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Results for "

slow-binding

" in MedChemExpress (MCE) Product Catalog:

18

Inhibitors & Agonists

1

Natural
Products

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-16693
    LDN-27219
    1 Publications Verification

    		 Others Cardiovascular Disease Others
    LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease .
    LDN-27219
  • HY-19548A
    BEC hydrochloride
    1 Publications Verification

    		 Arginase Metabolic Disease
    BEC hydrochloride is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM and 30 nM at pH 7.5 and pH 9.5, respectively .
    BEC hydrochloride
  • HY-134358A
    Ara-F-NAD+ sodium

    		CD38 Neurological Disease
    Ara-F-NAD+ sodium is an arabino analogue of NAD +. Ara-F-NAD+ sodium is a potent, reversible and slow-binding CD38 NADase inhibitor .
    Ara-F-NAD+ sodium
  • HY-19269
    FK706

    		Elastase Inflammation/Immunology
    FK706 is a potent, slow-binding and competitive inhibitor of human neutrophil elastase with an IC50 of 83 nM and a Ki of 4.2 nM. FK706 also inhibits mouse neutrophil elastase and porcine pancreatic elastase with IC50s of 22 nM and 100 nM, respectively, and has no inhibitory activity against other serine proteinases such as human pancreatic trypsin, human pancreatic α-chymotrypsin and human leukocyte cathepsin G. FK706 has anti-inflammatory effect .
    FK706
  • HY-124346
    T-3364366
    1 Publications Verification

    		 Others Metabolic Disease
    T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
    T-3364366
  • HY-134358
    Ara-F-NAD+

    		CD38 Neurological Disease
    Ara-F-NAD+ is an arabino analogue of NAD +. Ara-F-NAD+ is a potent, reversible and slow-binding CD38 NADase inhibitor .
    Ara-F-NAD+
  • HY-161304
    HDAC6-IN-33

    		HDAC Cancer
    HDAC6-IN-33 (compound 6) is a selective and irreversible HDAC6 inhibitor with an IC50 of 193 nM. HDAC6-IN-33 shows no activity against HDAC1-4. HDAC6-IN-33 is a tight-binding HDAC6 inhibitor capable of inhibiting HDAC6 via a two-step slow-binding mechanism .
    HDAC6-IN-33
  • HY-151927
    AChE-IN-28

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-28 (Compound 2h) is a selective slow-binding inhibitor of acetylcholinesterase with an IC50 of 0.2 nM .
    AChE-IN-28
  • HY-161306
    ITF5924

    		HDAC Cancer
    ITF5924 (compound 1) is a potent and highly selective HDAC6 inhibitor with an IC50 of 7.7 nM. ITF5924 shows greater than 104-fold selectivity for HDAC6 over all other HDAC subtypes. ITF5924 containing a difluoromethyl-1,3,4-oxadiazole (DFMO) moiety is slow-binding substrate analog of HDAC6 that undergo an enzyme-catalyzed ring opening reaction, forming a tight and long-lived enzyme-inhibitor complex .
    ITF5924
  • HY-144812
    Gü1303

    		Cathepsin Inflammation/Immunology Cancer
    Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
    Gü1303
  • HY-19548
    BEC

    		Arginase Endocrinology
    BEC, an arginine analogue, is a slow-binding competitive inhibitor of the binuclear manganese metalloenzyme arginase. BEC enhances substrate flux to NO synthase, thereby enhancing NO-dependent smooth muscle relaxation in the corpus cavernosum, and enhances penile erection .
    BEC
  • HY-158615
    STING18

    Stimulator of interferon genes 18

    		 Others Others
    STING18 (Stimulator of interferon genes 18) is a compound that inhibits STING protein by utilizing a small molecule active site dimer, with good oral exposure, slow binding kinetics, and functional inhibitory activity on STING-mediated cytokine release.
    STING18
  • HY-118175
    RG 14921

    		Others Others
    RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
    RG 14921
  • HY-19143
    L-697639

    		HIV Infection
    L-697639 is an inhibitor for HIV-1 reverse transcriptase (HIV-1 RT) with IC50 of 20-400 nM (in a template-primer-dependent manner). L-697639 exhibits antiviral activity, that inhibits 95% HIV-1 infection at concentrations of 12-200 nM in human T lymphocyte cultures .
    L-697639
  • HY-108611
    AACOCF3
    3 Publications Verification

    Arachidonyl trifluoromethyl ketone

    		 Phospholipase Cardiovascular Disease
    AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease .
    AACOCF3
  • HY-103353
    SID 26681509
    4 Publications Verification

    		 Cathepsin Parasite Infection Cancer
    SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
    SID 26681509
  • HY-103353A
    SID 26681509 quarterhydrate
    4 Publications Verification

    		 Cathepsin Parasite Infection Cancer
    SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
    SID 26681509 quarterhydrate
  • HY-117374
    HDAC3-IN-1

    		HDAC Cancer
    HDAC3-IN-1 (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM .
    HDAC3-IN-1

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