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good permeability

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62

Inhibitors & Agonists

5

Screening Libraries

1

Fluorescent Dye

2

Peptides

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • 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-11054

    meso-GS 164

    Others Neurological Disease
    TH-237A(meso-GS 164) is a neuroprotective agent with good blood-brain barrier permeability.
    TH-237A
  • HY-103266

    Aurora Kinase Cancer
    TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity .
    TC-A 2317 hydrochloride
  • HY-163350

    GPR84 Inflammation/Immunology
    TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability .
    TUG-2208
  • HY-15023
    Cligosiban
    5+ Cited Publications

    PF-3274167

    Oxytocin Receptor Endocrinology
    Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
    Cligosiban
  • HY-155992

    Sigma Receptor Neurological Disease
    WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
    WLB-89462
  • HY-147285

    mTOR PI3K Neurological Disease
    PI3K/mTOR Inhibitor-9 (Compound 1) is a potent mTOR and PI3K inhibitor with IC50 values of 38 nM, 6.6 μM, 6.6 μM and 0.8 μM against mTOR (phospho-S6 cellular assay), PI3Kα, PI3Kγ and PI3Kδ, respectively .
    PI3K/mTOR Inhibitor-9
  • HY-153715

    Mitochondria modulator-1

    Biochemical Assay Reagents Metabolic Disease
    Mitochondria modulator-1 is a mitochondrial regulator that stimulates mitochondrial ATP production. Mitochondria modulator-1 has good oral bioavailability, blood-brain barrier permeability, and good plasma stability. Mitochondria modulator-1 has the potential to study mitochondrial diseases .
    NV-354
  • HY-118147

    Fatty Acid Synthase (FASN) Others Cancer
    ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouse plasma .
    ML356
  • HY-153241

    Epigenetic Reader Domain Cancer
    GSK737 is a BRD4 BD1 and BD2 inhibitor, with pIC50 values of 5.3 and 7.3 respectively. GSK737 has low clearance and good solubility and permeability in rat .
    GSK737
  • HY-D2317

    Fluorescent Dye Others
    HaloFlipper 30 is a fluorescent probe that covalently reacts with HaloTag fusion proteins to form an ester bond, which allows the probe to be stably attached to membrane structures. HaloFlipper 30 has high specificity, precision and good cell permeability .
    HaloFlipper 30
  • HY-163797

    DNA/RNA Synthesis Cancer
    WRN inhibitor 10 (Compound P24) is an inhibitor for the Werner helicase WRN with an IC50 of 1.1 nM. WRN inhibitor 10 inhibits the proliferation of cancer cell SW48 with IC50 of 39 nM. WRN inhibitor 10 exhibits good liver microsomal stability and film permeability. WRN inhibitor 10 exhibits good pharmacokinetic characteristics in CD-1 mice .
    WRN inhibitor 10
  • HY-134406

    Phosphodiesterase (PDE) Neurological Disease
    6-Cl-cPuMP (sodium) is a cAMP analog with active chlorine function. 6-Cl-cPuMP (sodium) has good membrane permeability and phosphodiesterase (PDE) stability. 6-Cl-cPuMP (sodium) can be used for nervous system research .
    6-Cl-cPuMP sodium
  • HY-147726

    Microtubule/Tubulin Cancer
    Microtubule inhibitor 5 (compound 17f) is a potent microtubule inhibitor. Microtubule inhibitor 5 shows cytotoxicity with an IC50 value of 154.5 nM for NCI-H460 cells. Microtubule inhibitor 5 shows good cell permeability .
    Microtubule inhibitor 5
  • HY-149820

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 of 0.014 μM. MAO-B-IN-22 has high antioxidant activity, good metal chelating ability, proper BBB permeability and significant neuroprotective effect .
    MAO-B-IN-22
  • HY-161380

    Fungal Infection
    Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .
    Antifungal agent 96
  • HY-103234A

    iGluR Neurological Disease
    GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
    GYKI 52466 dihydrochloride
  • HY-147738

    Fluorescent Dye Others
    SQM-NBD is a potent and selectiveAIE fluorescent probe. SQM-NBD exhibits excellent sensitivity to Cys and Hcy with the LOD of 54 nM and 72 nM, respectively.SQM-NBD has good cell permeability and low cytotoxicity. SQM-NBD has the potential for Cys/Hcy identification under physiological and pathological conditions .
    SQM-NBD
  • HY-103234

    iGluR Neurological Disease
    GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
    GYKI 52466
  • HY-149242

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-20 (Compound C14) is a potent MAO-B inhibitor with an IC50 of 0.037 μM. MAO-B-IN-20 displays good metabolic stability and brain-blood barrier permeability. MAO-B-IN-20 can be used for the research of Parkinson's disease .
    MAO-B-IN-20
  • HY-103234B

    iGluR Neurological Disease
    GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
    GYKI 52466 hydrochloride
  • HY-161381

