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enzyme site

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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

    DNA/RNA Synthesis 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

    DNA/RNA Synthesis 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-P2931

    TPI

    Endogenous Metabolite Others Cancer
    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-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-P4552

    Angiotensin Receptor Others
    Hippuryl-Phe-Arg-OH is the active site on the cell surface of Angiotensin I converting enzyme (ACE) .
    Hippuryl-Phe-Arg-OH
  • 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-162674

    SARS-CoV Infection
    MERS-CoV-IN-2 (compound 3c) is a MERS-CoV 3CLpro inhibitor (IC50=17nM). MERS-CoV-IN-2 inhibits the activity of the 3CLpro enzyme by binding to the active site of the enzyme, specifically the S4 subsite, thereby exhibiting antiviral activity against SARS-CoV-2 and MERS-CoV .
    MERS-CoV-IN-2
  • HY-158378

    R-AST-OH

    Glutaminase Cancer
    Trivalent hydroxyarsinothricn (R-AST-OH) is a covalent and irreversible kidney-type glutaminase (KGA) inhibitor. Trivalent hydroxyarsinothricn binds to the glutamine binding site and forms a covalent bond with an active site cysteine residue. Trivalent hydroxyarsinothricn selectively kills triple-negative breast cancer (TNBC) cells and is not cytotoxic to the control cell line. KGA is the enzyme that controls glutamine metabolism and is correlated with tumor malignancy .
    Trivalent hydroxyarsinothricn
  • HY-E70393J

    Others Others
    Bovine Factor XIa is an enzyme, which is involved in the intrinsic pathway of blood coagulation. Bovine Factor XIa is highly selective and exhibits a minimal extended substrate recognition site of at least five residues long. Bovine Factor XIa is reactive as Bovine Factor IXa (HY-E70393I) does, that it cleaves all the peptides bearing factor IX activation site sequences .
    Bovine Factor XIa
  • HY-E70393I

    Others Others
    Bovine Factor IXa Beta is an inactive and highly specific enzyme, with a minimal extended substrate recognition site and a preference for particular amino acid residues at specific subsites. Bovine Factor IXa Beta plays a role in the blood coagulation cascade .
    Bovine Factor IXa Beta
  • 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 (?-site amyloid precursor protein cleaving enzyme 1). Scoulerine inhibits proliferation, arrests cell cycle, and induces apoptosis in cancer cells .
    Scoulerine
  • HY-133233

    1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine

    Endogenous Metabolite Phospholipase Metabolic Disease
    Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
    Thioetheramide-PC
  • HY-110079

    IPK Superfamily 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-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-117591

    Elastase Inflammation/Immunology Cancer
    L-684248 is an inhibitor of human leukocyte elastase (HLE). L-684248 exerts its inhibitory effect on HLE by forming a covalent bond with the active site of the enzyme, showing potential value for applications in anti-inflammatory and anti-tumor research .
    L 684248
  • HY-119737R

    Acetolactate Synthase (ALS) Metabolic Disease
    Chlorsulfuron (Standard) is the analytical standard of Chlorsulfuron. This product is intended for research and analytical applications. 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 (Standard)
  • 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
    2 Publications Verification

    AG 337

    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
    60+ 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-16183A

    Echothiophate chloride

    Others Cardiovascular Disease
    Echothiophate (Echothiophate) chloride is a highly effective, long-lasting cholinesterase inhibitor employed as a miotic for managing glaucoma. Echothiopate chloride forms a covalent bond with the serine residue at the active site of cholinesterase through its phosphate group, rendering the enzyme permanently inactive and necessitating the synthesis of new enzymes by the cell. Given its irreversible binding to cholinesterase and the extremely slow rate of hydrolysis, the effects of echothiophate can persist for a week or longer. Echothiopate chloride is utilized as an ocular antihypertensive agent in the treatment of chronic glaucoma and, in certain cases, accommodative esotropia.
    Echothiopate chloride
  • HY-15908
    BCA
    5 Publications Verification

    Disodium bicinchoninate

    Beta-secretase Neurological Disease Cancer
    BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
    BCA
  • 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-163885

