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Results for "

HEK 293

" in MCE Product Catalog:

97

Inhibitors & Agonists

1

Biochemical Assay Reagents

5

Peptides

7

Natural
Products

6268

Recombinant Proteins

4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-112683
    V-9302

    Others 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.
  • HY-112683A
    V-9302 hydrochloride

    Others 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.
  • HY-19774
    GNE-0946

    ROR Inflammation/Immunology
    GNE-0946 is a potent and selective RORγ( RORc) agonist with an EC50 value of 4 nM for HEK-293 cell.
  • HY-132934
    Ac32Az19

    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.
  • HY-143487
    Antimalarial agent 12

    Parasite Infection
    Antimalarial agent 12 (compound R-3b) is a potent antimalarial agent. Antimalarial agent 12 shows growth inhibition on P. falciparum Dd2 Strain (EC50=155 nM), 3D7 strain (EC50=136 nM). Antimalarial agent 12 has CC50 values of 10,000 to 50,000 nM for HEK-293 and hPHep cell lines. Antimalarial agent 12 has a MIC of >250,000 nM for Escherichia coli.
  • HY-100360
    MS049

    Histone Methyltransferase Cancer
    MS049 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.
  • HY-100360A
    MS049 dihydrochloride

    Histone Methyltransferase Cancer
    MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and does not affect the growth of HEK293 cells.
  • HY-136583
    28-Epirapamycin

    Others 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.
  • HY-109039
    Praliciguat

    IW-1973

    Guanylate Cyclase Cardiovascular Disease
    Praliciguat (IW-1973) is a potent and orally active soluble guanylate cyclase stimulator, enhances NO signaling, acts as a vasodilator. Praliciguat (IW-1973) stimulates sGC in HEK-293 cells with an EC50 of 197 nM.
  • HY-19775
    GNE-6468

    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.
  • HY-100013C
    2-PCCA hydrochloride

    Others 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.
  • HY-50883
    BMS 299897

    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).
  • HY-108682
    EMPA

    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.
  • HY-16934
    ML352

    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.
  • HY-102028
    KY1220

    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.
  • HY-125099
    PAD2-IN-2

    Protein Arginine Deiminase Cancer Infection
    PAD2-IN-2 is a potent PAD2 inhibitor. PAD2-IN-2 enters the HEK293T/PAD2 cells with an EC50 of 5.9 μM. PAD2-IN-2 inhibits histone H3 citrullination with an EC50 of 2.1 μM in HEK293/PAD2 cells. PAD2-IN-2 can be used for the research of cancer.
  • HY-15518
    LCL161

    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.
  • HY-12805
    ML171

    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.
  • HY-101560
    Linrodostat

    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.
  • HY-120006A
    (rel)-AR234960

    ERK Cardiovascular Disease
    (rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
  • HY-139848
    WS-898

    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).
  • HY-136555
    GSK717

    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.
  • HY-22024
    5-Hydroxyflavone

    Others Cancer
    5-Hydroxyflavone, a flavonoid ligand, shows no cytotoxic activity against MCF-7, FaDU, MDA-MB-435S, U87, RPE-1, and HEK293 cells.
  • HY-146071
    Antitrypanosomal agent 5

    Parasite Infection
    Antitrypanosomal agent 5 (Compound 25)is a selective anti-trypanosomal agent with IC50s of 1 nM and 483.3 µM against T. brucei cell growth and HEK293 cells growth , respectively.
  • HY-19889
    JNJ-18038683

    5-HT Receptor Neurological Disease
    JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
  • HY-19337
    ORM-15341

    Androgen Receptor Endocrinology
    ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct.
  • 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-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-103538
    JLK-6

    Amyloid-β Neurological Disease
    JLK-6 markedly reduce the production of amyloid β-peptide (Aβ) by amyloid-β Precursor protein (APP) expressing HEK293 cells by affecting the γ-secretase cleavage of APP, with no effect on the cleavage of the Notch receptor.
  • HY-10219
    Rapamycin

    Sirolimus; AY-22989

    mTOR FKBP Fungal Autophagy Endogenous Metabolite Antibiotic Cancer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-150737
    MI-1851

    SARS-CoV Infection
    MI-1851 is a potent furin inhibitor. MI-1851 prevents the proteolytic processing of the S protein of SARS-CoV-2 by endogenous flavoprotease in HEK293 cells. MI-185 has antiviral activity.
  • HY-146428
    Anti-MRSA agent 4