    Phosphodiesterase (PDE) TNF Receptor Inflammation/Immunology
    PDE4-IN-15 (compound 7b-1) is an inhibitor of PDE4 (IC50 = 0.17 μM) and has anti-TNF-α activity (EC50 = 0.19 μM). PDE4-IN-15 has a good skin permeability .
    PDE4-IN-15
  • HY-136026

    BLU-5937

    P2X Receptor Inflammation/Immunology
    Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
    Camlipixant
  • HY-124638

    MNK Cancer
    MNK inhibitor 9 is a potent and selective inhibitor of MNK1/2 with IC50 values of 0.003 µM and 0.003 µM for MNK1 and MNK2 respectively. MNK inhibitor 9 has good cell permeability. MNK inhibitor 9 can be used in tumor related research .
    MNK inhibitor 9
  • HY-137016

    HCN Channel Neurological Disease
    8-Pcpt-cGMP is an agonist for cyclic nucleotide-gated (CNG) channel with an EC50 of 0.5 μM. 8-Pcpt-cGMP exhibits good membrane permeability. 8-Pcpt-cGMP can be used in studies about the function of CNG channels in visual signal transduction and olfactory transduction .
    8-Pcpt-cGMP
  • HY-156432

    Anaplastic lymphoma kinase (ALK) mTOR PARP Caspase Cancer
    ALK-IN-26 is an ALK inhibitor with IC50 value of 7.0 μM for ALK tyrosine kinase. ALK-IN-26 has good pharmacokinetic properties and blood-brain barrier (BBB) permeability. ALK-IN-26 can induce apoptosis, autophagy and necrosis. ALK-IN-26 can be used in glioblastoma studies .
    ALK-IN-26
  • HY-161643

    Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
    S21-1011
  • HY-159091

    HIV Integrase Infection
    HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
    HIV-1 integrase inhibitor 12
  • HY-160656

    5-HT Receptor Neurological Disease
    5-HT/NA Reuptake inhibitor-1 (compound 9) is a selective dual 5-HT and NA reuptake inhibitor with IC50 of 660 nM and 70 nM respectively. . 5-HT/NA Reuptake inhibitor-1 has good in vitro human metabolic stability, hERG selectivity and passive membrane permeability .
    5-HT/NA Reuptake inhibitor-1
  • HY-163563

    Ligands for Target Protein for PROTAC Neurological Disease
    JYQ-173 is a selective inhibitor for human Parkinson disease protein 7 (PARK7), with an IC50 of 19 nM. JYQ-173 exhibits good cell permeability. JYQ-173 is the ligand for target protein PARK7, which can be utilized for synthesis of PROTAC Degrader JYQ-194 (HY-163564) .
    JYQ-173
  • HY-13340

    VU152100

    mAChR Neurological Disease
    VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
    VU0152100
  • HY-100855

    Histone Methyltransferase Cancer
    DC_C66 is a cell-permeable, selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 1.8 μM. DC_C66 has a good selectivity for CARM1 against PRMT1 (IC50=21 μM), PRMT6 (IC50= 47μM), and PRMT5 .
    DC_C66
  • HY-144660

    Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
    AChE-IN-7
  • HY-143330

    Monoamine Oxidase Neurological Disease
    MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
    MAO-B-IN-4
  • HY-122614
    S29434
    2 Publications Verification

    NMDPEF

    Autophagy Neurological Disease
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 induces autophagy and inhibits QR2-mediated ROS production .
    S29434
  • HY-147397

    Pyruvate Kinase Cancer
    PKM2 activator 3 is a potent PKM2 activator with an AC50 value of 90 nM. PKM2 activator 3 has good Caco-2 permeability, a low efflux ratio and high microsomal stability. PKM2 activator 3 can be used for researching anticancer .
    (AC50: the concentration which gives 50% activation of enzyme.)
    PKM2 activator 3
  • HY-151368

    Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-10 (Compound 7b) is a potent dual AChE and BChE inhibitor with IC50 values of 0.176, and 0.47 μM, respectively. AChE/BChE-IN-10 shows good blood brain barrier permeability. AChE/BChE-IN-10 can inhibit Aβ-aggregation and be used in Alzheimer’s disease (AD) research .
    AChE/BChE-IN-10
  • HY-152614

    Parasite Infection
    Antimalarial agent 19 (compound 6e) is an antimalarial active agent. Antimalarial agent 19 has antimalarial activity for the blood stage of P. falciparum K1 and P. berghei with EC50 values of 0.3 µM, 15.3 µM, respectively. Antimalarial agent 19 has good aqueous solubility, intestinal permeability and microsomal stability compared to gamhepathiopine .
    Antimalarial agent 19
  • HY-161663

