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tight binding

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39

Inhibitors & Agonists

1

Fluorescent Dyes

5

Peptides

2

Inhibitory Antibodies

1

Isotope-Labeled Compounds

1

Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18731
    1400W Dihydrochloride
    Maximum Cited Publications
    28 Publications Verification

    		 NO Synthase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    1400W dihydrochloride is the dihydrochloride form of 1400W (HY-18730). 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
    1400W Dihydrochloride
  • HY-12220
    MM-102
    4 Publications Verification

    HMTase Inhibitor IX

    		 WDR5 Apoptosis NF-κB TNF Receptor Interleukin Related Inflammation/Immunology Cancer
    MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
    MM-102
  • HY-115194
    Amastatin hydrochloride
    1 Publications Verification

    		 Aminopeptidase Bacterial Infection
    Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase .
    Amastatin hydrochloride
  • HY-15460
    CHIR-090
    3 Publications Verification

    		 Bacterial Antibiotic Infection
    CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CHIR-090
  • HY-D2468
    HRP-Streptavidin
    1 Publications Verification

    		 Fluorescent Dye Others
    Sulfonylurea Receptor HRP-Streptavidin is a biotin-binding signal amplifier designed to bind tightly with biotinylated anti-TSH monoclonal antibodies, thereby constituting a key component of the signal amplification system in immunoassays. HRP-Streptavidin is formed by the covalent coupling of Horseradish Peroxidase (HRP) with Streptavidin; it combines the highly efficient catalytic activity of the enzyme with the high affinity of Streptavidin for biotin, making it a potent and sensitive tool for signal amplification. HRP-Streptavidin is suitable for use in Western Blotting, ELISA, and other detection techniques .
    HRP-Streptavidin
  • HY-18730
    1400W
    Maximum Cited Publications
    28 Publications Verification

    W1400

    		 NO Synthase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
    1400W
  • HY-117766
    PC945

    		Fungal Cytochrome P450 Infection
    PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
    PC945
  • HY-B0306
    Prothionamide

    Protionamide

    		 Bacterial Infection
    Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
    Prothionamide
  • HY-19348
    Pimelic Diphenylamide 106
    5 Publications Verification

    RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII

    		 HDAC Monoamine Transporter Neurological Disease Cancer
    Pimelic Diphenylamide 106 (TC-H 106) is a slow, tight binding class I HDAC inhibitor (inhibits HDAC1, 2, and 3 with IC50 values of 150 nM, 760 nM, and 370 nM, respectively), with no activity against class II HDACs. Pimelic Diphenylamide 106 modulates dopamine concentration and protects dopamine cells by inducing VMAT2 expression. Pimelic Diphenylamide 106 can be used in the study of neuropsychiatric diseases such as attention deficit hyperactivity disorder (ADHD) .
    Pimelic Diphenylamide 106
  • HY-P991200
    OM-7D3-B3

    		HCV Claudin Infection
    OM-7D3-B3 is an antibody-based antiviral agent targeting the tight junction protein CLDN1 (Kd=4 nM). By binding to the first extracellular domain of CLDN1, OM-7D3-B3 disrupts the formation of the CLDN1-CD81 co-receptor complex, thereby effectively inhibiting the entry of hepatitis C virus (HCV). OM-7D3-B3 not only prevents de novo and chronic HCV infections in humanized liver chimeric mice and uPA-SCID mice transplanted with human livers, but also exhibits favorable safety with no toxic effects observed. OM-7D3-B3 serves as a critical tool for research on HCV infection mechanisms and antiviral drug development .
    OM-7D3-B3
  • HY-P11446
    AE105

    		Transmembrane Glycoprotein Cancer
    AE105 is a 9-mer peptide probe targeting the urokinase-type plasminogen activator receptor (uPAR). AE105 binds tightly to the uPA-binding cavity of uPAR. AE105 can be used for the study of cancer .
    AE105
  • HY-115450
    ONO-0300302

    		LPL Receptor Endocrinology Cancer
    ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research .
    ONO-0300302
  • HY-124796
    Qstatin

    		Bacterial Infection
    QStatin is a potent and selective inhibitor of SmcR (V. harveyi LuxR homologue) with an EC50 of 208.9 nM, binding tightly to SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin shows pan-QS (Vibrio quorum sensing) inhibitor activity in diverse Vibrio species and attenuates their virulence in an aquatic host. QStatin may be a sustainable antivibriosis agent useful in aquacultures .
    Qstatin
  • HY-125475
    Rivipansel