    Bacterial Infection
    Anti-MRSA agent 4 (compound 7a) is a potent and selective growth inhibitor of Gram-positive Methicillin-resistant Staphylococcus aureus (MRSA), with MIC ≤ 0.26 µM. Anti-MRSA agent 4 exhibits no cytotoxic and no hemolytic activity in HEK293 cells.
  • HY-103320A
    Calhex 231 hydrochloride

    CaSR Metabolic Disease
    Calhex 231 hydrochloride is a CaSR inhibitor via negative allosteric modulation. Calhex 231 hydrochloride blocks Ca 2+-induced accumulation of [ 3H]inositol phosphate with an IC50 of 0.39 μM in HEK293 cells. Calhex 231 hydrochloride has the potential for diabetic cardiomyopathy (DCM) treatment.
  • HY-150766
    KPC-2-IN-1

    Bacterial Infection
    KPC-2-IN-1, boronic acid derivative, is a potent KPC-2 inhibitor with Ki of 0.032 μM. KPC-2-IN-1 enhances the activity of cefotaxime in KPC-2 expressing E. coli. KPC-2-IN-1 exhibits well tolerated in human HEK-293 cells, which can be used for the study of E. coli resistance to β-lactam antibiotics.
  • HY-10219S
    Rapamycin-d3

    Sirolimus-d3; AY-22989-d3

    mTOR FKBP Autophagy Cancer
    Rapamycin-d3 (Sirolimus-d3) is the deuterium labeled Rapamycin. Rapamycin is a potent and specific mTOR inhibitor with an IC50of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-147917
    RNA polymerase II-IN-2

    DNA/RNA Synthesis Cancer
    RNA polymerase II-IN-2 (compound 20iii) is a potent RNA polymerase II (Pol II) inhibitor with Ki value of 9.5 nM. RNA polymerase II-IN-2 has cytotoxicity against cancer cells, and exhibits 2 and 5 fold toxicity than α-amanitin against CHO and HEK293.
  • HY-126195
    Fluoflavine

    ML-090

    NADPH Oxidase Cardiovascular Disease
    Fluoflavine (ML-090) is a selective NOX1 inhibitor with an IC50 of 90 nM. Fluoflavine has >100 selectivity for NOX1 over NOX2, NOX3, NOX4 (all IC50>10 μM). ML-090 has an IC50 of 360 nM in HEK293 cells.
  • HY-119695A
    Simvastatin acid ammonium

    Tenivastatin ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-150606
    ERK5-IN-4

    ERK Cancer
    ERK5-IN-4 (compound 34b) is a potent and selective inhibitor of extracellular signal-related kinase 5 (ERK5). ERK5-IN-4 inhibits ERK5 (full-length) and truncated ERK5 (ERK5 ΔTAD) kinase activity in HEK293 cells with an IC50 of 77 nM and 300 nM, respectively.
  • HY-145270
    ELOVL1-IN-2

    Others Metabolic Disease
    ELOVL1-IN-2 is an elongation of very long chain fatty acid 1 (ELOVL1) enzyme inhibitor, ELOVL1-IN-2 shows weak ELOVL1 inhibition (IC50=21 μM) and moderate potency in a primary cellular assay (HEK293 C26 IC50=6.7 μM) .
  • HY-18056
    PF-915275

    Others Metabolic Disease
    PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
  • HY-120348
    ML67-33

    Potassium Channel Neurological Disease Cardiovascular Disease
    ML67-33 is a selective activator of temperature- and mechano-sensitive K2P channels. ML67-33 rapidly and reversibly affects K2P2.1 (TREK-1) with EC50s of 36.3 μM and 9.7 μM in cell-free and HEK293 cells, respectively.
  • HY-13290
    KN-62

    CaMK P2X Receptor Metabolic Disease Cancer
    KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
  • HY-103118
    PU02

    5-HT Receptor Apoptosis Cancer Neurological Disease
    PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
  • HY-112705
    VU0529331

    Potassium Channel Neurological Disease
    VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel.
  • HY-101202
    SNC80

    NIH 10815

    Opioid Receptor Neurological Disease
    SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
  • HY-147552
    HIV-1 inhibitor-35

    HIV Infection
    HIV-1 inhibitor-35 (compound 74) is a potent HIV-1 inhibitor with EC50s of 80 nM and 70 nM for LTR and CMV in HEK293 cells, respectively. HIV-1 inhibitor-35 has inhibitory activity against liver cancer cell HepG2 with a CC50 of 40 nM. HIV-1 inhibitor-35 can be used as HIV-1 latency reversing agent.
  • HY-108584
    Flindokalner

    BMS-204352

    Potassium Channel Neurological Disease
    Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
  • HY-119695AS
    Simvastatin acid-d6 ammonium

