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Pathways Recommended: Metabolic Enzyme/Protease
Results for "

enzyme site

" in MedChemExpress (MCE) Product Catalog:

35

Inhibitors & Agonists

3

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1

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5

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4

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2

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1

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1

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18081

    FAAH Autophagy Metabolic Disease
    PF 750 is a selective and covalent fatty acid amide hydrolase (FAAH) inhibitor, with IC50s varied from 16.2-595 nM in different pre-incubation times. Covalently modifies the enzyme’s active site serine nucleophile .
    PF 750
  • HY-15345
    Tetrahydrouridine dihydrate
    1 Publications Verification

    THU dihydrate; NSC-112907 dihydrate

    Others Cancer
    Tetrahydrouridine dihydrate (THU dihydrate) is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine.
    Tetrahydrouridine dihydrate
  • HY-15345A
    Tetrahydrouridine
    1 Publications Verification

    THU; NSC-112907

    Others Cancer
    Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine .
    Tetrahydrouridine
  • HY-116750

    Tyrosinase Others
    6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .
    6-Hydroxykaempferol
  • HY-146125

    Others Metabolic Disease
    CGCG/CGG ligand 1 (compound 10), an anthracenone derivative, is a CGCG or CGG short spacer-ligand. CGCG/CGG ligand 1 can protect cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme .
    CGCG/CGG ligand 1
  • HY-P2931

    TPI

    Endogenous Metabolite Others
    Triosephosphate isomerase (TPI) is a glycolytic enzyme. Triosephosphate isomerase fast interconverts dihydroxyacetone phosphate and D: -glyceraldehyde-3-phosphate, its catalytic site is at the dimer interface .
    Triosephosphate isomerase
  • HY-119737

    Acetolactate Synthase (ALS) Metabolic Disease
    Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase .
    Chlorsulfuron
  • HY-144739

    Beta-secretase Neurological Disease
    BACE1-IN-8 (compound 70b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 3.9 µM .
    BACE1-IN-8
  • HY-144741

    Beta-secretase Neurological Disease
    BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM .
    BACE1-IN-9
  • HY-119689

    CNP520

    Beta-secretase Neurological Disease
    Umibecestat (CNP520) is a beta-site amyloid precursor protein cleaving enzyme-1 (BACE-1) inhibitor with IC50s of 11 nM and 10 nM for human BACE-1 and mouse BACE-1, respectively . Umibecestat can be used for the research of alzheimer's disease.
    Umibecestat
  • HY-112157
    PF-06751979
    1 Publications Verification

    Beta-secretase Neurological Disease
    PF-06751979 is a potent, brain penetrant, β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 7.3 nM in BACE1 binding assay.
    PF-06751979
  • HY-15345AS

    THU-d3; NSC-112907-d3

    Isotope-Labeled Compounds Cancer
    Tetrahydrouridine-d3 is the deuterium labeled Tetrahydrouridine[1]. Tetrahydrouridine dihydrate is potent inhibitor of cytidine deaminase (CDA), which competitively blocks the enzyme's active site more effectively than intrinsic cytidine[2][3].
    Tetrahydrouridine-d3
  • HY-110079

    Others Cancer
    TNP is a cell-permeable inhibitor of IP6K1 and IP3K, with IC50 values of 0.55 µM and 10.2 µM for IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes .
    TNP
  • HY-N1255

    (-)-Scoulerine; Discretamine

    Microtubule/Tubulin Beta-secretase Apoptosis Cancer
    Scoulerine ((-)-Scoulerine), an isoquinoline alkaloid, is a potent antimitotic compound. Scoulerine is also an inhibitor of BACE1 (ß-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
    Scoulerine
  • HY-108966

    Beta-secretase Inflammation/Immunology
    Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM .
    Kushenol C
  • HY-150702

    MAGL Neurological Disease Inflammation/Immunology
    MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
    MAGLi 432
  • HY-U00287

    Beta-secretase Neurological Disease
    BACE-IN-1 (Compound 13) is a substituted lmidazo[1 ,2-a]pyridine derivative which can inhibit β-site amyloid precursor protein-cleaving enzyme (BACE) and that may be useful in the treatment of diseases in which BACE is involved, such as Alzheimer's disease.
    BACE-IN-1
  • HY-108474
    Nolatrexed dihydrochloride
    1 Publications Verification

    AG 337; Thymitaq

    Thymidylate Synthase Cancer
    Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
    Nolatrexed dihydrochloride
  • HY-P0266B

    Ac-SDKP acetate

    Angiotensin-converting Enzyme (ACE) Inflammation/Immunology
    N-Acetyl-Ser-Asp-Lys-Pro (Ac-SDKP) acetate is a specific substrate for the N-terminal active site of angiotensin-converting enzyme (ACE). N-Acetyl-Ser-Asp-Lys-Pro acetate is a natural inhibitor of pluripotent hematopoietic stem cell proliferation. Anti-inflammatory and antifibrotic properties .
    N-Acetyl-Ser-Asp-Lys-Pro acetate
  • HY-P4739

