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HEK

" in MedChemExpress (MCE) Product Catalog:

423

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11

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4

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18

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2

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7

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7936

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17

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GMP Molecules

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-19608
    GSK1016790A
    35+ Cited Publications

    TRP Channel Calcium Channel Cardiovascular Disease Metabolic Disease
    GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEK cells .
    GSK1016790A
  • HY-112683
    V-9302
    30+ Cited Publications

    ASCT Cancer
    V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 μM) in HEK-293 cells .
    V-9302
  • HY-136626
    Z-Ala-Ala-Asn-AMC
    3 Publications Verification

    Cbz-Ala-Ala-Asn-AMC

    Fluorescent Dye Cancer
    Z-Ala-Ala-Asn-AMC (Cbz-Ala-Ala-Asn-AMC) is the legumain substrate. Overexpressed legumain in 293 HEK-Leg cells potently cleaved CBZ-Ala-Ala-Asn-AMC .
    Z-Ala-Ala-Asn-AMC
  • HY-126010
    Dooku1
    15+ Cited Publications

    Piezo Channel Others
    Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca 2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .
    Dooku1
  • HY-12805
    ML171
    15+ Cited Publications

    2-Acetylphenothiazine; 2-APT

    NADPH Oxidase Cardiovascular Disease
    ML171 (2-Acetylphenothiazine;2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation, with an IC50 of 0.25 μM in HEK293-Nox1 confirmatory assay.
    ML171
  • HY-101560
    Linrodostat
    5+ Cited Publications

    BMS-986205; ONO-7701

    Indoleamine 2,3-Dioxygenase (IDO) Cancer
    Linrodostat (BMS-986205) is a selective and irreversible indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 value of 1.1 nM in IDO1-HEK293 cells. Linrodostat is well tolerated with potent pharmacodynamic activity in advanced cancers .
    Linrodostat
  • HY-112683A
    V-9302 hydrochloride
    30+ Cited Publications

    ASCT Cancer
    V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5) not ASCT1. V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells .
    V-9302 hydrochloride
  • HY-15518
    LCL161
    40+ Cited Publications

    IAP Cancer
    LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.
    LCL161
  • HY-17038
    Agomelatine
    5+ Cited Publications

    S-20098

    Melatonin Receptor 5-HT Receptor Endogenous Metabolite Neurological Disease
    Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
    Agomelatine
  • HY-136555
    GSK717
    5+ Cited Publications

    NOD-like Receptor (NLR) Inflammation/Immunology
    GSK717 is a potent, selective NOD2 (nucleotide-binding oligomerization domain 2) inhibitor. GSK717 inhibits muramyl dipeptide (MDP)-induced NOD2-mediated signaling, with an IC50 of 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells .
    GSK717
  • HY-108317

    Phosphatase Cancer
    ABL127 is a selective and covalent inhibitor of protein methylesterase 1 (PME-1) with IC50s of 6.4 nM and 4.2 nM in HEK293T and MDA-MB-231 cells, respectively.
    ABL127
  • HY-175510

    TREM receptor Neurological Disease
    TREM2 agonist-5 is the microglial lipid-sensing receptor (TREM2) agonist with a Kd of 71.36 μM. TREM2 agonist-5 is a racemic structural analog of the TREM2 agonist VG-3927 and exhibits superior microglial phagocytosis and activates TREM2 signaling in HEK293-hTREM2/DAP12 cells. TREM2 agonist-5 displays a superior in vitro pharmacokinetic profile to VG-3927. TREM2 agonist-5 can used for the study of Alzheimer’s disease .
    TREM2 agonist-5
  • HY-108682
    EMPA
    10+ Cited Publications

    Orexin Receptor (OX Receptor) Neurological Disease
    EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [ 3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively .
    EMPA
  • HY-131881
    JHU37160
    2 Publications Verification

    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 .
    JHU37160
  • HY-50883

    γ-secretase Neurological Disease
    BMS 299897 is a sulfonamide γ-secretase inhibitor with an IC50 of 7 nM for Aβ production inhibition in HEK293 cells stably overexpressing amyloid precursor protein (APP).
    BMS 299897
  • HY-150024

