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Results for "

penetrant

" in MCE Product Catalog:

187

Inhibitors & Agonists

3

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1

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4

Peptides

5

Natural
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2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-122138
    VU6010572

    mGluR Neurological Disease
    VU6010572 is a potent and selective mGlu3 negative allosteric modulator with IC50 of 245 nM. VU6010572 is highly CNS penetrant.
  • HY-15608
    MPTP hydrochloride

    Dopamine Receptor Apoptosis Neurological Disease Cancer
    MPTP hydrochloride is a brain penetrant dopamine neurotoxin, inducing Parkinson’s Disease. MPTP hydrochloride, a precusor of MPP +, induces apoptosis.
  • HY-120878A
    (R,R)-CXCR2-IN-2

    CXCR Inflammation/Immunology
    (R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
  • HY-121488
    GP130 receptor agonist-1

    Interleukin Related Neurological Disease
    GP130 receptor agonist-1 is a potent, brain-penetrant and orally active GP130 receptor agonist. GP130 receptor agonist-1 has a neuroprotective effect on NMDA-induced neurotoxicity.
  • HY-133554
    ASK1-IN-1

    p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
  • HY-134661A
    CVN424

    Others Neurological Disease
    CVN424 is an orally active and selective GPR6 inverse agonist with a EC50 of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research.
  • HY-15010
    L-371,257

    Oxytocin Receptor Vasopressin Receptor Endocrinology
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
  • HY-106968
    ZD-9379

    iGluR Neurological Disease
    ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect.
  • HY-102050
    PF-05085727

    Phosphodiesterase (PDE) Neurological Disease
    PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.
  • HY-134188
    JNJ-54717793

    Orexin Receptor (OX Receptor) Neurological Disease
    JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.
  • HY-10936
    S 18986

    iGluR Neurological Disease
    S 18986 is a selective, orally active, brain penetrant positive allosteric modulator of AMPA-type receptors. S 18986 shows cognitive enhancing properties in rodents. S 18986 activates the release of noradrenaline and acetylcholine in rat hippocampus and enhances rat memory in object-recognition tests.
  • HY-15722
    SB-222200

    Neurokinin Receptor Neurological Disease Endocrinology
    SB-222200 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant NK-3 receptor antagonist. SB-222200 is developed for central nervous system (CNS) disorders.
  • HY-132308
    DYRK1-IN-1

    DYRK Neurological Disease
    DYRK1-IN-1 is a highly selective and ligand-efficient DYRK1A inhibitor. DYRK1-IN-1 inhibits DYRK1A phosphorylation activity with an IC50 value of 220 nM. DYRK1-IN-1 can be used for the research of central nervous system penetrant DYRK1A chemical probe.
  • HY-114153
    PLX5622

    c-Fms Neurological Disease
    PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals.
  • HY-114153A
    PLX5622 hemifumarate

    c-Fms Neurological Disease
    PLX5622 hemifumarate is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM). PLX5622 hemifumarate allows for extended and specific microglial elimination, preceding and during pathology development. PLX5622 hemifumarate demonstrates desirable PK properties in varies animals.
  • HY-12959
    Repinotan

    BAY x 3702 free base

    5-HT Receptor Neurological Disease
    Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
  • HY-133016
    M8891

    Others Cancer Cardiovascular Disease
    M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
  • HY-120878
    CXCR2-IN-2

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
  • HY-136233
    PSB 0777 ammonium

    Adenosine Receptor Inflammation/Immunology
    PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
  • HY-111653
    CycLuc1

    Reactive Oxygen Species Others
    CycLuc1 is a brain penetrant luciferase substrate.
  • HY-10622
    PF-00446687

    Melanocortin Receptor Endocrinology
    PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.
  • HY-110254
    AZD 9272

    mGluR Neurological Disease
    AZD 9272 is a brain penetrant mGluR5 antagonist.
  • HY-12829
    SR-3306

    JNK Neurological Disease
    SR-3306 is a selective, potent, highly brain penetrant JNK inhibitor.
  • HY-18163A
    GNE-7915 tosylate

    LRRK2 Neurological Disease
    GNE-7915 tosylate is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-18163
    GNE-7915

    LRRK2 Neurological Disease
    GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.
  • HY-13796
    IPSU

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    IPSU is a selective, orally available and brain penetrant OX2R antagonist with a pKi of 7.85.
  • HY-12477
    PF-06447475