    Phosphodiesterase (PDE) Cardiovascular Disease
    Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
    Phosphodiesterase-IN-2
  • HY-163799

    Histone Methyltransferase Cancer
    PRMT5-MTA-IN-1 (Compound A9a) is an inhibitor for protein arginine methyltransferase PRMT5-MTA. PRMT5-MTA-IN-1 inhibits the proliferation of colorectal cancer cell HCT116 wildtype and MTAP del mutant, with an IC50 of 16 nM and 2.47 μM. PRMT5-MTA-IN-1 exhibits good liver microsomal stability and film permeability. PRMT5-MTA-IN-1 exhibits good pharmacokinetic characteristics in CD-1 mice .
    PRMT5-MTA-IN-1
  • HY-155541

    Apoptosis Cancer
    Antitumor agent-110 (compound 13) is an anticancer imidazotetrazine with good permeability properties. Antitumor agent-110 arrests cell cycel at G2/M phase, and induces apoptosis . Antitumor agent-110 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Antitumor agent-110
  • HY-155478

    Androgen Receptor Cancer
    Androgen receptor-IN-6 (compound 16) is an orally available androgen receptor (Androgen Receptor) potent inhibitor (IC50=0.12 μM in vitro), targeting the disordered N-terminal domain (NTD). Androgen receptor-IN-6 has good Caco2 cell membrane permeability and has an oral activity (F/%) of 16% in male CD-1 mice .
    Androgen receptor-IN-6
  • HY-P10698

    LDLR Neurological Disease
    VH-N412 is a vectorized neuropeptide (NT) with good blood-brain barrier permeability. VH-N412 binds to the low-density lipoprotein receptor (LDLR) and neuropeptide receptor 1 (NTSR-1), and acts as a pharmacological-induced hypothermia (PIH) inducer. VH-N412 exhibits anticonvulsant and neuroprotective effects, and can be used in the study of neurological diseases such as epilepsy.
    VH-N412
  • HY-144272

    Cholinesterase (ChE) 5-HT Receptor Serotonin Transporter Neurological Disease
    AChE-IN-5 (compound 5) exhibits strong in vitro bioactivity against AChE/5-HT1A/SERT and exhibits good BBB permeability. AChE-IN-5 shows IC50 value 2.29 nM against AChE, EC50 value 58.6 nM against 5-HT1A and IC50 value against SERT. Orally active .
    AChE-IN-5
  • HY-118858

    EAAT Neurological Disease Cancer
    UCPH-102 is a highly selective EAAT1 inhibitor with an IC50 of 0.43 µM. UCPH-102 exhibits a specific anti-proliferative effect on T-ALL cells. UCPH-102 also shows good blood-brain permeability, which can be used in studies of amyotrophic lateral sclerosis, Alzheimer’s disease, chronic pain and obsessive compulsive disorder .
    UCPH-102
  • HY-137016A

    HCN Channel Neurological Disease
    8-Pcpt-cGMP sodium is the sodium salt form of 8-Pcpt-cGMP (HY-137016). 8-Pcpt-cGMP sodium is an agonist for cyclic nucleotide-gated (CNG) channel with an EC50 of 0.5 μM. 8-Pcpt-cGMP sodium exhibits good membrane permeability. 8-Pcpt-cGMP sodium can be used in studies about the function of CNG channels in visual signal transduction and olfactory transduction .
    8-Pcpt-cGMP sodium
  • HY-119190

    Phosphodiesterase (PDE) Neurological Disease
    PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study .
    PF-06445974
  • HY-138648

    Others Neurological Disease
    PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
    PB1
  • HY-168152

    SARS-CoV Virus Protease Infection
    SARS-CoV-2 3CLpro-IN-26 (Compound (S,R)-4y) is an allosteric inhibitor for SARS-CoV-2 3CLpro with an IC50 of 0.43 μM. SARS-CoV-2 3CLpro-IN-26 exhibits good cell permeability and is able to effectively cross the cell membrane, after co-incubation with Vero-E6 cells .
    SARS-CoV-2 3CLpro-IN-26
  • HY-146049

    Parasite Infection
    Antitrypanosomal agent 4 (compound 19) is a potent and blood-brain barrier permeable antitrypanosomal agent. Antitrypanosomal agent 4 has good activity against Trypanosoma cruzi (T. cruzi) and Trypanosoma brucei brucei (T. b. brucei) with IC50s of 1.2 μM and 70 nM, respectively . Antitrypanosomal agent 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Antitrypanosomal agent 4

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