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brain-permeable

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80

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-100614
    AS1517499
    Maximum Cited Publications
    35 Publications Verification

    STAT Inflammation/Immunology Cancer
    AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC50 of 21 nM.
    AS1517499
  • HY-16691
    AK-7
    3 Publications Verification

    Sirtuin Neurological Disease
    AK-7 is a selective cell- and brain-permeable SIRT2 inhibitor, with an IC50 of 15.5 μM.
    AK-7
  • HY-149966

    HDAC Inflammation/Immunology
    PB131 is a selective and brain-permeable HDAC6 inhibitor with high binding affinity (IC50: 1.8 nM). PB131 has potent anti-inflammatory activity. PB131 can be used for research of inflammation, especially neuroinflammation .
    PB131
  • HY-15262
    SRT 2104
    15+ Cited Publications

    Sirtuin Neurological Disease Metabolic Disease Cancer
    SRT 2104 is a first-in-class, highly selective and brain-permeable activator of the NAD + dependent deacetylase Sirt1, increases Sirt1 protein, but shows no effect on Sirt1 mRNA. Used in the research of diabetes mellitus and Huntington’s disease .
    SRT 2104
  • HY-131036

    Monoamine Oxidase Neurological Disease
    MAO-IN-M30 dihydrochloride is an orally active, brain-permeable, and brain selective irreversible MAO-A (IC50=37 nM) and MAO-B (IC50=57 nM) inhibitor. MAO-IN-M30 dihydrochloride is a potent iron chelator and radical scavenger. MAO-IN-M30 dihydrochloride has a neuroprotective effect against Dexamethasone-induced brain cell apoptosis. MAO-IN-M30 dihydrochloride also exhibits neurorestorative activity in post MPTP and lactacystin models of Parkinson's disease . MAO-IN-M30 (dihydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MAO-IN-M30 dihydrochloride
  • HY-136094

    Sirtuin Neurological Disease
    SRT3657 is a brain-permeable activator of SIRT1, with neuroprotective effect .
    SRT3657
  • HY-124947

    5-HT Receptor Neurological Disease
    PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI) .
    PF-4522654
  • HY-176487

    Toll-like Receptor (TLR) Neurological Disease
    SARM1-IN-6 (Compound 17a) is a brain-permeable SARM1 orthosteric inhibitor with IC50 of 14 nM for NAM and 74 nM for HEK cells .
    SARM1-IN-6
  • HY-10814

    nAChR Neurological Disease
    CP-810123 is a brain-permeable agonist of α7 nAChR for the research of cognitive impairment associated with psychiatric or neurological disorders such as schizophrenia and Alzheimer's disease .
    CP-810123
  • HY-119095

    Neurokinin Receptor Neurological Disease Endocrinology
    L-741671 is a selective and brain-permeable antagonist of neurokininl (hNKI) receptor, with Kis of 64 nM, 0.03 nM and 0.7 nM in rat, human and ferret, respectively .
    L-741671
  • HY-149202

    PGE synthase Inflammation/Immunology
    UT-11 is a potent and brain-permeable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor with IC50s of 0.10 μM and 2.00 μM for inhibiting PGE2 production in human (SK-N-AS) and murine (BV2) cells, respectively .
    UT-11
  • HY-P991380

    Transferrin Receptor Neurological Disease
    TXB4 is a brain-permeable human monoclonal antibody (mAb) targeting CD71. TXB4 prevents 6-OHDA-induced death of TH-positive neurons in the SNc in a 6-OHDA mouse model of Parkinson's disease (PD). TXB4 can be used in neurodegenerative diseases, acute brain and spinal cord injury, and depression research .
    TXB4
  • HY-14552
    Talnetant
    3 Publications Verification

    SB 223412

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant (SB 223412) is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant can be used in schizophrenia-related studies .
    Talnetant
  • HY-W686216

    Ferroptosis Neurological Disease
    VK-28, a brain-permeable iron chelator, inhibits both basal and Fe/ascorbate-induced mitochondrial membrane lipid peroxidation, with an IC50 of 12.7 μM. VK-28 exhibits significant neuroprotective effects on ICV-6-OHDA. VK-28 can be used for the research of Parkinson’s disease and other neurodegenerative diseases .
    VK-28
  • HY-14552A

    SB 223412 hydrochloride; SB 223412-A

    Neurokinin Receptor Neurological Disease Endocrinology
    Talnetant (SB 223412) hydrochloride is a selective, competitive, brain-permeable NK3 receptor antagonist with a Ki of 1.4 nM in hNK-3-CHO cells. Talnetant hydrochloride is 100-fold more selective for hNK-3 relative to the hNK-2 receptor and has no affinity for hNK-1. Talnetant hydrochloride can be used in schizophrenia-related studies .
    Talnetant hydrochloride
  • HY-18679

    mGluR Neurological Disease
    TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo .
    TC-N 22A
  • HY-133011