    LRRK2 Neurological Disease
    PF-06447475 is a highly potent, selective and brain penetrant LRRK2 inhibitor with an IC50 of 3 nM.
  • HY-100026
    PQR620

    mTOR Cancer
    PQR620 is an orally bioavailable and selective brain penetrant inhibitor of mTORC1/2.
  • HY-12282
    GNE-9605

    LRRK2 Neurological Disease
    GNE-9605 is a highly potent, selective, and brain-penetrant LRRK2 inhibitor with IC50 of 19 nM.
  • HY-101718
    Aticaprant

    CERC-501; LY-2456302

    Opioid Receptor Neurological Disease
    Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
  • HY-102020
    RG3039

    PF-06687859

    Others Neurological Disease
    RG3039 (PF-06687859) is an orally bioavailable and brain-penetrant DcpS inhibitor with an IC50 of 0.069 nM.
  • HY-14174
    MRK-560

    γ-secretase Neurological Disease
    MRK-560 is a potent, orally bioavailable and brain-penetrant γ-secretase inhibitor.
  • HY-125880
    SBI-553

    Neurotensin Receptor Endocrinology Neurological Disease
    SBI-553 is a potent and brain penetrant NTR1 allosteric modulator, with an EC50 of 0.34 μM.
  • HY-104028
    BAY 73-6691

    (R)-BAY 73-6691

    Phosphodiesterase (PDE) Neurological Disease
    BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.
  • HY-117632
    ABX-1431

    MAGL Neurological Disease
    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  • HY-101022
    CXCR2-IN-1

    CXCR Inflammation/Immunology Endocrinology
    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
  • HY-109566
    AZD1390

    ATM/ATR Cancer Inflammation/Immunology
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell.
  • HY-110255
    AZD 2066

    mGluR Neurological Disease
    AZD 2066 is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 has antinociception effects.
  • HY-110255A
    AZD 2066 hydrate

    mGluR Neurological Disease
    AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects.
  • HY-128569
    ALK-IN-5

    ALK Neurological Disease
    ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK), with an IC50 of 2.9 nM.
  • HY-10629
    LXR-623

    WAY 252623

    LXR Metabolic Disease Cancer
    LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
  • HY-114926
    KT185

    MAGL Neurological Disease
    KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells.
  • HY-133813A
    Apovincaminic acid hydrochloride salt

    Drug Metabolite Neurological Disease
    Apovincaminic acid hydrochloride salt is an orally active and brain-penetrant main active metabolite of Vinpocetine (VP). Apovincaminic acid hydrochloride salt exerts a neuroprotective type of action.
  • HY-100366
    Lu AF21934

    mGluR Neurological Disease
    Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.
  • HY-131002
    DPTIP

    Phospholipase Inflammation/Immunology
    DPTIP is a potent brain penetrant neutral sphingomyelinase 2 (N-SMase 2) inhibitor (exosome inhibitor), with an IC50 of 30 nM.
  • HY-137442
    Inupadenant

    EOS-850

    Adenosine Receptor Cancer
    Inupadenant is an orally active, highly selective A2A receptor antagonist. Inupadenant is not brain-penetrant. Inupadenant has potent anti-tumor activity.
  • HY-W015309
    Decanoic acid

    iGluR Neurological Disease
    Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects.
  • HY-15796
    GNE0877

    LRRK2 Neurological Disease
    GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.
  • HY-112623
    Vafidemstat

    ORY-2001

    Histone Demethylase Monoamine Oxidase Neurological Disease
    Vafidemstat (ORY-2001) is an oral, brain penetrant, dual lysine-specific histone demethylase (LSD1)/MAO-B inhibitor.
  • HY-114403
    VU6012962

    mGluR Neurological Disease
    VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM) with an IC50 of 347 nM.
  • HY-117626
    LP-935509

    Others Inflammation/Immunology Neurological Disease
    LP-935509 is a selective, ATP-competitive and brain-penetrant inhibitor of adapter protein-2 associated kinase 1 (AAK1) with an IC50 and a Ki of 3.3 nM and 0.9 nM, respectively. LP-935509 is also a potent inhibitor of BIKE (IC50=14 nM) and a modest inhibitor of GAK (IC50=320 nM). LP-935509 is highly brain-penetrant and reverses fully established pain behavior following the SNL procedure.
  • HY-109055
    Elenbecestat