    Cholinesterase (ChE) Beta-secretase γ-secretase Neurological Disease
    SSZ is a multi-target inhibitor, which targets multiple pathological mechanisms of Alzheimer's disease (AD). SSZ targets acetylcholinesterase, butyrylcholinesterase, β-site amyloid precursor protein cleavage enzyme 1 (BACE1), and γ-secretase. SSZ ameliorates Alzheimer’s diseases and exhibits neuroprotective effect in mice .
    SSZ
  • HY-18112

    Beta-secretase Neurological Disease
    AZ-4217 is an inhibitor for β-site amyloid precursor protein cleavage enzyme 1 (BACE1), with IC50 of 160 pM in human SH-SY5Y cells. AZ-4217 reduces amyloid deposition in Tg2576 mouse models, and is used for Alzheimer’s Disease research .
    AZ-4217
  • HY-117798

    Thrombin Cardiovascular Disease
    LY 806303 is a potent and selective inhibitor of human α-thrombin. LY 806303 specifically acylates Ser-205 within the catalytic triad of α-thrombin on the heavy chain and a key site involved in the enzymatic activity of thrombin. The mechanism of action of LY 806303 as an enzyme inhibitor is through the specific acylation of this catalytic serine residue .
    LY 806303
  • HY-113658

    Others Others
    ts-SA is a carbonic anhydrase (CA) inhibitor with activity against seven human CA homologues. ts-SA can bind to the Zn(II) ion in the enzyme active site in a deprotonated form. The organic skeleton of ts-SA extends in the enzyme cavity and participates in multiple interactions with amino acid residues and water molecules. Due to its structural differences, the inhibitory performance of ts-SA is significantly better than that of another pyridine derivative. ts-SA exhibits low nanomolar inhibitory activity and is a multi-target CA inhibitor .
    ts-SA
  • 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-10572A

    (R)-DMP 266; (R)-EFV; (R)-L-743726

    Reverse Transcriptase Infection
    (R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
    (R)-Efavirenz
  • 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-NP009

    Biochemical Assay Reagents Others
    α-Lactalbumin is a Ca 2+-binding protein. α-Lactalbumin has a single strong Ca 2+-binding site and for this reason it frequently serves as a simple model Ca 2+-binding protein. α-Lactalbumin is a component of lactose synthase, an enzyme system, which consists of galactosyltransferase (GT) and α-Lactalbumin .
    α-Lactalbumin
  • HY-161681

    Guanylate Cyclase Metabolic Disease
    Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
    Formycin triphosphate
  • HY-117925

    HBV Others
    Personalised postprandial-targeting is a way to modulate water-heme interactions with activity against low-spin P450 complexes. Personalised postprandial-targeting is able to maintain the axial water ligands of CYP2C9 even in the presence of inhibitors. Personalised postprandial-targeting also allows the hydrogen atoms of the axial water ligands to be observed by EPR spectroscopy, providing insights into the enzyme active site .
    Personalised postprandial-targeting
  • HY-14156

    11β-HSD Metabolic Disease
    11β-HSD1-IN-15 is an inhibitor of 11β-hydroxysteroid dehydrogenase type I (11β-HSD1). 11β-HSD1-IN-15 blocks the conversion of corticosterone to cortisol by binding to the active site of the 11β-HSD1 enzyme. 11β-HSD1-IN-15 can be used to investigate the role of 11β-HSD1 enzymes IN the development of metabolic syndrome, obesity, cognitive decline and type 2 diabetes .
    11β-HSD1-IN-15
  • HY-15463
    Imatinib
    Maximum Cited Publications
    85 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-P2823

    Endogenous Metabolite Biochemical Assay Reagents Others
    Trypsinogen, a proenzyme synthesized in the pancreas, is activated to form trypsin by enterokinase upon reaching the small intestine lumen, where it opens a hexapeptide bond at the Lys6 - Ile7 junction, leading to the production of the active enzyme. This single polypeptide chain, composed of 229 amino acids and stabilized by six disulfide bridges, further autocatalytically converts additional trypsinogen into trypsin, which is initially present as β-trypsin before undergoing autolysis at the Lys131 - Ser132 site to form α-trypsin. As a serine protease, trypsin features His46 and Ser183 at its active site and exhibits optimal enzymatic activity at a pH range of 7 to 9.
    Trypsinogen
  • 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-118061

    Others Infection
    VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
    VCC234718

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