    GnRH Receptor Others
    LHRH (1-5) (free acid) is a polypeptide generated by the cleavage of LHRH at the Tyr 55-Gly 66 site. LHRH (1-5) (free acid) is converted into LHRH (1-3) and LHRH (4-5) fragments under the catalysis of Angiotensin-converting enzyme (HY-P2983) .
    LHRH (1-5) (free acid)
  • HY-108331
    3-TYP
    45+ Cited Publications

    Sirtuin Methionine Adenosyltransferase (MAT) Indoleamine 2,3-Dioxygenase (IDO) Others
    3-TYP is an inhibitor of SIRT3 (IC50: ~377 μM) and an inhibitor of Methionine Adenosyltransferase (MAT) 2 and Indoleamine 2,3-Dioxygenase (IDO). There may be many off-target sites for 3-TYP that need to be examined, such as NAD-dependent enzymes, including dehydrogenases .
    3-TYP
  • HY-N7263

    Cholinesterase (ChE) Neurological Disease
    Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .
    Galanthamine N-Oxide
  • HY-P1435

    NADPH Oxidase Cardiovascular Disease
    NoxA1ds is a highly efficacious and selective Nox1 (NADPH oxidase isoform 1) inhibitor. NoxA1ds establishes a critical interaction site for Nox1-NOXA1 binding required for enzyme activation. NoxA1ds can be used for the research of hypertension, atherosclerosis and neoplasia .
    NoxA1ds
  • HY-109052

    JNJ-54861911

    Beta-secretase Neurological Disease
    Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat s tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat has the potential for Alzheimer's Disease treatment .
    Atabecestat
  • HY-130244

    Beta-secretase Neurological Disease
    BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux .
    BACE1-IN-5
  • HY-15463
    Imatinib
    Maximum Cited Publications
    69 Publications Verification

    STI571; CGP-57148B

    Bcr-Abl PDGFR c-Kit SARS-CoV Autophagy Cancer
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib
  • HY-12404
    Diminazene aceturate
    5 Publications Verification

    Diminazene diaceturate

    Parasite Angiotensin-converting Enzyme (ACE) Infection Inflammation/Immunology
    Diminazene aceturate (Diminazene diaceturate) is an anti-trypanosome agent for livestock. The main biochemical mechanism of the trypanocidal actions of Diminazene aceturate is by binding to trypanosomal kinetoplast DNA (kDNA) in a non-intercalative manner through specific interaction with sites rich in adenine-thymine base pairs. Diminazene aceturate is also an angiotensin-converting enzyme 2 (ACE2) activator and has strong and potent anti-inflammatory properties .
    Diminazene aceturate
  • HY-15463S2

    STI571-d3 hydrochloride; CGP-57148B-d3 hydrochloride

    Autophagy Bcr-Abl c-Kit SARS-CoV PDGFR Cancer
    Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-d3 hydrochloride
  • HY-13240
    LY2886721
    2 Publications Verification

    Beta-secretase Neurological Disease
    LY2886721 is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
    LY2886721
  • HY-131275

    Drug Metabolite Others
    Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively . Imatinib also is an inhibitor of SARS-CoV and MERS-CoV .
    Imatinib Impurity E
  • HY-13240A

    Beta-secretase Neurological Disease
    LY2886721 hydrochloride is a potent, selective and orally active beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 20.3 nM for recombinant human BACE1. LY2886721 hydrochloride is selectivity against cathepsin D, pepsin, and renin, but lacking selectivity against BACE2 (IC50 of 10.2 nM). LY2886721 hydrochloride can across blood-brain barrier and has the potential for Alzheimer's disease treatment .
    LY2886721 hydrochloride
  • HY-128774

    Beta-secretase Neurological Disease
    AM-6494 is a potent and orally active BACE1 (efficacious β-site amyloid precursor protein cleaving enzyme 1) inhibitor (IC50=0.4 nM) with in vivo selectivity over BACE2 (IC50=18.6 nM) . AM-6494 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    AM-6494
  • HY-144381

    Bacterial Infection
    Glutamate-5-kinase-IN-1 (compound 50) is a potent glutamate-5-kinase (G5K) inhibitor with an MIC (minimum inhibitory concentration) of 4.1 µM. Glutamate-5-kinase-IN-1 shows G5K inhibition by alters the ATP binding site architecture for enzyme recognition. Glutamate-5-kinase-IN-1 has the potential for the research of anti-TB agents .
    Glutamate-5-kinase-IN-1
  • HY-128206
    I3MT-3
    4 Publications Verification

    HMPSNE

    Hippo (MST) Metabolic Disease
    I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST .
    I3MT-3
  • HY-150260

    Bacterial Infection
    SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
    SA09-Cu

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