    E2609

    Beta-secretase Neurological Disease
    Elenbecestat (E2609) is a potent, orally bioavailable and CNS-penetrant BACE-1 inhibitor. Elenbecestat has the potential for Alzheimer's disease (AD) research.
  • HY-12981
    RG7713

    RO5028442

    Vasopressin Receptor Neurological Disease Endocrinology
    RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
  • HY-110123
    ML-00253764 hydrochloride

    Melanocortin Receptor Cancer Endocrinology
    ML-00253764 hydrochloride is a brain penetrant nonpeptidic melanocortin receptor 4 (MC4R) antagonist with a Ki and IC50 of 0.16 µM and 0.103 µM, respectively.
  • HY-100182
    BACE1-IN-1

    Beta-secretase Neurological Disease
    BACE1-IN-1 is a potent and highly brain penetrant BACE1 inhibitor with IC50s of 32 and 47 nM for human BACE1 and BACE2, respectively.
  • HY-114396
    BR351

    MMP Cancer
    BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  • HY-112157
    PF-06751979

    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.
  • HY-112286
    PI3Kγ inhibitor 2

    PI3K Inflammation/Immunology
    PI3Kγ inhibitor 2 (Compound 16) is an orally bioavailable, CNS-penetrant, isoform selective PI3Kγ inhibitor with a Ki of 4 nM.
  • HY-12776
    GSK805

    ROR Inflammation/Immunology
    GSK805 is a potent, orally bioavailable, and CNS penetrant RORγt inhibitor with pIC50 of 8.4 and >8.2 for RORγ FRET assay and Th17 assay.
  • HY-104003
    S 38093

    Histamine Receptor Neurological Disease Endocrinology
    S 38093 is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
  • HY-17001
    Flupirtine Maleate

    Potassium Channel iGluR Neurological Disease
    Flupirtine Maleate is a brain penetrant, and orally bioavailable, non-opioid and centrally acting analgesic agent. Flupirtine Maleate is an indirect N-methyl-D-aspartate receptor (NMDAR) antagonist. Neuroprotective properties.
  • HY-16636
    ML337

    mGluR Neurological Disease
    ML337 is a selective and brain-penetrant negative allosteric modulator of mGlu3, with an IC50 of 593 nM. ML337 possesses a favorable dystrophia myotonica protein kinase (DMPK) and ancillary pharmacology profile.
  • HY-110278
    ADX71743

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
  • HY-111351
    MLK-IN-1

    Mixed Lineage Kinase Neurological Disease
    MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1.
  • HY-112217A
    PSEM 89S TFA

    nAChR Neurological Disease
    PSEM 89S TFA is a selective and brain penetrant agonists for the resulting ion channels. PSEM 89S TFA is orthogonally selective for Q79G and L141F, respectively.
  • HY-107982
    VU6005649

    mGluR Neurological Disease
    VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.
  • HY-16425
    RG2833

    RGFP109

    HDAC Cancer
    RG2833 is a brain-penetrant HDAC inhibitor with IC50s of 60 nM and 50 nM for HDAC1 and HDAC3, respectively. The Ki values for HDAC1 and HDAC3 are 32 and 5 nM, respectively.
  • HY-108703
    Foliglurax

    PXT002331

    mGluR Neurological Disease
    Foliglurax (PXT002331) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-109024
    Balovaptan

    RG7314

    Vasopressin Receptor Neurological Disease Endocrinology
    Balovaptan (RG7314) is a highly potent and selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
  • HY-100732
    Cambinol

    Sirtuin Apoptosis Phospholipase Cancer
    Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-119943
    PF-06256142

    Dopamine Receptor Neurological Disease
    PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
  • HY-14859
    Dipraglurant

    ADX48621

    mGluR Neurological Disease
    Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC50 of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo.
  • HY-136660
    PQR626

    mTOR Neurological Disease
    PQR626, a rapamycin derivative, is a potent, selective, orally active, and brain-penetrant mTOR inhibitor, with an IC50 and Ki of 5 nM and 3.6 nM, respectively. PQR626 can be can be used for the research of neurological disorders.
  • HY-136430
    JCN037