    GMI-1070

    		 E-Selectin Cardiovascular Disease
    Rivipansel is a small-molecule glycomimetic pan-selectin antagonist with inhibitory activity against E-selectin and P-selectin. Rivipansel binds tightly to the lectin domain of E-selectin, and selectively blocks the recognition of CD62L by E-selectin without affecting the binding of PSGL-1 to E-selectin. Rivipansel functionally inhibits the adhesion of hematopoietic cells to endothelial cells, and is applicable to research related to sickle cell disease .
    Rivipansel
  • 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-P3828
    Biotin-myelin basic protein (94-102)

    		Fluorescent Dye Neurological Disease
    Biotin-myelin basic protein (94-102) is a peptide fragemt. Myelin basic protein is responsible for adhesion of the cytosolic surfaces of multilayered compact myelin, it plays an important role in the process of myelination of nerves in the nervous system. Myelin basic protein also acts as a membrane actin-binding protein, which might allow it to participate in transmission of extracellular signals to the cytoskeleton in oligodendrocytes and tight junctions in myelin .
    Biotin-myelin basic protein (94-102)
  • HY-125969
    Rtt109 inhibitor 1

    		Histone Acetyltransferase Fungal Infection
    Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .
    Rtt109 inhibitor 1
  • HY-P2713
    OM99-2

    		Beta-secretase Neurological Disease
    OM99-2, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
    OM99-2
  • HY-P11446A
    AE105 TFA

    		Transmembrane Glycoprotein Cancer
    AE105 TFA is a 9-mer peptide probe targeting the urokinase-type plasminogen activator receptor (uPAR). AE105 TFA binds tightly to the uPA-binding cavity of uPAR. AE105 TFA can be used for the study of cancer .
    AE105 TFA
  • HY-113646
    Shield-2

    		FKBP Others
    Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
    Shield-2
  • HY-120621
    BMS-229724

    		Phospholipase Inflammation/Immunology
    BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation .
    BMS-229724
  • 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-178343
    Aurora A-IN-5

    		Aurora Kinase Apoptosis Cancer
    Aurora A-IN-5 is a potent and highly selective Aurora A inhibitor (IC50 = 0.02 μM), showing 362-fold selectivity for over Aurora B. Aurora A-IN-5 shows its selectivity through unique C−H/π interactions, enhanced hydrophobic contacts, an open binding pocket, and tighter protein packing. Aurora A-IN-5 suppresses Aurora A autophosphorylation, thereby inhibiting cancer cell proliferation by inducing G2/M phase arrest, triggering apoptosis, and suppressing colony formation. Aurora A-IN-5 inhibits tumor growth in MDA-MB-231 xenograft mouse models. Aurora A-IN-5 can be used for breast, cervical, prostate, and lymphoma cancer research .
    Aurora A-IN-5
  • HY-121908
    FCPT

    		ATP Synthase Cancer
    FCPT, an ATP competitive inhibitor, induces a tight-binding of kinesin-5 onto microtubules and induced loss of microtubules selectively at the poles of Xenopus extract spindles without altering microtubule dynamics .
    FCPT
  • HY-172764
    L-ENIPO hydrochloride

    		NO Synthase Metabolic Disease
    L-ENIPO (hydrochloride) is an inhibitor of iNOS, nNOS, and eNOS with Ki values of 17, 10.3, and 58.2 μM. L-ENIPO (hydrochloride) exerts reversible tight binding inhibition selective for iNOS with longer incubation time .
    L-ENIPO hydrochloride
  • HY-111150
    AMG-222

    		Dipeptidyl Peptidase Metabolic Disease
    AMG-222 is a dipeptidyl peptidase IV (DPP-IV) inhibitor that exerts its inhibitory effect by tightly and reversibly binding to DPPIV. AMG 222 binds to human plasma proteins in a saturable and concentration-dependent manner, with a binding rate of 80.8% at 1 nM, while the binding rate decreases to 29.4% at concentrations above 100 nM. AMG-222 can be used in research related to diabetes .
    AMG-222
  • HY-P2713A
    OM99-2 TFA