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease .
    nAChR agonist 1
  • HY-158115

    Molecular Glues Raf MEK Cancer
    NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. NST-628 inhibits RAS- and RAF-driven cancers and demonstrated potent inhibition in mutant KRAS, NRAS, BRAF class II/III, and NF1-mutant tumors .
    NST-628
  • HY-16936

    LRRK2 Neurological Disease
    JH-II-127 is an orally active, highly potent, selective and brain-permeable LRRK2 inhibitor, with IC50s of 6, 2 and 48 nM for wild-type LRRK2 and LRRK2-G2019S and mutant LRRK2-A2016T. JH-II-127 inhibits Ser935 phosphorylation in all tissues of mice, including the brain. JH-II-127 can be used in the study of parkinson's syndrome .
    JH-II-127
  • HY-172941

    NOD-like Receptor (NLR) Neurological Disease
    VEN-02XX is an orally active and brain-permeable NLRP3 inhibitor. VEN-02XX inhibits the release of IL-1β and IL-18 (IC50 0.3 and 0.28 μM, respectively). VEN-02XX restores memory and cognition, inhibits microgliosis, and reduces neuroinflammation and tau pathology in the 5XFAD/Rubicon KO mouse model. VEN-02XX may be used in the study of Alzheimer's disease (AD) .
    VEN-02XX
  • HY-155088

    mGluR Metabolic Disease
    MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
    MK-8768
  • HY-W156961

    PARP Neurological Disease
    LS-75 is a PARP-1 inhibitor with blood-brain permeability and IC50 value of 18 μM. LS-75 has neuroprotective activity .
    LS-75
  • HY-133555

    mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
    mGluR2 antagonist 1
  • HY-U00046

    COX Inflammation/Immunology
    Apyramide is an anti-inflammatory agent (NSAID) and behaves as a proagent of indomethacin (HY-14397). Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2.
    Apyramide
  • HY-10547
    OSU-03012
    5 Publications Verification

    AR-12; PDK1 inhibitor AR-12

    PDK-1 Autophagy Cancer
    OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM .
    OSU-03012
  • HY-107409

    iGluR Neurological Disease
    GNE 5729 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 37 nM for GluN2A, 4.7 and 9.5 μM for GluN2C and GluN2D, respectively.
    GNE 5729
  • HY-146101

    iGluR Neurological Disease
    NMDA receptor antagonist 5 (Compound 10e) is a potent, brain permeable and non-toxic NMDA receptor antagonist. NMDA receptor antagonist 5 can be used for neurological disorder research .
    NMDA receptor antagonist 5
  • HY-108337

    iGluR Neurological Disease
    GNE-0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively .
    GNE-0723
  • HY-163465

    Fluorescent Dye Neurological Disease
    DTNP is a BchE -activated near infrared (NIR) probe with blood-brain permeability. DTNP can be activated by BchE and inhibit its enzyme activity. DTNP can be used in Alzheimer's disease (AD) research .
    DTNP
  • HY-157132

    FAAH Neurological Disease
    FAAH-IN-8 (compound 11) is a competitive inhibitor of FAAH with an IC50 value of 6.7 nM and a Ki value of 5 nM. FAAH-IN-8 has high blood-brain permeability and a significant antioxidant profile with no neurotoxicity .
    FAAH-IN-8
  • HY-155079

    EGFR Cancer
    DZD1516 is a potent and selective HER2 inhibitor (IC50=0.56 nM) with good blood-brain permeability. DZD1516 exhibits antitumor activity in CNS and subcutaneous xenograft mouse models .
    DZD1516
  • HY-148246

    TGF-β Receptor Cancer
    MU1700 is an orally active and potent ALK1/2 inhibitor with IC50s of 13 nM and 6 nM, respectively. MU1700 shows cell membrane permeability and high brain permeability .
    MU1700
  • HY-163656

    Methionine Adenosyltransferase (MAT) Cancer
    MAT2A inhibitor 5(compound 39) is an orally active, selectivity and blood-brain permeability inhibitor of MAT2A with the IC50 of 11 nM. MAT2A inhibitor 5 inhibits tumor cell growth in vivo .
    MAT2A inhibitor 5
  • HY-110176

    GlyT Neurological Disease
    ASP2535 is a potent, orally bioavailable, selective, brain permeable and centrally-active glycine transporter-1 (GlyT1) inhibitor. ASP2535 can improve cognitive impairment in animal models of schizophrenia and Alzheimer's disease .
    ASP2535
  • HY-133898

    TAK-925

    Orexin Receptor (OX Receptor) Others
    Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms .
    Danavorexton
  • HY-161377

