhibitor.
  13. Calpain inhibitor

    PD 151746 is a selective, cell-permeable calpain inhibitor with Ki of 0.26 uM for μ-Calpain, about 20-fold selectivity over m-calpain.
  14. MMP-2/MMP-9 inhibitor

    SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9.
  15. HIV protease inhibitor

    Nelfinavir Mesylate is a potent HIV protease inhibitor with Ki of 2 nM.
  16. aspartic protease inhibitor

    Pepstatin A is a potent aspartic protease inhibitor, and also inhibits HIV replication.
  17. phosphatase inhibitor

    (-)-p-Bromotetramisole Oxalate is a potent and non-specific alkaline phosphatase inhibitor.
  18. Irreversible Cysteine Protease inhibitor

    Z-FA-FMK is an irreversible cysteine protease inhibitor.
  19. CCT007093 is a potent PPM1D (WIP1) inhibitor with IC50 of 8.4 μM.
  20. eIF2α phosphatase inhibitor

    Sal003 is a potent and cell-permeable eIF-2α phosphatase inhibitor.
  21. protein phosphatase inhibitor

    Microcystin-LR is a potent protein phosphatase inhibitor with IC50 of 0.04 nM for PP2A, >40-fold selectivity over PP1.
  22. osteoblast differentiation inducer

    Asperosaponin VI, A saponin component from Dipsacus asper wall, induces osteoblast differentiation through BMP?\2/p38 and ERK1/2 pathway. Asperosaponin ?? inhibits apoptosis in hypoxia-induced cardiomyocyte by increasing the Bcl-2/Bax ratio and decreasing active caspase-3 expression, as well as enhancing of p-Akt and p-CREB.
  23. MMP9 inhibitor

    JNJ0966 is a highly selective MMP-9 zymogen inhibitor with an IC50 of 440 nM.
  24. γ-Secretase Modulator

    NGP-555 is a gamma-secretase modulator with a selective mechanism to reduce Abeta 42 while raising shorter Abeta forms such as Abeta 37 and 38.
  25. DHODH inhibitor

    DSM265 is a long-duration, potent and selective dihydroorotate dehydrogenase (DHODH)) inhibitor.
  26. DUSP26 inhibitor

    F1063-0967 is a novel inhibitor of dual-specificity phosphatase 26 (DUSP26), inducing apoptosis in IMR-32 cell line.
  27. DPPI inhibitor

    AZD7986, also known as INS 1007, is a second generation reversible covalent, potent and selective DPP1 inhibitor potentially for the treatment of chronic obstructive pulmonary disease (COPD) with predicted human PK properties suitable for once daily human dosing.
  28. TNK2 inhibitor

    XMD16-5 is a tyrosine kinase nonreceptor 2(TNK2) inhibitor.
  29. TNK2 Inhibitor

    XMD8-87 is an inhibitor of tyrosine kinase non-receptor 2 (TNK2) with an IC50 value of 1.9 μM
  30. serine hydrolase inhibitor

    AA26-9 is a potent and broad-spectrum serine hydrolase inhibitor.
  31. uPA inhibitor

    UK-371804 is a potent urokinase-type plasminogen activator (uPA) inhibitor.
  32. 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.
  33. 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)
  34. TACE/MMP inhibitor

    TMI-1 is a novel orally active dual inhibitor of ADAM17 (TACE) and MMP.
  35. pan-caspase inhibitor

    MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1, caspase-3, and caspase-6, 7, 8, and 9.
  36. MMP inhibitor

    Iincyclinide, also known as CMT-3 and COL-3, is a MMP inhibitor and a chemically-modified tetracycline with potential antineoplastic activity. Incyclinide inhibits matrix metalloproteinases (MMPs), thereby inducing extracellular matrix degradation, and inhibiting angiogenesis, tumor growth and invasion, and metastasis. This agent also causes mitochondrial depolarization in tumor cells and induces both cellular apoptosis and tissue necrosis.
  37. Calpain inhibitor

    SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly.
  38. HCV NS5A inhibitor

    Velpatasvir, also known as GS-5816, is a potent and selective Hepatitis C virus NS5A inhibitor.
  39. MMP inhibitor

    Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
  40. HCV NS5A inhibitor

    Ombitasvir is a potent inhibitor of the hepatitis C virus protein NS5A, with EC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5, and 366 pM against genotype 6a.
  41. HCV NS3/4A inhibitor

    Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
  42. MMP inhibitor

    Doxycycline monohydrate is an antibiotic and broad-spectrum metalloproteinase (MMP) inhibitor.
  43. Elastase release inhibitor

    Acetylglucosamine or N-acetylglucosamine is potentially for the treatment of irritable bowel syndrome. N-Acetylglucosamine (GlcNAc) is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. GlcNAc has been reported to be an inhibitor of elastase release from human polymorphonuclear leukocytes (range 8?C17% inhibition), however this is much weaker than the inhibition seen with N-acetylgalactosamine (range 92?C100%).
  44. Hydroxyacetic acid is a dermatologic agent. It has also been used as a plant-tissue based biosensor and chemiluminescence flow sensor.
  45. 20S proteasome inhibitor

    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
  46. HCV NS5A inhibitor

    Ledipasvir acetone is the active pharmaceutical ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
  47. 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.
  48. Thevetiaflavone could upregulate the expression of Bcl?2 and downregulate that of Bax and caspase?3.
  49. 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.
  50. 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.

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