    JGK037

    EGFR Cancer
    JCN037 (JGK037) is non-covalent and BBB-penetrant EGFR tyrosine kinase inhibitor, with IC50 values of 2.49 nM, 3.95 nM, 4.48 nM for EGFR, p-wtEGFR and pEGFRvⅢ, respectively.
  • HY-B0534
    Moclobemide

    Ro111163

    Monoamine Oxidase Neurological Disease
    Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A.Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
  • HY-108710
    VU0650786

    mGluR Neurological Disease
    VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents.
  • HY-13662
    Lansoprazole

    AG-1749

    Proton Pump Bacterial Phospholipase Inflammation/Immunology Cancer
    Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-108703A
    Foliglurax monohydrochloride

    PXT002331 (monohydrochloride)

    mGluR Neurological Disease
    Foliglurax monohydrochloride (PXT002331 monohydrochloride) is a highly selective and potent, brain-penetrant metabotropic glutamate receptor 4 positive allosteric modulator (mGluR4 PAM) , with an EC50 of 79 nM. Antiparkinsonian effect.
  • HY-10716A
    PF-03463275

    GlyT Neurological Disease
    PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research.
  • HY-13662A
    Lansoprazole sodium

    AG-1749 sodium

    Proton Pump Phospholipase Bacterial Inflammation/Immunology
    Lansoprazole sodium (AG 1749 sodium) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole sodium (AG 1749 sodium) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-112612A
    RTI-13951-33 hydrochloride

    Others Neurological Disease
    RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats.
  • HY-112612
    RTI-13951-33

    Others Neurological Disease
    RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats.
  • HY-133016A
    (R)-M8891

    Others Others
    (R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor.
  • HY-15976
    P7C3

    Others Neurological Disease
    P7C3 is an orally bioavailable and blood-brain barrier penetrant aminopropyl carbazole, with neuroprotective effects. P7C3 can be used for the research of neurodegenerative diseases, including Parkinson's disease.
  • HY-100483
    A-804598

    P2X Receptor Cancer
    A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
  • HY-43586
    BR351 precursor

    MMP Cancer
    BR351 precursor is a precursor of BR351. BR351 is a brain penetrant MMP inhibitor with IC50s of 4, 2, 11, 50 nM for MMP2, MMP8, MMP9 and MMP13, respectively.
  • HY-117508
    JNJ-54175446

    P2X Receptor Neurological Disease
    JNJ-54175446 is a potent and selective brain penetrant P2X7 receptor antagonist, with pIC50s of 8.46 and 8.81 for hP2X7 receptor and rP2X7 receptor, respectively.
  • HY-13058
    ADX-47273

    mGluR Neurological Disease
    ADX-47273 is a potent, selective and brain-penetrant mGluR5 positive allosteric modulator (PAM), with an EC50 of 0.17 μM for potentiation of glutamate (50 nM) response. ADX-47273 has antipsychotic and procognitive activities.
  • HY-117516
    SR10067

    Others Neurological Disease
    SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
  • HY-116819
    VU0453379

    Glucagon Receptor Metabolic Disease
    VU0453379 is a highly selective and central nervous system (CNS) penetrant positive allosteric modulator (PAM) of glucagon-like peptide-1R (GLP-1R) with an EC50 of 1.3 μM.
  • HY-111455
    LP-211

    5-HT Receptor Neurological Disease
    LP-211 is a selective and blood−brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
  • HY-101116
    GLP-1R Antagonist 1

    Glucagon Receptor Metabolic Disease
    GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM.
  • HY-12206
    Thioperamide

    MR-12842

    Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-10328
    Neflamapimod

    VX-745

    p38 MAPK Autophagy Inflammation/Immunology
    Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
  • HY-12206A
    Thioperamide maleate

    MR-12842 maleate

    Histamine Receptor Neurological Disease
    Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide maleate inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-13662B
    (R)-Lansoprazole

    Dexlansoprazole

    Proton Pump Inflammation/Immunology
    (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-12768
    Sotuletinib

    BLZ945

    c-Fms Cancer
    Sotuletinib (BLZ945) is a potent, selective and brain-penetrant CSF-1R (c-Fms) inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
  • HY-134968
    TTBK1-IN-1

    Others Neurological Disease
    TTBK1-IN-1 is a potent, selective and brain-penetrant tau tubulin kinase 1 (TTBK1) inhibitor with an IC50 of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies.
  • HY-129586
    AT-007

