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catalytic sites

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80

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3

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Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10519
    BMS-345541
    Maximum Cited Publications
    33 Publications Verification

    		 IKK Cancer
    BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
    BMS-345541
  • HY-10518
    BMS-345541 hydrochloride
    Maximum Cited Publications
    33 Publications Verification

    		 IKK Cancer
    BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
    BMS-345541 hydrochloride
  • HY-11107
    PHA-665752
    10+ Cited Publications

    		 c-Met/HGFR Autophagy Apoptosis Cancer
    PHA-665752 is a selective, ATP-competitive, and active-site inhibitor of the catalytic activity of c-Met kinase (Ki=4 nM; IC50=9 nM). PHA-665752 exhibits >50-fold selectivity for c-Met compared with a panel of diverse tyrosine and serine-threonine kinases. PHA-665752 induces apoptosis and cell cycle arrest, and exhibits cytoreductive antitumor activity .
    PHA-665752
  • HY-123847
    KPT-6566
    1 Publications Verification

    		 PIN1 Cancer
    KPT-6566 is a selective and covalent prolyl isomerase PIN1 inhibitor, covalently binds to the catalytic site of PIN1, selectively inhibits and degrades PIN1. KPT-6566 shows an IC50 value of 640 nM and a Ki value of 625.2 nM for PIN1 PPIase domain. KPT-6566 can be used for the research of cancer .
    KPT-6566
  • HY-161762
    RA-0002034

    RA-2034

    		 CHIKV Virus Protease Infection
    RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with an IC50 of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner .
    RA-0002034
  • HY-N6675
    Gardenia yellow

    		Amylases Glycosidase Inflammation/Immunology
    Gardenia yellow is a competitive inhibitor of α-Amylase (HY-B2193) and α-glucosidase. Gardenia yellow can bind to the catalytic sites of α-Amylase and α-glucosidase, inhibit starch digestion, and significantly increase the contents of resistant starch and slowly digestible starch in starch-based systems. Gardenia yellow reduces the glycemic index and hydrolysis index. Gardenia yellow can be used in diabetes-related research .
    Gardenia yellow
  • HY-146725
    FBPase-IN-1

    		FBPase Metabolic Disease
    FBPase-IN-1 is a potent FBPase (Fructose-1,6-bisphosphatase) inhibitor for Type 2 diabetes (T2D) study with an IC50 of 0.22 μM. FBPase-IN-1 can reduce blood glucose levels and ameliorate glucose tolerance. FBPase-IN-1 modifies the C128 site, regulates the N125-S124-S123 allosteric pathway of FBPase and affects the catalytic activity of FBPase .
    FBPase-IN-1
  • HY-P3823
    Asp-Asp-Asp-Asp-Asp-Asp

    		Influenza Virus Infection
    Asp-Asp-Asp-Asp-Asp-Asp is a polyaspartic acid. The specificity of the catalytic and antigenic sites of influenza virus neuraminidase is related to the number of specific amino acids.
    Asp-Asp-Asp-Asp-Asp-Asp
  • HY-P5979
    LRRKtide

    		LRRK2 Neurological Disease
    LRRKtide is a polypeptide substrate. LRRKtide is a specific phosphorylation substrate of LRRK2, a kinase associated with Parkinson's disease, and its phosphorylation site is a threonine residue. LRRKtide can be used for characterization of the catalytic properties of LRRK2, as well as studies on kinase activity and inhibition. LRRKtide is applicable to research related to Parkinson's disease .
    LRRKtide
  • HY-111930
    5-Iodo-indirubin-3'-monoxime

    		GSK-3 CDK Cancer
    5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase, with IC50s of 9, 20 and 25 nM, respectively .
    5-Iodo-indirubin-3'-monoxime
  • HY-157521
    AANAT-IN-1

