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stimuli

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27

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3

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3

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2

Natural
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1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108460

    TRP Channel Neurological Disease
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
    A-784168
  • HY-B0562

    Carbonic Anhydrase Cardiovascular Disease Metabolic Disease
    Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro .
    Methyclothiazide
  • HY-106660

    Dopamine Receptor Neurological Disease
    BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
    BP 897 hydrochloride
  • HY-123388

    Others Others Inflammation/Immunology
    SCH 12223 free base is an orally available drug that protects the gastric and intestinal epithelium from harmful irritants .
    SCH 12223 free base
  • HY-P5440

    ERK Others
    ERKtide is a biological active peptide. (ERKtide is a peptide substrate for ERK2. Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by mitogenic stimuli.)
    ERKtide
  • HY-136392

    IKK Inflammation/Immunology
    IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively .
    IKK-IN-3
  • HY-114085

    Dopamine Receptor Neurological Disease
    BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a high affinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
    BP 897
  • HY-B0562R

    Reference Standards Carbonic Anhydrase Cardiovascular Disease Metabolic Disease
    Methyclothiazide (Standard) is the analytical standard of Methyclothiazide. This product is intended for research and analytical applications. Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro .
    Methyclothiazide (Standard)
  • HY-129236

    Na+/K+ ATPase Apoptosis Cancer
    Hellebrin is a bufadienolide compound extracted from plants that can inhibit tumor cell growth. Hellebrigenin shows potential in overcoming cancer cells' resistance to apoptosis stimuli and has also demonstrated anti-proliferation effects in multidrug-resistant (MDR) cancer cell models. Hellebrin can act on Na+/K+-ATPase to regulate intracellular signaling pathways .
    Hellebrin
  • HY-114981

    Sirtuin Inflammation/Immunology
    SRTCX1002 is a potent activator of SIRT1 (STAC), suppresses inflammatory responses through promotion of p65 deacetylation and inhibition of NF-κB Activity. SRTCX1002 suppresses stimuli-induced NF-κB transcriptional activation and LPS-induced TNFα secretion with IC50s of 0.71 and 7.58 µM, respectively .
    SRTCX1002
  • HY-163607

    Apoptosis NF-κB Cancer
    SpiD3, a spirocyclic dimer, is an anticancer agent. SpiD3 markedly inhibits malignant B-cell proliferation and suppressed NF-κB activation independent of TME-associated stimuli. SpiD3 induces apoptosis and inhibits protein synthesis in chronic lymphocytic leukemia cells. SpiD3 can be used for study of chronic lymphocytic leukemia (CLL) .
    SpiD3
  • HY-149143
    JNJ-28583113
    2 Publications Verification

    TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-N2543R

    (E/Z)-Damascenone (Standard)

    Reference Standards NF-κB Endogenous Metabolite Inflammation/Immunology
    Damascenone (Standard) is the analytical standard of Damascenone. This product is intended for research and analytical applications. Damascenone ((E/Z)-Damascenone) is an active compound of Epipremnum pinnatum with anti-inflammatory activity . Damascenone is a mixture complex of E-isomer-Damascenone and Z-isomer Damascenone.
    Damascenone (Standard)
  • HY-N2543
    Damascenone
    1 Publications Verification

    (E/Z)-Damascenone

    NF-κB Endogenous Metabolite Inflammation/Immunology
    Damascenone ((E/Z)-Damascenone) is an active compound of Epipremnum pinnatum with anti-inflammatory activity . Damascenone is a mixture complex of E-isomer-Damascenone and Z-isomer Damascenone.
    Damascenone
  • HY-B0364A
    Dyclonine hydrochloride
    1 Publications Verification

    Dyclocaine hydrochloride

    Bacterial Fungal Aldehyde Dehydrogenase (ALDH) Infection Cancer
    Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
    Dyclonine hydrochloride
  • HY-117702

    Prolyl Endopeptidase (PREP) Aminopeptidase Metabolic Disease
    RB 101 is an active mixed inhibitor against two enzymes which metabolize the enkephalins neutral endopeptidase and aminopeptidase N. RB 101 has rather long-lasting antinociceptive effects. RB 101 inhibits the in vivo [ 3H]DPN binding both under basal conditions and after swim stress in mice. RB 101 can be used to determine the precise in vivo localization of enkephalinergic pathways recruited by various stimuli .
    RB 101
  • HY-108035

    MR04A3

    GABA Receptor Neurological Disease
    (-)-JM-1232 (MR04A3) targets GABA A receptors and exerts its analgesic effects by binding to the benzodiazepine binding site of GABA A receptors. (-)-JM-1232 demonstrates potent analgesic effects in mice against acute thermal stimuli, mechanically induced pain, and visceral pain, with CI50 values of 2.96, 3.06, and 2.27 mg/kg, respectively. (-)-JM-1232 can be used in research related to pain and analgesia .
    (-)-JM-1232
  • HY-B0364AR