    Aldose Reductase Metabolic Disease
    AT-007 is an orally active central nervous system (CNS) penetrant Aldose Reductase inhibitor for treatment of Galactosemia with an IC50 value of 100 pM. AT-007 reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.
  • HY-14569
    CDPPB

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
  • HY-13459
    PF-5274857

    Smo Cancer
    PF-5274857 is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
  • HY-19630
    ML289

    VU0463597

    mGluR Neurological Disease
    ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC50=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5.
  • HY-116761
    GSK467

    Histone Demethylase Cancer
    GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM, shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members.
  • HY-13459A
    PF-5274857 hydrochloride

    Smo Cancer
    PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
  • HY-14602
    Tramiprosate

    Homotaurine; 3-Amino-1-propanesulfonic acid

    Amyloid-β Cancer
    Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects.
  • HY-18750
    Zorifertinib

    AZD3759

    EGFR Cancer
    Zorifertinib (AZD3759) is a potent, orally active, central nervous system-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively.
  • HY-137472
    SAR502250

    GSK-3 Neurological Disease
    SAR502250 is a potent, selective, ATP competitive, orally active and brain-penetrant inhibitor of GSK3, with an IC50 of 12 nM for human GSK-3β. SAR502250 displays antidepressant-like activity. SAR502250 can be used for the research of Alzheimer’s disease (AD).
  • HY-120111
    MW-150

    MW01-18-150SRM

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-P1335
    CTAP

    Opioid Receptor Neurological Disease
    CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
  • HY-12567
    ML375

    VU0483253

    mAChR Neurological Disease
    ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC50s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4.
  • HY-107365
    PQR530

    PI3K mTOR Cancer
    PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
  • HY-10847
    SB-277011

    SB-277011A

    Dopamine Receptor Neurological Disease
    SB-277011 is a potent and delective dopamine D3 receptor antagonist (pKi values are 8.0, 6.0, 5.0 and <5.2 for D3, D2, 5-HT1D and 5-HT1B respectively); brain penetrant.
  • HY-131971
    AChE/BChE-IN-1

    AChE Neurological Disease
    AChE/BChE-IN-1 is a potent and brain-penetrant dual inhibitor of Acetylcholinesterase and Butyrylcholinesterase, with IC50s of 1.06 and 7.3 nM for hAChE and hBChE, respectively. AChE/BChE-IN-1 also has antioxidant activity. AChE/BChE-IN-1 can be used for the research of Alzheimer’s disease.
  • HY-17363
    Dimethyl fumarate

    DMF

    Keap1-Nrf2 Reactive Oxygen Species HIV Autophagy Endogenous Metabolite Cancer Infection Inflammation/Immunology Neurological Disease
    Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
  • HY-105692
    DR2313

    PARP Neurological Disease
    DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo.
  • HY-14450
    JNJ-31020028

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    JNJ-31020028 is a selective brain penetrant antagonist of neuropeptide Y2 receptor with high affinity (pIC50=8.07, human; pIC50=8.22 rat); >100-fold selective versus human Y1/Y4/Y5 receptors.
  • HY-139279
    TPX-0131

    ALK Cancer
    TPX-0131 is a potent, selective, CNS-penetrant and orally active inhibitor of wild-type ALK (IC50 of 1.4 nM) and ALK-resistant mutation, e.g. G1202R (IC50 of 0.3 nM), L1196M (IC50 of 0.3 nM). TPX-0131 has strong antitumor activities.
  • HY-P1335A
    CTAP TFA

    Opioid Receptor Neurological Disease
    CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
  • HY-16936
    JH-II-127

    LRRK2 Neurological Disease
    JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
  • HY-103493
    TAK-915

    Phosphodiesterase (PDE) Neurological Disease
    TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment.
  • HY-12215
    Lorlatinib

    PF-06463922

    ALK ROS Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib has anticancer activity.
  • HY-134189A
    EST73502 hydrochloride

    Sigma Receptor Opioid Receptor Neurological Disease
    EST73502 hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 hydrochloride has antinociceptive activity.
  • HY-134189
    EST73502

    Opioid Receptor Sigma Receptor Neurological Disease
    EST73502 is a selective, orally active and blood-brain barrier (BBB) penetrant dual μ-opioid receptor (MOR) agonist and σ1 receptor (σ1R) antagonist, with Kis of 64 nM and 118 nM for MOR and σ1R, respectively. EST73502 has antinociceptive activity.
  • HY-128772
    XPC-6444

