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binding sites

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255

Inhibitors & Agonists

6

Screening Libraries

8

Fluorescent Dye

2

Biochemical Assay Reagents

41

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1

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1

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14

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24

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157508

    p97 Others
    VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
    VCP Activator 1
  • HY-162089

    Microtubule/Tubulin Apoptosis Cancer
    MY-1442 (I-3) is a microtubulin polymerization inhibitor. MY-875 inhibits tubulin polymerization by targeting colchicine binding sites. MY-1442 has anticancer activity. MY-1442 can induce apoptosis of MGC-803 cells and inhibit cell migration .
    MY-1442
  • HY-150761

    Microtubule/Tubulin Apoptosis Cancer
    MY-875 is a competitive microtubulin polymerization inhibitor with an IC50 value of 0.92 μM. MY-875 inhibits microtubulin polymerization by targeting colchicine binding sites and activates the Hippo pathway. MY-875 induces apoptosis and has anticancer activity .
    MY-875
  • HY-149020

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin polymerization-IN-26 (compound 12h) can inhibit the polymerization of microtubulin by binding to the colchicine binding site of microtubulin with an IC50 value of 4.64 μM. Tubulin polymerization-IN-26 can induce apoptosis and inhibit cell metastasis or migration, and can be used as a potential compound for lung cancer research .
    Tubulin polymerization-IN-26
  • HY-D1608

    Calcium Channel Others
    BODIPY FL Thapsigargin is a potent green fluorescent dye. BODIPY FL Thapsigargin inhibits intracellular SERCA-type Ca2+ pumps present in the sarcoplasmic/endoplasmic reticulum. BODIPY FL Thapsigargin used for investigation of thapsigargin binding sites in live cells .
    BODIPY FL Thapsigargin
  • HY-149414

    Microtubule/Tubulin Apoptosis ERK TGF-beta/Smad Cancer
    MY-673 is a colchicine binding site inhibitor (CBSI), that inhibits tubulin polymerization. MY-673 inhibits the ERK signaling pathway, which in turn affects SMAD4 protein expression levels in the TGF-β/SMAD pathway. MY-673 inhibited cell proliferation, migration and induced apoptosis in vivo and in vitro .
    MY-673
  • HY-147736

    GABA Receptor Neurological Disease
    GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression .
    GABAA receptor agonist 2
  • HY-18698

    iGluR Neurological Disease
    L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with high affinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
    L-701324
  • HY-147947

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-30 (compound 6e) is a potent Tubulin polymerization inhibitor. Tubulin polymerization-IN-30 is a colchicine binding site inhibitor. Tubulin polymerization-IN-30 can disrupt intracellular microtubule organization, arrest cell cycle at the G2/M phase. Tubulin polymerization-IN-30 exhibits the high potency against the cancer cell lines including SGC-7901, A549 and HeLa, with IC50 values of 2.16, 2.21, and 0.403 μM .
    Tubulin polymerization-IN-30
  • HY-P5343

    p53 Consensus binding sequence

    MDM-2/p53 Others
    p53 CBS (p53 Consensus binding sequence) is a biological active peptide. (p53 consensus DNA binding site)
    p53 CBS
  • HY-101344

    5-HT Receptor Neurological Disease
    Cyanopindolol fumarate is a 5-HT receptor antagonist .
    Cyanopindolol fumarate
  • HY-N7652

    Bacterial Infection Inflammation/Immunology
    Terminolic acid is a pentacyclic triterpenoid glucoside isolated from Combretum racemosum. Terminolic acid can inhibit the pro-inflammatory cytokines by binding to receptor active site of IL-1β and IL-6, and enhance anti-inflammatory cytokines by binding to IL-4 receptor binding sites. Terminolic acid also exhibits moderate antibacterial activity .
    Terminolic acid
  • HY-N7437

    Opioid Receptor DNA/RNA Synthesis Neurological Disease Inflammation/Immunology
    Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties .
    Akuammidine
  • HY-107578

    Macbecin I; NSC 330499

    HSP Cancer
    Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities .
    Macbecin
  • HY-103172

    nAChR Metabolic Disease
    8-Aminoadenine is an adenine receptor ligand, with a Ki of 6.51 μM at the human binding site .
    8-Aminoadenine
  • HY-N0549

    GABA Receptor Bacterial Virus Protease Endogenous Metabolite Neurological Disease
    (-)-α-Pinene is a monoterpene and shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site .
    (-)-α-Pinene
  • HY-18601
    (±)-BI-D
    5 Publications Verification

    HIV HIV Integrase Infection
    (±)-BI-D is a potent ALLINI(An allosteric IN inhibitor) that binds integrase at the LEDGF/p75 binding site.
    (±)-BI-D
  • HY-100143

    CGS 10746

    Dopamine Receptor Neurological Disease
    Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites .
    Pentiapine
  • HY-D1030

    Fluorescent Dye Inflammation/Immunology
    Fluorescein Biotin is used as an alternative to radioactive biotin for detecting and quantitating biotin-binding sites by either fluorescence or absorbance; the the fluorescence or absorbance of Fluorescein Biotin is quenched, upon binding to avidin or streptavidin.
    Fluorescein Biotin
  • HY-D0987

    Calmodulin Others
    Stains-All, a cationic carbocyanine dye, is a convenient probe to study the structural features of the individual calcium-binding sites of calmodulin (CaM) and related calcium-binding proteins (CaBP) .
    Stains-All
  • HY-100998

    Others Neurological Disease
    Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates . Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms .
    Metaphit
  • HY-119105

