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cell-based assay

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42

Inhibitors & Agonists

1

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1

Peptides

3

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129634
    TrkA-IN-1

    		Trk Receptor Neurological Disease
    TrkA-IN-1 is a potent and selective Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 of 99 nM in a cell-based assay. TrkA-IN-1 has analgesic activity .
    TrkA-IN-1
  • HY-112476
    PRL-3 Inhibitor I

    		Phosphatase Cancer
    PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay .
    PRL-3 Inhibitor I
  • HY-112437
    PF-06737007

    		Trk Receptor Neurological Disease
    PF-06737007 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 7.7 nM, 15 nM and 3.9 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
    PF-06737007
  • HY-109042
    Relacorilant

    CORT 125134

    		 Glucocorticoid Receptor Cardiovascular Disease Endocrinology
    Relacorilant is a potent, selective and orally bioavailable glucocorticoid receptor antagonist, with a Ki of 7.2 nM in HepG2 TAT assay, and also shows Kis of 12, 81.2, 210 nM for rat, human and monkey glucocorticoid receptor in cell-based assay, respectively. Relacorilant has the potential for Cushing’s syndrome treatment.
    Relacorilant
  • HY-112436
    PF-6683324

    Trk-IN-4

    		 Trk Receptor Neurological Disease
    PF-6683324 (Trk-IN-4) is a potent pan-Trk inhibitor in cell-based assays with IC50s of 1.9 nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
    PF-6683324
  • HY-10237
    Boceprevir
    30+ Cited Publications

    EBP 520; SCH 503034

    		 HCV Protease HCV SARS-CoV Infection
    Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CL pro activity .
    Boceprevir
  • HY-161352
    NPI52

    		Others Infection
    NPI52 (Compound E1) is a foot-and-mouth disease virus 3C protease (FMDV 3Cpro) inhibitor, with IC50 values of 0.05 and 0.11 µM in FRET and cell-based assay, respectively .
    NPI52
  • HY-163520
    IDO1-IN-24

    		Indoleamine 2,3-Dioxygenase (IDO) Others
    IDO1-IN-24 (compound 2c) inhibits IDO1 production in cell-based assay with an IC50 value of 17 μM .
    IDO1-IN-24
  • HY-112434
    PF-06733804

    		Trk Receptor Neurological Disease
    PF-06733804 is a potent pan-Trk inhibitor in cell-based assays with IC50s of 8.4 nM, 6.2 nM and 2.2 nM for TrkA, TrkB and TrkC, respectively . Anti-hyperalgesic effect .
    PF-06733804
  • HY-10555
    AMG-221

    		11β-HSD Metabolic Disease
    AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC50 of 10.1 nM in cell-based assays . AMG-221 can be used for the research of type 2 diabetes .
    AMG-221
  • HY-10237S
    Boceprevir-d9

    EBP 520-d9; SCH 503034-d9

    		 Isotope-Labeled Compounds HCV Protease HCV SARS-CoV Infection
    Boceprevir-d9 is the deuterium labeled Boceprevir. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6].
    Boceprevir-d9
  • HY-110267
    DY268

    		FXR Metabolic Disease
    DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI) .
    DY268
  • HY-111538
    MAGL-IN-1

    		MAGL Cancer
    MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
    MAGL-IN-1
  • HY-10237R
    Boceprevir (Standard)

    		HCV Protease HCV SARS-CoV Infection
    Boceprevir (Standard) is the analytical standard of Boceprevir. This product is intended for research and analytical applications. Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay . Boceprevir inhibits SARS-CoV-2 3CL pro activity .
    Boceprevir (Standard)
  • HY-110134
    S07662

    		Constitutive Androstane Receptor Metabolic Disease
    S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .
    S07662
  • HY-168194
    DYR684

    		PROTACs DYRK Cancer
    DYR684 is a PROTAC of the protein kinases DYRK1A. DYR684 promotes fast, efficient, potent, and selective degradation of DYRK1A in cell-based assays. (Pink: ligand for target protein (HY-168195); Black: linker (HY-168200); Blue: ligand for E3 ligase (HY-168198)) .
    DYR684
  • HY-151193
    NNMT-IN-3

    		Others Metabolic Disease Cancer
    NNMT-IN-3 (compound 14) is a potent and selective nicotinamide N-methyltransferase NNMT inhibitor with IC50 values of 1.1 nM and 0.4 μM in cell-free and cell-based assays, respectively. NNMT-IN-3 can be used to research obesity, type 2 diabetes, alcohol-related liver disease, cancer, sarcopenia and so on .
    NNMT-IN-3
  • HY-111551
    FT113
    2 Publications Verification

    		 Fatty Acid Synthase (FASN) Cancer
    FT113 is a potent and orally active fatty acid synthase (FASN) inhibitor, with an IC50 of 213 nM for full-length recombinant human FASN enzyme. In cell-based assay, FT113 blocks FASN activity in BT474 cells (IC50, 90 nM). FT113 shows anti-proliferative activity, and exhibits anti-cancer activity both in vitro and in vivo .
    FT113
  • HY-115510
    SPR inhibitor 3

    SPRi3

    		 Others Inflammation/Immunology
    SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels .
    SPR inhibitor 3
  • HY-138696
    Zanzalintinib
    1 Publications Verification

    XL092

    		 TAM Receptor c-Met/HGFR VEGFR Cancer
    Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
    Zanzalintinib
  • HY-151813
    NNMT-IN-4