    Sodium Channel Neurological Disease
    XPC-6444 is a highly potent, isoform-selective, and CNS-penetrant NaV1.6 inhibitor (IC50=41 nM for hNaV1.6). XPC-6444 also displays potent block of NaV1.2 (IC50=125 nM). XPC-6444 shows anticonvulsant activity.
  • HY-106003
    GSK356278

    Phosphodiesterase (PDE) Inflammation/Immunology Neurological Disease
    GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects.
  • HY-126244
    CDK4/6-IN-3

    CDK Cancer
    CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.
  • HY-114452A
    LY2940094 tartrate

    BTRX-246040 tartrate

    Opioid Receptor Neurological Disease
    LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with high affinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models.
  • HY-116451
    PF-04859989 hydrochloride

    Others Neurological Disease
    PF-04859989 hydrochloride is a brain-penetrant, irreversible kynurenine aminotransferase (KAT) II inhibitor with IC50s of 23 and 263 nM for hKAT II and rKAT II. PF-04859989 hydrochloride is selective for KAT II over human KAT I, KAT III, and KAT IV (IC50s of 22, 11, and >50 μM, respectively).
  • HY-101478
    Fenobam

    mGluR Neurological Disease
    Fenobam is a selective, orally active, and brain-penetrant mGluR5 antagonist acting at an allosteric modulatory site (Kds of 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively). Fenobam displays inverse agonist activity which blocks the mGlu5 receptor basal activity with an IC50 of 84 nM. Fenobam exerts anxiolytic activity.
  • HY-14418
    VU0361737

    ML-128

    mGluR Neurological Disease
    VU0361737 (ML-128) is a potent, selective and CNS penetrant positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4 PAM), with EC50s of 240 nM and 110 nM for human and rat mGluR4 receptors, respectively. VU0361737 has neuroprotective effect. VU0361737 is potential for Parkinson's disease research.
  • HY-120619
    BMS-193885

    Neuropeptide Y Receptor Neurological Disease Endocrinology
    BMS-193885 is a potent, selective, competitive, and brain penetrant neuropeptide Y1 receptor antagonist with a Ki of 3.3 nM, and has an IC50 of 5.9 nM for hY1, which displays > 100, > 160, > 160 and > 160-fold selectivity over α1, hY2, hY4 and hY5 receptors, respectively .
  • HY-109192
    Tolebrutinib

    SAR442168; PRN2246

    Btk Neurological Disease
    Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS).
  • HY-14325
    L-745870

    Dopamine Receptor Neurological Disease
    L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-131881
    JHU37160

    mAChR Neurological Disease
    JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
  • HY-14325A
    L-745870 trihydrochloride

    Dopamine Receptor Neurological Disease
    L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-10985
    Marizomib

    Salinosporamide A; NPI-0052

    Proteasome Cancer
    Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
  • HY-120111A
    MW-150 hydrochloride

    MW01-18-150SRM hydrochloride

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-131891
    JHU37152

    mAChR Neurological Disease
    JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue.
  • HY-112601
    IDH1 Inhibitor 1

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1 R132H, IDH1 R132C, and IDH1 WT, respectively. Anticancer activity.
  • HY-14325B
    L-745870 hydrochloride

    Dopamine Receptor Neurological Disease
    L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-B0688
    Dapsone

    4,4′-Diaminodiphenyl sulfone; DDS

    Antibiotic Parasite Bacterial Reactive Oxygen Species Infection Inflammation/Immunology
    Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al.
  • HY-12439
    ML380

    mAChR Neurological Disease
    ML380 is a potent, subtype-selective, and brain-penetrant positive allosteric modulator (PAM) of M5 mAChR, with EC50s of 190 and 610 nM for human and rat M5, respectively. ML380 exhibits moderate selectivity versus the M1 and M3 mAChR subtypes. ML380 could increase the affinity of ACh for the M5 mAChR.
  • HY-109052
    Atabecestat

    JNJ-54861911

    Beta-secretase Neurological Disease
    Atabecestat (JNJ-54861911) is a potent brain-penetrant and orally active β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor, achieves robust and high CSF Aβ reduction. Atabecestat (JNJ-54861911) is tolerated and displays a sustained pharmacokinetic (PK) and pharmacodynamic (PD) characteristics. Atabecestat (JNJ-54861911) has the potential for Alzheimer's Disease treatment.
  • HY-B0113A
    Omeprazole sodium