    Dyclocaine hydrochloride (Standard)

    Reference Standards Bacterial Fungal Aldehyde Dehydrogenase (ALDH) Infection Cancer
    Dyclonine (hydrochloride) (Standard) is the analytical standard of Dyclonine (hydrochloride). This product is intended for research and analytical applications. Dyclonine (Dyclocaine) hydrochloride is an orally effective ALDH covalent inhibitor (crosses blood-brain barrier), with an IC50 of 35 μM for ALDH2 and 76 μM for ALDH3A1. Dyclonine hydrochloride has sensitizing activities for targeted cancer cells and antibacterial. Dyclonine hydrochloride is also a local agent that can suppress or relieve pain. that blocks the transmission of various nerve impulses or stimuli and inhibits the sensation of touch and pain .
    Dyclonine hydrochloride (Standard)
  • HY-101849
    Fasentin
    4 Publications Verification

    GLUT TNF Receptor Apoptosis Cardiovascular Disease Cancer
    Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
    Fasentin
  • HY-168773

    EAAT Neurological Disease
    (R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research .
    (R)-AS-1
  • HY-156104

    PROTACs CaMK Neurological Disease
    CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains .
    CaMKIIα-PHOTAC
  • HY-P10464

    TRP Channel Neurological Disease Inflammation/Immunology
    TAT-AKAP79 326-336 is a cytoosmotic peptide. TAT-AKAP79 326-336 mimics a specific region on the AKAP79 protein that binds to TRPV1 ion channels (amino acid sequence 326-336). TAT-AKAP79 326-336 inhibits the sensitization of TRPV1 and reduce the overresponse of TRPV1 channels to stimuli caused by the activation of cellular kinases such as protein kinase A (PKA) and protein kinase C (PKC) by inflammatory mediators. TAT-AKAP79 326-336 can be used to study the mechanism of pain transduction and inflammatory hyperalgesia .
    Tat-AKAP79 (326-336)
  • HY-101849R

    Reference Standards GLUT TNF Receptor Apoptosis Cardiovascular Disease Cancer
    Fasentin (Standard) is the analytical standard of Fasentin. This product is intended for research and analytical applications. Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC50=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity .
    Fasentin (Standard)
  • HY-112825

    Platelet-activating Factor Receptor (PAFR) Inflammation/Immunology
    TSI-01 is a pro-inflammatory phospholipid mediator that is rapidly synthesized by lyso-PAF acetyltransferase (lyso-PAFAT) in response to extracellular stimuli. Two types of lyso-PAFAT have been identified: lysophosphatidylcholine acyltransferase (LPCAT)1, which is mostly expressed in the lungs, and LPCAT2, which is expressed in inflammatory cells. TSI-01 is a selective inhibitor of LPCAT2 (IC50s=0.47 versus 3.02 μM for human LPCAT2 and LPCAT1, respectively). 60 μM it is shown to suppress PAF biosynthesis in mouse peritoneal macrophages stimulated with a calcium ionophore.
    TSI-01
  • HY-A0139

    NSC 108165; Navan; Navane

    Sigma Receptor mAChR Histamine Receptor Dopamine Receptor Adrenergic Receptor Others
    Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    Thiothixene
  • HY-W748758

    NSC 108165-d8; Navan-d8; Navane-d8

    Isotope-Labeled Compounds Dopamine Receptor Histamine Receptor mAChR Adrenergic Receptor Sigma Receptor Others
    (Z)-Thiothixene-d8 (NSC 108165-d8; Navan-d8; Navane-d8) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
    (Z)-Thiothixene-d8
  • HY-170872

    PROTACs DNA/RNA Synthesis Cancer
    PT-129 is an RPOTAC degrader targeting the NTF2 domain (protein-RNA interaction site) of G3BP1/2, which mediates the disassembly of intracellular stress granules. PT-129 can inhibit the formation of stress granules in stressed cells and disassemble existing stress granules, and can disrupt the transmission of ATF4, thereby inhibiting the proliferation of cancer cells. Stress granules (SGs) are membrane-less cytoplasmic compartments formed under stress stimuli. SGs promote the transmission of ATF4 from fibroblasts to tumor cells through a migratory effect, mediating fibroblast-related tumor growth. And G3BP1/2 is a central protein of the SGs network, and the inhibition of G3BP1/2 may reduce the stress resistance of cancer cells in the tumor microenvironment. PT-129 is composed of a target protein ligand (red part) G3BP1/2-Targeting ligand-1 (HY-170873), an E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a PROTAC linker (black part) Amino-PEG3-C2-acid (HY-W040165); among them, the E3 ligase ligand + linker form a complex Thalidomide-NH-PEG3-propionic acid (HY-136166) .
    PT-129

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