    Tenivastatin-d6 ammonium

    Endogenous Metabolite Cardiovascular Disease
    Simvastatin acid-d6 (Tenivastatin-d6) ammoniumis the deuterium labeled Simvastatin acid ammonium. Simvastatin ammonium is an active metabolite of simvastatin lactone mediated by CYP3A4/5 in the intestinal wall and liver (pKa=5.5). Simvastatin ammonium reduces indoxyl sulfate-mediated reactive oxygen species and modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.
  • HY-100403
    Ro 67-7476

    mGluR Cancer
    Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM).
  • HY-134581A
    Enpatoran hydrochloride

    M5049 hydrochloride

    Toll-like Receptor (TLR) Inflammation/Immunology
    Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research.
  • HY-134581
    Enpatoran

    M5049

    Toll-like Receptor (TLR) Inflammation/Immunology
    Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
  • HY-122416
    6,8-Diprenylnaringenin

    Lonchocarpol A; Senegalensin

    BCRP Cancer Metabolic Disease
    6,8-Diprenylnaringenin (Lonchocarpol A; Senegalensin), a hop prenylflavonoid, is a inhibitor of breast cancer resistance protein (BCRP/ABCG2). 6,8-Diprenylnaringenin inhibits ABCG2-mediated efflux of Mitoxantrone, and 3H-Methotrexate transport (IC50=0.41 μM) in HEK293 cells. 6,8-Diprenylnaringenin exhibits some estrogenicity, but its potency is less than 1% of that of 8-Prenylnaringenin.
  • HY-N0930B
    Galegine hydrochloride

    AMPK Bacterial Infection Metabolic Disease
    Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains.
  • HY-12033
    2-Methoxyestradiol

    2-ME2; NSC-659853

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-107535
    AS1269574

    GPR119 TRP Channel Metabolic Disease
    AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.
  • HY-100769
    Hypidone hydrochloride

    YL0919

    5-HT Receptor Neurological Disease
    Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
  • HY-12033S2
    2-Methoxyestradiol-d5

    2-ME2-d5; NSC-659853-d5

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite
    2-Methoxyestradiol-d5 is the deuterium labeled 2-Hydroxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-19408
    Pyr10

    TRP Channel Others
    Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca 2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca 2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.
  • HY-18332A
    Amitifadine hydrochloride

    DOV-21947 hydrochloride; EB-1010 hydrochloride

    Serotonin Transporter Dopamine Transporter Neurological Disease
    Amitifadine 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.
  • HY-136190
    TRPC6-PAM-C20

    TRP Channel Neurological Disease
    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals.
  • HY-12033S1
    2-Methoxyestradiol-13C6

    2-ME2-13C6; NSC-659853-13C6

    Microtubule/Tubulin Reactive Oxygen Species Apoptosis Autophagy Endogenous Metabolite Cancer
    2-Methoxyestradiol-13C6 (2-ME2-13C6) is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
  • HY-108317
    ABL127

    Others 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.
  • HY-132866
    YS-370

    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.
  • HY-15888
    PTC-209

    Autophagy Cancer
    PTC-209 is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-100545
    BAPTA-AM

    Potassium Channel Cardiovascular Disease
    BAPTA-AM is a well-known membrane permeable Ca 2+ chelator. BAPTA-AM inhibits hERG channels, hKv1.3 and hKv1.5 channels in HEK 293 cells with IC50s of 1.3 μM, 1.45 μM and 1.23 μM, respectively.
  • HY-122716
    PTGR2-IN-1

    Others Others
    PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
  • HY-15888A
    PTC-209 hydrobromide

    Autophagy Cancer
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
  • HY-126010
    Dooku1

    Others Cardiovascular Disease
    Dooku1, an analog of Yoda1, is a selective antagonist of the endogenous Piezo1 channel. Dooku1 inhibited 2 μM Yoda1-induced Ca 2+-entry with IC50 values of 1.3 μM (in HEK 293 cells) and 1.5 μM (in HUVECs). Dooku1 inhibits Yoda1-induced relaxation of aorta.
  • HY-P1432A
    K-(D-1-Nal)-FwLL-NH2 TFA

    GHSR
    K-(D-1-Nal)-FwLL-NH2 TFA is a high affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
  • HY-10171
    NPS-2143 hydrochloride

    SB-262470A hydrochloride

    CaSR Metabolic Disease
    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
  • HY-10007
    NPS-2143

    SB-262470A

    CaSR Metabolic Disease
    NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
  • HY-101698B
    Alniditan dihydrochloride