    H 16868 sodium

    Proton Pump Autophagy Bacterial Phospholipase Cancer Infection Metabolic Disease
    Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-A0031
    Bazedoxifene

    TSE-424

    Estrogen Receptor/ERR Cancer
    Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
  • HY-17387
    (-)-Huperzine A

    Huperzine A

    AChE Apoptosis iGluR Neurological Disease
    (-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
  • HY-100719
    BRD-6929

    HDAC HIV Infection Cardiovascular Disease
    BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.
  • HY-P1061
    Colivelin

    STAT Amyloid-β Neurological Disease
    Colivelin is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin has the potential for the treatment of alzheimer's disease and ischemic brain injury
  • HY-120111B
    MW-150 dihydrochloride dihydrate

    MW01-18-150SRM dihydrochloride dihydrate

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease
    MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
  • HY-114226
    Olutasidenib

    FT-2102

    Isocitrate Dehydrogenase (IDH) Cancer Inflammation/Immunology
    Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
  • HY-124634
    PZ-2891

    Others Neurological Disease
    PZ-2891 is an orally bioavailable, brain penetrant pantothenate kinase (PANK) modulator. PZ-2891 act as an orthosteric inhibitor at high concentrations and an allosteric activator at lower sub-saturating concentrations. PZ-2891 inhibits human pantothenate kinases PANK1β, PANK2, and PANK3 with IC50s of 40.2 nM, 0.7 nM and 1.3 nM, respectively.
  • HY-137466
    ARN-21934

    Topoisomerase Cancer
    ARN-21934 is a potent, highly selective, blood-brain barrier (BBB) penetrant inhibitor for human topoisomerase II α over β. ARN-21934 inhibits DNA relaxation with an IC50 of 2 μM as compared to the anticancer agent Etoposide (IC50=120 μM). ARN-21934 exhibits a favorable in vivo pharmacokinetic profile and is a promising lead compound for anticancer research.
  • HY-A0031A
    Bazedoxifene hydrochloride

    TSE-424 hydrochloride

    Estrogen Receptor/ERR Cancer
    Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.
  • HY-131031
    KCC-07

    DNA Alkylator/Crosslinker Cancer
    KCC-07 is a potent, selective and brain-penetrant MBD2 (methyl-CpG-binding domain protein 2) inhibitor. KCC-07 prevents binding of MBD2 to methylated DNA and activates brain specific angiogenesis inhibitor 1 (BAI1) inducing anti-proliferative BAI1/p53/p21 signaling. Anticancer activity.
  • HY-136390
    ML417

    Dopamine Receptor Neurological Disease
    ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.
  • HY-B0410A
    Pramipexole dihydrochloride hydrate

    Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride hydrate is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride hydrate can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-109118A
    Masupirdine mesylate

    SUVN-502 mesylate

    5-HT Receptor Neurological Disease
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-P1061A
    Colivelin TFA

    STAT Amyloid-β Apoptosis Neurological Disease
    Colivelin TFA is a brain penetrant neuroprotective peptide and a potent activator of STAT3, suppresses neuronal death by activating STAT3 in vitro. Colivelin TFA exhibits long-term beneficial effects against neurotoxicity, Aβ deposition, neuronal apoptosis, and synaptic plasticity deficits in neurodegenerative disease. Colivelin TFA has the potential for the treatment of alzheimer's disease and ischemic brain injury.
  • HY-B0113
    Omeprazole

    H 16868

    Proton Pump Autophagy Bacterial Phospholipase Cancer Infection Metabolic Disease
    Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
  • HY-134923
    CA77.1

    Autophagy Neurological Disease
    CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research.
  • HY-B0410
    Pramipexole

    Dopamine Receptor Neurological Disease
    Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-106634
    Mitoguazone

    Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG

    HIV Apoptosis Cancer Infection
    Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
  • HY-17355
    Pramipexole dihydrochloride

    Dopamine Receptor Neurological Disease
    Pramipexole dihydrochloride is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole dihydrochloride can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-19752A
    VU0357017 hydrochloride

    CID-25010775

    mAChR Neurological Disease
    VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
  • HY-12868
    Bimiralisib