    		Beta-secretase Neurological Disease
    OM99-2 TFA, an eight residue peptidomimetic, tight-binding inhibitor of human brain memapsin 2 with a Ki value of 9.58 nM . OM99-2 TFA is significantly advanced the development of BACE1 inhibitor . OM99-2 has the potential for the research of the Alzheimer's disease .
    OM99-2 TFA
  • HY-15460R
    CHIR-090 (Standard)

    		Reference Standards Bacterial Antibiotic Infection
    CHIR-090 (Standard) is the analytical standard of CHIR-090. This product is intended for research and analytical applications. CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CHIR-090 (Standard)
  • HY-18731R
    1400W Dihydrochloride (Standard)

    		NO Synthase Apoptosis Cardiovascular Disease Inflammation/Immunology Cancer
    1400W (Dihydrochloride) (Standard) is the analytical standard of 1400W (Dihydrochloride). This product is intended for research and analytical applications. 1400W dihydrochloride is the dihydrochloride form of 1400W (HY-18730). 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
    1400W Dihydrochloride (Standard)
  • HY-B0306S
    Prothionamide-d5

    Protionamide-d5

    		 Isotope-Labeled Compounds Bacterial Infection
    Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
    Prothionamide-d5
  • HY-B0306R
    Prothionamide (Standard)

    Protionamide (Standard)

    		 Reference Standards Bacterial Infection
    Prothionamide (Standard) is the analytical standard of Prothionamide (HY-B0306). This product is intended for research and analytical applications. Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
    Prothionamide (Standard)
  • 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-133031A
    CSV0C018875 hydrochloride

    		Histone Methyltransferase Others
    CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
    CSV0C018875 hydrochloride
  • HY-179655
    ST17

    		HDAC Cancer
    ST17 is a light-activatable ST13 prodrug. ST17 readily releases ST13 upon irradiation. ST13 is a selective, slow- and tight-binding HDAC1/HDAC2 inhibitor with antiproliferative activity. ST17 can be used in the research of melanoma and breast cancer .
    ST17
  • HY-W800818
    (Z)-Non-2-enyl 6-bromohexanoate

    		Biochemical Assay Reagents Others
    (Z)-Non-2-enyl 6-bromohexanoate is an analogue of Biotin and a protein cross-linking agent.(Z)-Non-2-enyl 6-bromohexanoate binds less tightly to biotin-binding proteins such as Avidin and is easily displaced by Biotin. It is used in the preparation of agarose matrices for affinity-based isolation of streptavidin-fluorophore conjugates.
    (Z)-Non-2-enyl 6-bromohexanoate
  • HY-182303
    Carboxyatractyloside

    CATR

    		 Methionine Adenosyltransferase (MAT) Neurological Disease
    Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A (HY-B0579), Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease .
    Carboxyatractyloside
  • HY-181085
    RD0448

    		DYRK Neurological Disease Inflammation/Immunology Cancer
    RD0448 is a potent inhibitor of DYRK1A, DYRK1B, and DYRK2. RD0448 selectively targets the non-native (folded intermediate) state of DYRK1A and DYRK1B. The binding site of RD0448 is hidden in the native state of DYRK1A and DYRK1B, and as a stabilizing binder, it binds tightly to both DYRK1A and DYRK1B, forming a stable complex with slow dissociation kinetics. In contrast, RD0448 targets the native state of DYRK2 without selectivity between its native and non-native states, acting as a weak binder with weaker binding affinity to DYRK2 and forming a rapidly dissociating complex .
    RD0448
  • HY-P991869
    Aquaporumab

    AQmabAM; rAb-53

    		 Aquaporin Neurological Disease
    Aquaporumab (AQmabAM) is an engineered human monoclonal IgG antibody. Aquaporumab is a selective inhibitor of aquaporin 4 (AQP4), binding tightly to AQP4 and competitively displacing AQP4-IgG from serum [1][2]. Aquaporumab significantly reduces neuromyelitis optica lesions in spinal cord slice cultures and in mice receiving intracerebral injection of AQP4-IgG and complement [1][2]. Aquaporumab can be used for research on neuromyelitis optica spectrum disorders [1][2]."}
    Aquaporumab
  • HY-179654
    ST13

    		HDAC Apoptosis Cancer
    ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC50s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC50 = 4.30 μM) and HDAC6 (IC50 > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex E*I. ST13 induces apoptosis in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast .
    ST13

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