    		Acyltransferase Neurological Disease Metabolic Disease
    AANAT-IN-1 is an arylalkylamine N-acetyltransferase (AANAT) inhibitor with a sheep AANAT IC50 of 9.9 μM. AANAT-IN-1 binds to the active site of sheep AANAT, interacting with amino acid residues via hydrogen bonds, hydrophobic interactions, ionic interactions, and water bridges, inhibiting the enzyme's catalytic activity. AANAT-IN-1 can be used for the researches of circadian rhythm-associated neuropsychiatric conditions, seasonal affective disorder, and other diseases associated with abnormally elevated melatonin levels .
    AANAT-IN-1
  • HY-P2931
    Triosephosphate isomerase

    TPI

    		 Biochemical Assay Reagents Metabolic Disease Cancer
    Triosephosphate isomerase (TPI) is a biocatalyst that interconverts dihydroxyacetone phosphate and D-glyceraldehyde-3-phosphate. Triosephosphate isomerase utilises Glu167 as catalytic base, mediates proton shuttling, and stabilises a cis-enediolate intermediate via loop-6 and loop-7 closure to shield its catalytic site. Triosephosphate isomerase can be used for the research of triosephosphate isomerase deficiency .
    Triosephosphate isomerase
  • HY-136276
    DMNB-caged-Serine

    		Amino Acid Derivatives Others
    DMNB-caged-Serine is a photocaged amino acid. DMNB-caged-Serine can be used as a catalytic residue, hydrogen bonding partner or site of post-translational modification. DMNB-caged-Serine can be used for the control of protein phosphorylation .
    DMNB-caged-Serine
  • HY-171036
    GAPDH-IN-1

    		Endogenous Metabolite Metabolic Disease
    GAPDH-IN-1 (Compound F8) is a GAPDH inhibitor (IC50 of 39.31 μM for GAPDH enzymatic activity). GAPDH-IN-1 forms a covalent adduct with an aspartic acid in the active site to displace NAD +, a cofactor of the enzyme, with concomitant enhancement of the cysteine-reactive probe reaction with the catalytic cysteine .
    GAPDH-IN-1
  • HY-P10422A
    Multi-Leu peptide triacetate

    ML-peptide, Multi-Leucine (ML)-peptide triacetate

    		 Autophagy Cancer
    Multi-Leu peptide (ML-peptide) triacetate is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide triacetate can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide triacetate can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
    Multi-Leu peptide triacetate
  • HY-N10686
    Tanshinone IIA anhydride

    		Carboxylesterase (CES) Cancer
    Tanshinone IIA anhydride, present in root extracts of Salvia miltiorrhiza, acts as an inhibitor of human carboxylesterase (CE). Tanshinone IIA anhydride has a Ki value of 1.9 nM against hCE1 and a Ki value of 1.4 nM against hiCE. Tanshinone IIA anhydride forms a stable covalent complex with serine Ser221 at the active site of hCE1, blocking the catalytic cycle of carboxylesterase, and the activity of the inactivated enzyme cannot recover spontaneously. Tanshinone IIA anhydride is applicable in metabolism-related studies .
    Tanshinone IIA anhydride
  • HY-167920
    Glutathione sulfonate

    S-Sulfoglutathione

    		 Endogenous Metabolite Cancer
    Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
    Glutathione sulfonate
  • HY-D2188
    IMP-2373

    		Deubiquitinase Cancer
    IMP-2373 is a low-toxicity activity-based probe targeting covalent pan-deubiquitinase (DUB), which modulates and monitors DUB activity via covalent binding to the catalytic cysteine and active site of DUB. IMP-2373 enables real-time tracking of dynamic intracellular DUB activity in physiologically relevant living cell systems, and quantitative analysis of activity changes induced by pharmacological inhibition or MYC dysregulation. IMP-2373 can be used for research on related diseases such as B-cell lymphoma .
    IMP-2373
  • HY-N15159
    Cladophorol A