    PQR309

    PI3K mTOR Cancer
    Bimiralisib (PQR309) is a potent, brain-penetrant, orally bioavailable, pan-class I PI3K/mTOR inhibitor with IC50s of 33 nM, 451 nM, 661 nM, 708 nM and 89 nM for PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ and mTOR, respectively. Bimiralisib is an mTORC1 and mTORC2 inhibitor.
  • HY-124761
    Poloppin

    Polo-like Kinase (PLK) Autophagy Cancer
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
  • HY-104036
    IDH-305

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH-305 is an orally available, mutant-selective and brain-penetrant IDH1 inhibitor that targets IDH1 (R132) mutation. IDH-305 exhibits greater than 200 fold selectivity for mutant IDH1 isoforms vs. WT (IC50= 27 nM (IDH1 R132H), 28 nM (IDH1 R132C), 6.14 µM (IDH1 WT)).
  • HY-59201A
    A-582941 dihydrochloride

    nAChR 5-HT Receptor Neurological Disease
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
  • HY-B0688S
    Dapsone D8

    4,4′-Diaminodiphenyl sulfone D8; DDS D8

    Antibiotic Parasite Bacterial Reactive Oxygen Species Infection Inflammation/Immunology
    Dapsone D8 (4,4′-Diaminodiphenyl sulfone D8) is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, such as leprosy, dermatitis herpetiformis, acne vulgaris et al.
  • HY-136569
    DSR-141562

    Phosphodiesterase (PDE) Neurological Disease
    DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
  • HY-111520
    NVS-SM2

    DNA/RNA Synthesis Neurological Disease
    NVS-SM2 is a potent, orally active and brain-penetrant SMN2 splicing enhancer with an EC50 of 2 nM for SMN. NVS-SM2 enhances U1-pre-mRNA association. NVS-SM2 promotes exon 7 inclusion and restores normal survival motor neuron (SMN) protein expression. NVS-SM2 can be used for spinal muscular atrophy (SMA) research.
  • HY-105685
    SRX246

    Vasopressin Receptor Neurological Disease
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-119939
    CHDI-390576

    HDAC Cancer
    CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
  • HY-128879
    VP3.15

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-103565
    AMN082

    mGluR Neurological Disease
    AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects.
  • HY-128879A
    VP3.15 dihydrobromide

    Phosphodiesterase (PDE) GSK-3 Neurological Disease
    VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  • HY-109086
    Edicotinib

    JNJ-40346527; JNJ-527

    c-Fms Inflammation/Immunology Neurological Disease
    Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively. Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research.
  • HY-107479
    (R)-JNJ-31020028

    Neuropeptide Y Receptor Neurological Disease
    (R)-JNJ-31020028 is a high affinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects.
  • HY-123857
    JNJ-55308942

    P2X Receptor Inflammation/Immunology Neurological Disease
    JNJ-55308942 is a high-affinity, selective, brain-penetrant P2X7 functional antagonist (hP2X7: IC50=10 nM, Ki=7.1 nM; rP2X7: IC50=15 nM, Ki=2.9 nM). JNJ-55308942 is orally bioavailable, binds to brain P2X7 and blocks IL-1β release from adult rodent brain.
  • HY-109118
    Masupirdine free base

    SUVN-502 free base

    5-HT Receptor Neurological Disease
    Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
  • HY-103169
    SCH442416

    Adenosine Receptor Neurological Disease
    SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). SCH442416 can be used for imaging of adenosine A2A receptors in rat and primate brain.
  • HY-B0410S
    Pramipexole (N-Propyl-3,3,3-d3) (dihydrochloride)

    Dopamine Receptor Neurological Disease
    Pramipexole (N-Propyl-3,3,3-d3) dihydrochloride is the deuterium labeled Pramipexole. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
  • HY-112289
    IDH889

    Isocitrate Dehydrogenase (IDH) Cancer
    IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
  • HY-12624
    ON123300

    CDK AMPK Cancer
    ON123300, a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors. ON123300 inhibits CDK6 with an IC50 of 9.82 nM.
  • HY-104042
    Vorasidenib

    AG-881

    Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K.
  • HY-131997
    2'MeO6MF

    GABA Receptor Inflammation/Immunology Neurological Disease
    2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
  • HY-18137
    PF-04995274

    5-HT Receptor Neurological Disease
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.