    EGFR Cancer
    BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM .
    BI-4142
  • HY-P1066

    Apelin Receptor (APJ) HIV Infection
    Apelin-17(human, bovine) is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-17(human, bovine)
  • HY-N125722

    Aabomycin A1

    ATP Synthase Antibiotic Infection
    Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
    Venturicidin A
  • HY-132934
    Ac32Az19
    1 Publications Verification

    BCRP Cancer
    Ac32Az19 is a potent, nontoxic, and highly selective BCRP inhibitor with an EC50 value of 13 nM in the BCRP-overexpressed HEK293/R2 cells.
    Ac32Az19
  • HY-134988

    FXR Phosphatase Cytochrome P450 Inflammation/Immunology
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research .
    EDP-305
  • HY-P4376A

    CaSR Neurological Disease
    Gamma-Glu-Abu TFA is the TFA salt form of Gamma-Glu-Abu (HY-P4376). Gamma-Glu-Abu TFA is an agonist for calcium sensing receptor (CaSR), that activates the CaSR with an EC50 of 0.21 μM in HEK-293 cell .
    Gamma-Glu-Abu TFA
  • HY-153460

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR7/8/9 antagonist 2 is an orally active TLR7/8/9 antagonist. TLR7/8/9 antagonist 2 has inhibitory activities for HEK/hTLR7, HEK/hTLR8 and HEK/hTLR9 with IC50 values of 0.011 μM, 0.029 μM and 0,052 μM, respectively.TLR7/8/9 antagonist 2 has high bioavailability in vivo.TLR7/8/9 antagonist 2 can be used for the research of auto-inflammatory diseases such as systemic lupus erythematosus or lupus nephritis .
    TLR7/8/9 antagonist 2
  • HY-100360
    MS049
    1 Publications Verification

    Histone Methyltransferase Cancer
    MS049, a chemical probe, is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and does not affect the growth of HEK293 cells .
    MS049
  • HY-143481

    Sodium Channel Neurological Disease Inflammation/Immunology
    Nav1.8-IN-2 (compound 35A) is a Nav1.8 voltage-gated sodium ion inhibitor with an IC50 of 0.4 nM (HEK 293 cells). Nav1.8-IN-2 inhibits the activity of Nav1.8 voltage-gated sodium ion channels, mediates sodium ion influx in excitable cells, and is associated with the initiation and conduction of action potentials. Nav1.8-IN-2 can be used for research related to pain, cough, itching, etc .
    Nav1.8-IN-2
  • HY-135783
    AT 1001
    1 Publications Verification

    nAChR Neurological Disease Metabolic Disease Inflammation/Immunology
    AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
    AT 1001
  • HY-100013C

    GPR88 Neurological Disease
    2-PCCA hydrochloride is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.
    2-PCCA hydrochloride
  • HY-102028
    KY1220
    3 Publications Verification

    Wnt β-catenin Cancer
    KY1220 is a compound that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway, with an IC50 of 2.1 μM in HEK293 reporter cells .
    KY1220
  • HY-P1064

    Apelin Receptor (APJ) HIV Infection Cardiovascular Disease Metabolic Disease
    Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-36(human)
  • HY-19774

    ROR Inflammation/Immunology
    GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
    GNE-0946
  • HY-120538

    Toll-like Receptor (TLR) Inflammation/Immunology
    CPG-52364 (compound 2) is a TLR9 antagonist. CPG-52364 inhibits the HEK293-hTLR9 cell with an IC50 value of 4.6 nM .
    CPG-52364
  • HY-19775
    GNE-6468
    1 Publications Verification

    ROR Inflammation/Immunology
    GNE-6468 is a highly potent and selective RORγ (RORc) inverse agonist with an EC50 value of 13 nM for HEK-293 cell. GNE-6468 exhibits an EC50 of 30 nM for IL-17 PBMC .
    GNE-6468
  • HY-120026
    KB130015
    1 Publications Verification