    		Cyclic GMP-AMP Synthase STING Parasite Infection Inflammation/Immunology
    Cladophorol A is a cyclic GMP-AMP synthase (cGAS) inhibitor. Cladophorol A binds to the conserved adenosine nucleobase binding site within the cGAS active site to inhibit its catalytic activity. Cladophorol A effectively inhibits the overactivation of the cGAS-STING pathway with an IC50 of 370 nM. Cladophorol A inhibits asexual blood-stage Plasmodium falciparum with an EC50 of 0.7 μg/mL. Cladophorol A can be used for the researches of inflammatory disease and malaria .
    Cladophorol A
  • HY-175595
    ADEP-14

    ADEP26

    		 ClpP Bacterial Infection
    ADEP-14 (ADEP26) is a ClpP activator. ADEP-14 exhibits antibacterial activity against Gram-negative and Gram-positive bacteria. ADEP-14 can be used in studies related to bacterial infections .
    ADEP-14
  • HY-D2297
    AIE-GA

    		Fluorescent Dye Others
    AIE-GA is a Golgi apparatus (GA) fluorescent probe (green channel: λex = 405 nm, λem = 500-700 nm). AIE-GA has a favourable binding ability to interact with COX-2. AIE-GA binds to the cyclooxygenase catalytic site of COX-2 .
    AIE-GA
  • HY-146201
    PDE4B/7A-IN-1

    		Phosphodiesterase (PDE) 5-HT Receptor Neurological Disease
    PDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression .
    PDE4B/7A-IN-1
  • HY-N12982
    α-Calacorene

    		Others Others
    α-Calacorene is a sesquiterpene that can be isolated from Réunion vetiver oil .
    α-Calacorene
  • HY-W753281
    Dexamethasone metasulfobenzoate sodium

    		SARS-CoV Infection
    Dexamethasone metasulfobenzoate sodium is a SARS-CoV-2 exonuclease (ExoN) inhibitor that binds to the catalytic site of ExoN .
    Dexamethasone metasulfobenzoate sodium
  • HY-W753281R
    Dexamethasone metasulfobenzoate sodium (Standard)

    		Reference Standards SARS-CoV Infection
    Dexamethasone metasulfobenzoate (sodium) (Standard) is the analytical standard of Dexamethasone metasulfobenzoate (sodium). This product is intended for research and analytical applications. Dexamethasone metasulfobenzoate sodium is a SARS-CoV-2 exonuclease (ExoN) inhibitor that binds to the catalytic site of ExoN .
    Dexamethasone metasulfobenzoate sodium (Standard)
  • HY-10572A
    (R)-Efavirenz

    (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-P10422
    Multi-Leu peptide

    ML-peptide, Multi-Leucine (ML)-peptide

    		 Autophagy Cancer
    Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
    Multi-Leu peptide
  • HY-124308
    PS315

    		PKC Cancer
    PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
    PS315
  • HY-175031
    GRL-07524

    		HIV Protease Infection
    GRL-07524 (Compound 4e) is a potent inhibitor of HIV-1 protease (Ki = 0.22 nM). GRL-07524 contains oxaspirocyclic carbamates as the P2 ligands. GRL-07524 exhibits good antiviral activity with an EC50 = 210 nM. GRL-07524 binds to the HIV-1 PR active site in one of the four symmetry independent molecules along with key catalytic residues .
    GRL-07524
  • HY-162094
    CMX410

    		Acyltransferase Bacterial Infection
    CMX410 is an orally active and selective Mycobacterium tuberculosis Pks13 acyltransferase domain inhibitor and anti-bacterial agent. CMX410 reacts with the catalytic serine of the Pks13-AT domain to form a stable β-lactam ring, disables the enzyme’s active site, reduces trehalose monomycolate and trehalose dimycolate levels, triggers cell lysis, and reduces intracellular bacterial burden. CMX410 can be used for the research of tuberculosis .
    CMX410
  • HY-177787A
    2'-Deoxy-N-methyl-AMP ammonium