    Alnitidan dihydrochloride

    5-HT Receptor Inflammation/Immunology Neurological Disease
    Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects.
  • HY-101698
    Alniditan

    Alnitidan

    5-HT Receptor Inflammation/Immunology Neurological Disease
    Alniditan (Alnitidan) is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects.
  • HY-P1066
    Apelin-17(human, bovine)

    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.
  • HY-13285
    Ki16425

    Debio 0719

    LPL Receptor Neurological Disease Cancer
    Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 can also inhibit LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
  • HY-P1066A
    Apelin-17(human, bovine) TFA

    HIV Infection
    Apelin-17(human, bovine) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-17(human, bovine) TFA binds to human APJ receptors expressed in HEK 293 cells (pIC50=9.02). Apelin-17(human, bovine) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
  • HY-126037
    (±)-ML 209

    ROR Inflammation/Immunology
    (±)-ML 209 (compound 4n), a diphenylpropanamide, is a retinoic acid-related orphan receptor RORγ antagonist with an IC50 of 1.1 μM. (±)-ML 209 inhibits RORγt transcriptional activity with an IC50 of 300 nM in HEK293t cells. (±)-ML 209 inhibits the transcriptional activity of RORγt, but not RORα in cells. (±)-ML 209 selectively inhibits murine Th17 cell differentiation without affecting the differentiation of naïve CD4 + T cells into other lineages, including Th1 and regulatory T cells.
  • HY-P1064
    Apelin-36(human)

    HIV Infection Metabolic Disease Cardiovascular 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.
  • HY-P1064A
    Apelin-36(human) TFA

    HIV Infection Metabolic Disease Cardiovascular 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.
  • HY-146094
    Antitumor agent-63

    Topoisomerase Cancer
    Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition.
  • HY-147971
    Anticancer agent 75

    Parasite Topoisomerase Cancer Infection
    Anticancer agent 75 is a potent anticancer agent. Anticancer agent 75 shows cytotoxicity and selectivity in cancer cell lines. Anticancer agent 75 shows cytotoxicity to normal human kidney cell lines is at least 35 times lower than that of the Doxorubicin standard. Anticancer agent 75 shows good activity of antiplasmodial.
  • HY-114962
    S-22153

    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.
  • HY-14542
    Ziprasidone

    CP-88059

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
  • HY-B0736
    Sertaconazole

    FI7056 free base

    Fungal Autophagy Apoptosis p38 MAPK Microtubule/Tubulin Cancer Infection Inflammation/Immunology
    Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
  • HY-14542B
    Ziprasidone mesylate trihydrate

    CP-88059 mesylate trihydrate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
  • HY-B0736A
    Sertaconazole nitrate

    FI7056

    Fungal Autophagy Apoptosis p38 MAPK Microtubule/Tubulin Infection
    Sertaconazole nitrate (FI7056) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole nitrate is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.
  • HY-14542C
    Ziprasidone mesylate

    CP-88059 mesylate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
  • HY-17407
    Ziprasidone hydrochloride monohydrate

    CP 88059 hydrochloride monohydrate

    5-HT Receptor Dopamine Receptor Neurological Disease
    Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
  • HY-146317
    P1788

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer Inflammation/Immunology
    P1788 is a dihydroorotate dehydrogenase (DHODH) inhibitor. P1788 induces DNA damage.
  • HY-103691
    ARN5187

    Autophagy Apoptosis Cancer
    ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis.
  • HY-N3376
    Liriodenine

    Spermatheridine; VLT045

    Apoptosis Cancer
    Liriodenine (Spermatheridine; VLT045) is an aporphine alkaloid isolated from the plant Mitrephora sirikitiae and has anti-cancer activities. Liriodenine induces cell apoptosis, activates the intrinsic pathway by induction of caspase-3 and caspase-9.
  • HY-103691A
    ARN5187 trihydrochloride

    Autophagy Apoptosis Cancer
    ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.
  • HY-146410
    AT2R antagonist 1

    Angiotensin Receptor Others
    AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2R affinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common drug-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes.
  • HY-122051
    AC1903

    TRP Channel Metabolic Disease
    AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model.
  • HY-146431
    AT1R antagonist 1

    Angiotensin Receptor Others
    AT1R antagonist 1 (compound 10) is a potent AT1R selective ligand. AT1R antagonist 1 exhibits a fair AT1R affinity, with a Ki of 8.5 nM.
  • HY-146436
    AT1R antagonist 2

    Angiotensin Receptor Others
    AT1R antagonist 2 (compound 6) is a potent AT1R selective ligand. AT1R antagonist 2 exhibits a fair AT1R affinity, with a Ki of 26 nM.