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Results for "

tight binding

" in MedChemExpress (MCE) Product Catalog:

21

Inhibitors & Agonists

3

Peptides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-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-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-115194
    Amastatin hydrochloride

    		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-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-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-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-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-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-133233
    Thioetheramide-PC

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

    		 Endogenous Metabolite Metabolic Disease
    Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
    Thioetheramide-PC
  • 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-18730
    1400W

    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-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-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-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-18731
    1400W Dihydrochloride
    Maximum Cited Publications
    15 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-19348
    Pimelic Diphenylamide 106
    4 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-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-12220
    MM-102
    4 Publications Verification

    HMTase Inhibitor IX

    		 Histone Methyltransferase 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-106395A
    (Rac)-Telinavir

    (Rac)-SC-52151

    		 Others Infection
    (Rac)-Telinavir ((Rac)-SC-52151) is a potent, selective, tight-binding human immunodeficiency virus (HIV) protease inhibitor that exhibits significant anti-HIV activity. (Rac)-Telinavir has a mean 50% effective concentration of 26 ng/ml (43 nM) against various strains of HIV, including HIV-1, HIV-2, and simian immunodeficiency virus. (Rac)-Telinavir, in combination with nucleoside reverse transcriptase inhibitors, demonstrates synergistic effects on inhibiting HIV-1 replication without additive toxicity. (Rac)-Telinavir is highly protein bound in human plasma and exhibits low partitioning into erythrocytes.
    (Rac)-Telinavir
  • 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

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