    TGF-β Receptor Cancer
    M4K2306 is a selective inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 7 nM. M4K2306 is blood brain permeable with a brain to plasma ratio of 75.6 .
    M4K2306
  • HY-161116

    Acetyl-CoA Carboxylase Cancer
    AD-5584 is an ACSS2 inhibitor with blood-brain permeability. AD-5584 can significantly reduce lipid storage, reduce colony formation, and increase cell death. AD-5584 has antitumor activity .
    AD-5584
  • HY-169107

    RIP kinase Neurological Disease
    RIPK1-IN-25 (WL8) is a blood-brain permeable RIPK1 inhibitor with EC50 and Kd values are 19.9 and 25 nM, respectively. RIPK1-IN-25 can be used in the study of neurometabolic diseases .
    RIPK1-IN-25
  • HY-162235

    Orexin Receptor (OX Receptor) Cardiovascular Disease
    CVN766 is an orally active inhibitor of orexin 1 receptor antagonist with blood-brain permeability with the IC50 values of 8 nM and >10 μM for OX1R and OX2R, respectively. CVN766 can be used for study schizophrenia .
    CVN766
  • HY-129545
    DS-1001b
    1 Publications Verification

    Isocitrate Dehydrogenase (IDH) Cancer
    DS-1001b is an orally active, blood-brain permeable, potent IDH-1 (isocitrate dehydrogenase-1) mutant inhibitor. DS-1001b has antitumor activity .
    DS-1001b
  • HY-108920

    4-Cl-KYN; AV-101

    iGluR Neurological Disease
    4-Chlorokynurenine (4-Cl-KYN) is a prodrug of a NMDA receptor antagonist, 7-Chlorokynurenic acid (HY-100811). 4-Chlorokynurenine has orally active and blood-brain permeability that can be used for the research of depression .
    4-Chlorokynurenine
  • HY-161376

    TGF-β Receptor Cancer
    M4K2281 is a selecitve inhibitor for activin receptor-like kinase-2 (ALK2) with an IC50 of 2 nM. M4K2281 exhibits a moderate blood brain permeability with a brain to plasma ratio of 3.7 at 4h .
    M4K2281
  • HY-172101

    Cholinesterase (ChE) Monoamine Oxidase Amyloid-β Neurological Disease
    AChE/MAO-B-IN-7 (VAV-8) is a blood-brain permeable dual inhibitor of acetylcholinesterase (AchE) and MAO-B agent. AChE/MAO-B-IN-7 can also inhibit Aβ42 aggregation for use in Alzheimer's disease (AD) research .
    AChE/MAO-B-IN-7
  • HY-153268

    BDTX-1535; EGFR-IN-76

    EGFR Cancer
    BDTX-1535 (EGFR-IN-76) is an orally available, blood-brain permeable, selective EGFR inhibitor with anti-tumor activity. BDTX-1535 is indicated in a variety of models including non-small cell lung cancer, glioblastoma patient-derived tumors, and intracranial tumors .
    Silevertinib
  • HY-158155

    Potassium Channel NOD-like Receptor (NLR) Neurological Disease Inflammation/Immunology
    CVN293 is a selective and brain permeable potassium ion (K +) channel KCNK13 inhibtor with IC50s of 41 nM and 28 nM for hKCNK13 and mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome mediated production of the proinflammatory cytokine IL-1β in microglia .
    CVN293
  • HY-14397S

    Indometacin-d4

    Isotope-Labeled Compounds COX Autophagy Inflammation/Immunology Cancer
    Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells . Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
    Indomethacin-d4
  • HY-111274

    Indometacin farnesil

    COX Autophagy Inflammation/Immunology
    Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes .
    Indomethacin farnesil
  • HY-B1343

    Cholinesterase (ChE) Neurological Disease
    Pridinol mesylate is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol mesylate reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol mesylate inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol mesylate
  • HY-B1343A

    Cholinesterase (ChE) Neurological Disease
    Pridinol is an orally active, blood-brain permeable, muscarinic acetylcholine receptor (mAChR)-directed muscle relaxant. Pridinol reduces the conduction of impulses to spinal motor neurons and exerts muscle relaxant activity. Pridinol inhibits skeletal muscle contractures in diseases of both central and peripheral origin and can be used in research in the field of musculoskeletal diseases .
    Pridinol
  • HY-161992

    Keap1-Nrf2 Apoptosis Neurological Disease Inflammation/Immunology
    Nrf2 activator-11 (compound M11) is a Nrf2 activator with blood-brain permeability. Nrf2 activator-11 has anti-oxidation, anti-inflammation, anti-ferroptosis and anti-apoptosis. Nrf2 activator-11 can be used to study cerebral  ischemia-reperfusion (CI/R) injury models .
    Nrf2 activator-11

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