    KB015

    Thyroid Hormone Receptor Calcium Channel Potassium Channel Sodium Channel Cardiovascular Disease
    KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca 2+-activated K + (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease .
    KB130015
  • HY-161074

    FAP Cancer
    PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
    PNT6555
  • HY-120170
    BMS-466442
    1 Publications Verification

    ASCT Adrenergic Receptor Dopamine Transporter Neurological Disease
    BMS-466442 is a potent and selective inhibitor of asc-1 (alanine serine cysteine transporter-1), with an IC50 of 11 nM. BMS-466442 inhibits [ 3H] D-serine uptake into rat brain synaptosomes, with an IC50 of 400 nM. BMS-466442 can be used for schizophrenia research .
    BMS-466442
  • HY-148338

    Toll-like Receptor (TLR) Inflammation/Immunology
    TLR8 agonist 5 is a potent TLR8 agonist with an EC50 value of 20 nM for HEK-Blue hTLR8. TLR8 agonist 5 activates the immune response .
    TLR8 agonist 5
  • HY-W585876

    FXR Metabolic Disease
    Chenodeoxycholic acid 3-glucuronide is a metabolite of Chenodeoxycholic acid that can activate the key nuclear receptor (FXR), with an EC50 of 8 μM, and in HEK293T cells, the EC50 for activating FXR is 11 μM .
    Chenodeoxycholic acid 3-glucuronide
  • HY-148939

    iGluR Neurological Disease
    MPX-004 is a potent GluN2A antagonist. MPX-004 inhibits GluN2A-containing NMDA receptors expressed in HEK cells with an IC50 of 79 nM. MPX-004 has no inhibitory effect on GluN2B or GluN2D receptor-mediated responses. MPX-004 has the potential for neuropsychiatric and developmental disorders research .
    MPX-004
  • HY-139848

    P-glycoprotein Cancer
    WS-898 is a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC50 = 5.0, 3.67, and 3.68 nM, respectively).
    WS-898
  • HY-131891

    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 .
    JHU37152
  • HY-136583

    Drug Metabolite Others
    28-Epirapamycin is an impurity of Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells .
    28-Epirapamycin
  • HY-118368

    Influenza Virus Infection Inflammation/Immunology
    L-742001 hydrochloride is an influenza virus PA endonuclease inhibitor, with an EC90 of 4.3 μM for vRNP activity in HEK293T cells .
    L-742001 hydrochloride
  • HY-16934

    Cholinesterase (ChE) Neurological Disease
    ML352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively .
    ML352
  • HY-100801

    EAAT Neurological Disease
    L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor with Kis of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3, respectively in HEK293 cell lines .
    L-threo-3-Hydroxyaspartic acid
  • HY-114633
    VU625
    2 Publications Verification

    Potassium Channel Others
    VU625 is an inhibitor for potassium channel, that selectively inhibits mosquito Aedes aegypti inward rectifier potassium channel 1 (AeKir), with IC50 of 96.8 nM in HEK293 cell. VU625 can be used in development of insecticide .
    VU625
  • HY-168758

    GABA Receptor Neurological Disease
    Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC50 values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .
    Delta3,5-cholestadien-7-one
  • HY-P1064A

    HIV Apelin Receptor (APJ) Infection Cardiovascular Disease Metabolic Disease
    Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
    Apelin-36(human) TFA
  • HY-114962

    Melatonin Receptor Neurological Disease
    S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes .
    S-22153
  • HY-132866

    P-glycoprotein Cancer
    YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity .
    YS-370
  • HY-18332A

    DOV-21947 hydrochloride; EB-1010 hydrochloride

    Serotonin Transporter Dopamine Transporter Infection Neurological Disease
    Amitifadine (DOV-21947; EB-1010) hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI), with IC50s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
    Amitifadine hydrochloride
  • HY-153132

    mGluR Metabolic Disease
    mGluR3 modulator-1 (compound 3) is a mGluR3 modulator, with an EC50 of 1-10 μM in HEK293T-mGluR-Gqi5 Calcium Mobilization Assay .
    mGluR3 modulator-1

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