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Binding site

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363

Inhibitors & Agonists

6

Screening Libraries

8

Fluorescent Dye

3

Biochemical Assay Reagents

56

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1

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2

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23

Natural
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26

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3

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4

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-157508
    VCP Activator 1

    		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
    MY-1442

    		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
    MY-875

    		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-18698
    L-701324

    		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-161800
    Aminoacyl tRNA synthetase-IN-3

    		Aminoacyl-tRNA Synthetase Infection
    Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysine tRNA synthetase (PfLysRS) from Plasmodium falciparum (IC50=59.2 nM), which inhibits the activity of PfLysRS by occupying the ATP binding site and L-lysine binding site of PfLysRS. Aminoacyl tRNA synthetase-IN-3 can be used in the development of antimalarial drugs .
    Aminoacyl tRNA synthetase-IN-3
  • HY-149020
    Tubulin polymerization-IN-26

    		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-19111
    R-82150

    TIBO-R 82150

    		 HIV Reverse Transcriptase Infection
    R-82150 (TIBO-R 82150) is an HIV-1 reverse transcriptase inhibitor that blocks the reverse transcription of viral RNA by binding to the non-substrate binding site of reverse transcriptase, thereby inhibiting viral replication. R-82150 does not inhibit the replication of HIV-2, other RNA viruses, and DNA viruses .
    R-82150
  • HY-D1608
    BODIPY FL Thapsigargin

    		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
    MY-673

    		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
    GABAA receptor agonist 2

    		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-147947
    Tubulin polymerization-IN-30

    		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-162659
    β2AR ligand 1

    		Adrenergic Receptor Others
    β2AR ligand 1 (Compound 4) is a homobivalent bitopic ligand for β2 adrenergic receptor (β2AR) on the orthosteric binding site (OBS) and the metastable binding sites (MBS) .
    β2AR ligand 1
  • HY-101344
    Cyanopindolol fumarate

    		5-HT Receptor Neurological Disease
    Cyanopindolol fumarate is a 5-HT receptor antagonist .
    Cyanopindolol fumarate
  • 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-P5343
    p53 CBS

    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-N7652
    Terminolic acid

    		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
    Akuammidine

    		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

    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-126054
    A1062

    		Others Others
    A1062 is an inhibitor for Tn3 encoded resolvase with IC50 in micromolar level. A1062 suppresses the binding of resolvase proteins to res sites, and blocks resolvase-induced site-specific recombination .
    A1062
  • HY-103172
    8-Aminoadenine

    		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
    (-)-α-Pinene

    		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-D1030
    Fluorescein Biotin

    		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
    Stains-All

    		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-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
    Pentiapine

    CGS 10746

    		 Dopamine Receptor Neurological Disease
    Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites .
    Pentiapine
  • HY-100998
    Metaphit

    		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-120524
    CGP 31358

    		iGluR Neurological Disease
    CGP 31358 is an anticonvulsant agent that binds to a site on the NMDA receptor complex that is coupled to both the transmitter recognition site and to the channel domain. CGP 31358 inhibits the binding of L-Glutamate to the NMDA receptor complex with an IC50 of 53 μM .
    CGP 31358
  • HY-119105
    LY81067

    		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-NP009
    α-Lactalbumin

    		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-163097
    ZCAN262

    		iGluR Neurological Disease
    ZCAN262 (compound 6 ) is an AMPA modulator. ZCAN262 prevents AMPA-mediated excitotoxicity by targeting an allosteric binding site .
    ZCAN262
  • HY-118168
    A 9387

    Galosfen

    		 Others Others
    A9387 is a Tn3-encoded resolvase protein that promotes site-specific recombination reactions between two directly repeated recombination sites. Several inhibitors have been isolated that inhibit this event. In this study, four inhibitors were tested at different steps of the recombination reaction. Two inhibitors, A9387 and A1062, inhibited the binding of resolvase to the res site. In addition, DNase I footprinting experiments showed that at certain concentrations of A9387 and A1062, resolvase preferred to bind to res site I containing the recombination junction. Two other inhibitors, A20812 and A21960, did not affect the binding and bending of resolvase to DNA but inhibited the formation of a synteny between resolvase and two directly repeated res sites.
    A 9387
  • HY-A0005
    Clofarabine
    4 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
    Fequesetide

    		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-163746
    BuChE-IN-11

    		Cholinesterase (ChE) Neurological Disease
    BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
    BuChE-IN-11
  • HY-B0149S
    Tranexamic acid-d2

    		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
    Methyl p-hydroxyphenyllactate

    		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-119453
    Oxycinchophen

    		Others Metabolic Disease Inflammation/Immunology
    Oxycinchophen exhibits anti-inflammatory and uricosuric activity. Oxycinchophen displaces urate from albumin, exhibits high affinity for the DNSA-binding site on the albumin molecule .
    Oxycinchophen
  • 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-118251
    PD130883

    		Antifolate Dihydrofolate reductase (DHFR) Cancer
    PD130883 is an antifolate DHFR inhibitor that directly inhibits thymidylate synthase at the 5,10-methylenetetrahydrofolate binding site, reducing the net conversion of tetrahydrofolate cofactor to dihydrofolate.
    PD130883
  • HY-100982
    (E)-4-Hydroxycrotonic acid

    trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA

    		 Others Neurological Disease
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
    (E)-4-Hydroxycrotonic acid
  • HY-153178
    HECT E3-IN-1

    		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-121820
    DMJ-I-228

    		HIV Infection
    DMJ-I-228 is a CD4-mimetic. DMJ-I-228 binds to HIV-1 gp120 within the conserved Phe 43 cavity near the CD4-binding site, thereby blocking CD4 binding and inhibiting HIV-1 infection .
    DMJ-I-228
  • HY-136280
    Panamesine

    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
    CHES

    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
    2 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-129927
    Thiomuscimol

    		Others Others
    Thiomuscimol is a GABAA receptor agonist (IC50=19 nM). It has been used as a photoaffinity label for the purification and identification of GABA binding sites within the GABAA receptor complex.
    Thiomuscimol
  • 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-146801
    PDHK-IN-3

    		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-120788
    VMAT2-IN-4

    		Monoamine Transporter Others
    VMAT2-IN-4 (compound 11) is a vesicular monoamine transporter-2 (VMAT2) inhibitor. VMAT2-IN-4 inhibits [ 3H]-DTBZ binding (Ki = 560 nM). VMAT2-IN-4 inhibits [ 3H]-DA (Ki = 45 nM) from entering vesicles and being taken up by cells. VMAT2-IN-4 can be used in methamphetamine addiction research .
    VMAT2-IN-4

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