    		Nucleoside Antimetabolite/Analog Others
    2'-Deoxy-N-methyl-AMP ammonium is an N6-substituted adenine nucleotide derivative and a glycosyl donor. On one hand, 2'-Deoxy-N-methyl-AMP ammonium acts as a specific substrate for N6-methyl-AMP aminohydrolase, and it is catalytically converted to dIMP to participate in the nucleotide metabolic cycle. On the other hand, 2'-Deoxy-N-methyl-AMP ammonium also serves as a guanosine diphosphate (GDP)-linked fucose derivative donor, driving site-specific glycoconjugation of proteins under the mediation of α-1,3-fucosyltransferase. 2'-Deoxy-N-methyl-AMP ammonium is an important molecular tool for investigating the mechanisms of nucleotide modification and protein glycosylation .
    2'-Deoxy-N-methyl-AMP ammonium
  • HY-149484
    AChE/BChE-IN-15

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-15 (Compound 6d) is an AChE/BChE inhibitor, with IC50s of 20 nM and 220 nM respectively. AChE/BChE-IN-15 binds to both catalytic anionic site (CAS) and peripheral anionic site (PAS) in the active sites of AChE and BChE. AChE/BChE-IN-15 can be used for research of Alzheimer’s disease .
    AChE/BChE-IN-15
  • HY-D1493
    FIM-1

    		PKC Others
    FIM-1 is a fluorescent PKC (protein kinase C) probe that can be used for mitochondrial staining. FIM-1 inhibits PKC and acts as ATP-competitive catalytic site inhibitor .
    FIM-1
  • HY-W165085
    1,10-Bis(pyridinium)decane

    Decamethylenebispyridinium dibromide

    		 Cholinesterase (ChE) Neurological Disease
    1,10-Bis(pyridinium)decane (Decamethylenebispyridinium dibromide) is an acetylcholinesterase (AChE) inhibitor with an IC50 of 25.8 nM. 1,10-Bis(pyridinium)decane acts as a bis-quaternary ligand that bridges the enzyme's catalytic site and peripheral site via its two pyridinium groups. 1,10-Bis(pyridinium)decane can be used for the research of alzheimer's disease .
    1,10-Bis(pyridinium)decane
  • HY-157527
    hAChE-IN-7

    		Cholinesterase (ChE) Beta-secretase Neurological Disease
    hAChE-IN-7 (compound 5s) is a mixed inhibitor affecting both the catalytic active site (CAS) and peripheral anionic site (PAS) of hAChE. hAChE-IN-7 displays the balanced inhibitory effect on hAChE (IC50=69.8 nM) and hBuChE (IC50=68.0 nM), and exhibits inhibitory activity against β-secretase-1 (BACE-1) (IC50=3.6 μM). hAChE-IN-7 has the potential for Alzheimer's disease (AD) research .
    hAChE-IN-7
  • HY-122685
    UC-773587

    		SOS1 Cancer
    UC-773587 is a selective SOS1 catalytic activity inhibitor. UC-773587 binds to the catalytic site of Sos1 over HRas and ITSN (a RhoGEF) and inhibits nucleotide exchange with an IC50 value of 4.5 μM. UC-773587 mappes to the Ras switch II interaction region of the Sos1 catalytic site. UC-773587 can be used for the study of prostate cancer .
    UC-773587
  • HY-101796
    NSC-70220

    		Ras SOS1 Cancer
    NSC-70220 is a selective and allosteric SOS1 inhibitor. NSC-70220 inhibits allosteric site activation, and partially inhibited catalytic site activation. NSC-70220 has an anticancer effect .
    NSC-70220
  • HY-P3823A
    Asp-Asp-Asp-Asp-Asp-Asp TFA