    Others Neurological Disease
    LY81067, a diaryltriazine, effectively protects against Pentylenetetrazole- and Picrotoxin-induced convulsions in mice. LY81067 exerts its anticonvulsant effects by binding to or near Picrotoxin (HY-101391) binding sites .
    LY81067
  • HY-163097

    iGluR Neurological Disease
    ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site .
    ZCAN262
  • HY-A0005
    Clofarabine
    3 Publications Verification

    Nucleoside Antimetabolite/Analog Autophagy Apoptosis Metabolic Disease Cancer
    Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit .
    Clofarabine
  • HY-16307
    MB05032
    4 Publications Verification

    FBPase Metabolic Disease
    MB05032 is a special and efficacious gluconeogenesis inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM.
    MB05032
  • HY-P2463

    Arp2/3 Complex Inflammation/Immunology
    Fequesetide, a peptide segment, is the active site within the protein thymosin β4 responsible for actin binding, cell migration and wound healing .
    Fequesetide
  • HY-B0149S

    Isotope-Labeled Compounds Cardiovascular Disease
    Tranexamic acid-d2 is the deuterium labeled Tranexamic acid. Tranexamic acid (Transamin) is an antifibrinolytic for blocking lysine-binding sites of plasmin and elastase-derived plasminogen fragments.
    Tranexamic acid-d2
  • HY-N3269

    Others Others
    Methyl p-hydroxyphenyllactate (MeHPLA) is an important cell growth-regulating agent which binds to nuclear type II binding sites in normal and malignant cells .
    Methyl p-hydroxyphenyllactate
  • HY-B0115
    Pizotifen
    2 Publications Verification

    Pizotyline; BC-105

    5-HT Receptor Neurological Disease
    Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen
  • HY-153178

    E1/E2/E3 Enzyme Others
    HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor. HECT E3-IN-1 (compound 3) disrupts Ub binding to the noncovalent Ub-binding site of Nedd4-1 .
    HECT E3-IN-1
  • HY-136280

    EMD 57445

    Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-D0871

    N-Cyclohexyltaurine

    Biochemical Assay Reagents Others
    CHES (N-Cyclohexyltaurine) is a zwitterionic buffer. CHES can bind to hemagglutinin (HA) emulating with sialic acid (SA) and receptor binding site (RBS)-targeting broadly neutralizing antibodies .
    CHES
  • HY-17592
    Bithionol
    1 Publications Verification

    Parasite Bacterial Infection Cancer
    Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM) .
    Bithionol
  • HY-12062
    PD318088
    1 Publications Verification

    MEK Cancer
    PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
    PD318088
  • HY-136299
    Sepimostat
    1 Publications Verification

    FUT-187 free base

    iGluR Neurological Disease
    Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
    Sepimostat
  • HY-136299A

    FUT-187

    iGluR Neurological Disease
    Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
    Sepimostat dimethanesulfonate
  • HY-B0115A
    Pizotifen malate
    2 Publications Verification

    Pizotyline malate; BC-105 malate

    5-HT Receptor Neurological Disease
    Pizotifen malate (Pizotyline malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen malate
  • HY-P0186

    Opioid Receptor Neurological Disease
    Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2
  • HY-100815B

    (±)-AMPA

    (RS)-AMPA ((±)-AMPA) is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA
  • HY-100815D

    (±)-AMPA monohydrate

    iGluR Neurological Disease
    (RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA monohydrate
  • HY-124673

    Neurotensin Receptor Neurological Disease
    AF40431, the first reported small-molecule ligand of sortilin, has an IC50 of 4.4 µM and a Kd of 0.7 µM . AF40431 is bound in the neurotensin-binding site of sortilin .
    AF40431
  • HY-152156

    Microtubule/Tubulin Apoptosis Cancer
    Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis .
    Tubulin inhibitor 11
  • HY-157543

    Microtubule/Tubulin Cancer
    Tubulin polymerization-IN-59 ((R)-9k) is a potent inhibitor of colchicine binding site inhibitor (CBSI). Tubulin polymerization-IN-59 inhibits tubulin polymerization .
    Tubulin polymerization-IN-59
  • HY-101178

    iGluR Neurological Disease
    L-689560 is a potent N-methyl-D-aspartate (NMDA) receptor antagonist at the GluN1 glycine binding site. L-689560 is widely used as a radiolabeled ligand in binding studies and used for study the roles of NMDA receptors in normal neurological processes as well as in diseases .
    L-689560
  • HY-129123

    Antibiotic Infection
    ML318 is a biaryl nitrile inhibitor of PvdQ acylase with an IC50 of 20 nM by binding in the acyl-binding site. ML318 inhibits P. aeruginosa (PAO1) with an IC50 of 19 μM. ML318 prevents pyoverdine production and limits the growth of P. aeruginosa under iron-limiting conditions .
    ML318
  • HY-146801

    PDHK Metabolic Disease Cancer
    PDHK-IN-3 (compound 7) is a potent PDHK (pyruvate dehydrogenase kinase) inhibitor, with IC50 values of 0.21 and 1.54 μM for PDHK2 and PDHK4, respectively .
    PDHK-IN-3
  • 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-P0186A

    Opioid Receptor Neurological Disease
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
    Endomorphin 2 TFA
  • HY-131941

    GABA Receptor Neurological Disease
    SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
    SJM-3
  • HY-100815C

    (±)-AMPA hydrobromide

    (RS)-AMPA ((±)-AMPA) hydrobromide is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA hydrobromide does not interfere with binding sites for kainic acid or NMDA receptors .
    (RS)-AMPA hydrobromide

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