    		Influenza Virus Infection
    Asp-Asp-Asp-Asp-Asp-Asp TFA is a polyaspartic acid. The specificity of the catalytic and antigenic sites of influenza virus neuraminidase is related to the number of specific amino acids.
    Asp-Asp-Asp-Asp-Asp-Asp TFA
  • HY-133233
    Thioetheramide-PC

    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-161762A
    (E/Z)-RA-0002034

    (E/Z)-RA-2034

    		 Influenza Virus CHIKV Cancer
    (E/Z)-RA-0002034 is a Chikungunya virus (CHIKV) nsP2 protease inhibitor with IC50 of 58 nM. RA-0002034 covalently modifies the catalytic cysteine in a site-specific manner.
    (E/Z)-RA-0002034
  • HY-117798
    LY 806303

    		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-133126A
    hDDAH-1-IN-1 TFA

    		NO Synthase Inflammation/Immunology Cancer
    hDDAH-1-IN-1 TFA (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 μM .
    hDDAH-1-IN-1 TFA
  • HY-150728
    AChE-IN-22

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-22 (compound 10q) is a selective acetylcholinesterase (AChE) inhibitor against AChE and BuChE with the IC50 values of 0.88 μM and 10 μM, respectively. AChE-IN-22 can bind to both the CAS (catalytic active site) and PAS (peripheral anionic site) of AChE and has the potential for the research of Alzheimer's disease .
    AChE-IN-22
  • HY-154976
    SARS-CoV-2-IN-50

    		SARS-CoV Infection
    SARS-CoV-2-IN-50 (Compound X77C) is a SARS-CoV-2 main protease (M Pro) inhibitor.. SARS-CoV-2-IN-50 has a high affinity to the catalytic site of M Pro .
    SARS-CoV-2-IN-50
  • HY-P1799
    [pTyr5] EGFR (988-993)

    		Phosphatase Others
    [pTyr5] EGFR (988-993) is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B) .
    [pTyr5] EGFR (988-993)
  • HY-151885
    Dual AChE-MAO B-IN-3

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    Dual AChE-MAO B-IN-3 (compound C10) is a potent dual AChE/MAO-B inhibitior, with IC50 values of 0.58 and 0.41 μM, respectively. Dual AChE-MAO B-IN-3 is a dual-binding inhibitor bound to both the catalytic anionic site and peripheral anionic site of AChE. Dual AChE-MAO B-IN-3 can be used for Alzheimer’s disease (AD) research .
    Dual AChE-MAO B-IN-3
  • HY-P1799A
    [pTyr5] EGFR (988-993) TFA

    		Phosphatase Others
    [pTyr5] EGFR (988-993) TFA is derived from the autophosphorylation site (Tyr992) of epidermal growth factor receptor (EGFR 988-993). [pTyr5] EGFR (988-993) TFA is often complexed with the catalytically inactive protein-tyrosine phosphate 1B (PTP1B) .
    [pTyr5] EGFR (988-993) TFA
  • HY-163360
    PI3Kα-IN-19

    		PI3K Cancer
    PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .
    PI3Kα-IN-19
  • HY-133126
    hDDAH-1-IN-1

    		NO Synthase Dimethylargininase (DDAH) Inflammation/Immunology Cancer
    hDDAH-1-IN-1 (compound 8a) is a potent and selective non-amino acid catalytic site inhibitor of human dimethylarginine dimethylaminohydrolase-1 (hDDAH-1), with a Ki of 18 μM. DDAH mediates ADMA metabolism, thereby regulating nitric oxide production in a variety of disease states .
    hDDAH-1-IN-1
  • HY-W728451
    URB694

    		FAAH Cardiovascular Disease Neurological Disease
    URB694 is a carbamate FAAH inhibitor that irreversibly carbamoylate the nucleophile catalytic serine in FAAH active site. URB694 exhibits antidepressant-like activity and cardioprotective effects. URB694 can be used to prepare 11C-Carbonyl-URB694 for in vivo positron emission tomography (PET) imaging studies of the brain FAAH .
    URB694

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