    		Others Cancer
    NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
    NNMT-IN-4
  • HY-155151
    RIPK2/3-IN-1

    		RIP kinase Inflammation/Immunology
    RIPK2/3-IN-1 is a potent dual RIPK2/3 kinases inhibitor with IC50 values of 3 nM and 117 nM, respectively. RIPK2/3-IN-1 is against RIPK2 with IC50 value 14 nM in 14-TriLAN-Gly/NOD1 THP-1 cell-based NF-κB reporter assay .
    RIPK2/3-IN-1
  • HY-50878
    Crizotinib
    Maximum Cited Publications
    66 Publications Verification

    PF-02341066

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib
  • HY-50878B
    Crizotinib acetate

    PF-02341066 acetate

    		 Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR Cancer
    Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
    Crizotinib acetate
  • HY-50878S
    Crizotinib-d5

    PF-02341066-d5

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib-d5
  • HY-163343
    Enpp-1-IN-20

    		Phosphodiesterase (PDE) STING Cancer
    Enpp-1-IN-20 (Compound 31) is an ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) inhibitor, with an IC50 of 0.09 nM. Enpp-1-IN-20 has strongest inhibitory activity in the cell-based assay, with an IC50 of 8.8 nM. Enpp-1-IN-20 has significant potency in both ENPP1 inhibition and STING pathway stimulation in vitro. Enpp-1-IN-20 can be used for the research of cancer .
    Enpp-1-IN-20
  • HY-50878A
    Crizotinib hydrochloride
    Maximum Cited Publications
    66 Publications Verification

    PF-02341066 hydrochloride

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib hydrochloride
  • HY-103608
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl

    VHL Ligand-Linker Conjugates 11; E3 ligase Ligand-Linker Conjugates 11

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is a small molecule HaloPROTAC that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    (S,R,S)-AHPC-(C3-​PEG)​2-​C6-​Cl
  • HY-50878R
    Crizotinib (Standard)

    		Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib (Standard)
  • HY-122038
    NU-8165

    		MDM-2/p53 Cancer
    NU-8165 is an inhibitor of the MDM2-p53 protein-protein interaction with anti-tumor activity. Optimization of NU-8165 was guided by MDM2 NMR titrations, which indicated key binding interaction regions. NU-8165 activated MDM2 and p21 transcription in cell-based assays and showed modest selectivity for wild-type p53 cell lines .
    NU-8165
  • HY-W806047
    BRD4 Inhibitor-37

    		Others Cancer
    BRD4 Inhibitor-37 is a compound with anticancer activity that has inhibitory activity against BRD4. BRD4 Inhibitor-37 has an IC50 of approximately 0.05-0.1 μM in binding assays and shows a GI50 of 0.1-0.3 μM in cell-based assays. The effect of BRD4 Inhibitor-37 on c-Myc, a downstream protein of BRD4, has been validated, demonstrating its ability to intervene in this signaling pathway. BRD4 Inhibitor-37 exhibits selectivity among five different bromodomain proteins, enhancing its potential as a BET protein inhibitor .
    BRD4 Inhibitor-37
  • HY-124305
    ML395

    		Endogenous Metabolite Infection
    ML395 is a potent and selective allosteric inhibitor of phospholipase D2 with antiviral activity. The cellular PLD1 IC50 value of ML395 exceeds 30,000 nM, while its cellular PLD2 IC50 value is 360 nM. ML395 shows excellent pharmacokinetic characteristics in vitro and physiochemical properties superior to other reported phospholipase inhibitors. ML395 shows interesting antiviral activity in cell-based assays against multiple influenza virus strains (H1, H3, H5, and H7) .
    ML395
  • HY-117427
    D5D-IN-326

    		Others Metabolic Disease
    D5D-IN-326 is a selective, orally active delta-5 desaturase (D5D) inhibitor, with IC50s of 72 and 22 nM for rat and human D5D in enzymic and cell-based assays, respectively, has no effect on D6D or D9D activity. D5D-IN-326 reduces insulin resistance and decreases body weight in diet-induced obese C57BL/6J mice .
    D5D-IN-326
  • HY-50878AS
    Crizotinib-d9 hydrochloride

    PF-02341066-d9 hydrochloride

    		 c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds Cancer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib-d9 hydrochloride
  • HY-103606
    (S,R,S)-AHPC-PEG6-C4-Cl

    VH032-PEG6-C4-Cl; VHL Ligand-Linker Conjugates 10; E3 ligase Ligand-Linker Conjugates 9

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-PEG6-C4-Cl is a conjugate of ligands for E3 and 25-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG6-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and 6-unit PEG linker. (S,R,S)-AHPC-PEG6-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    (S,R,S)-AHPC-PEG6-C4-Cl
  • HY-112495
    VH032-PEG5-C6-Cl
    1 Publications Verification

    HaloPROTAC 2

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate of ligands for E3 and 21-atom-length linker. The connector of linker is Halogen group. VH032-PEG5-C6-Cl incorporates the VH032 based VHL ligand and 5-unit PEG linker. VH032-PEG5-C6-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    VH032-PEG5-C6-Cl
  • HY-133031A
    CSV0C018875 hydrochloride

    		Histone Methyltransferase Others
    CSV0C018875 hydrochloride is a G9a (EHMT2) inhibitor that inhibits G9a activity. CSV0C018875 can effectively inhibit G9a activity in both enzyme and cell-based assays, and its toxicity is much lower than that of the known G9a inhibitor BIX-01294. CSV0C018875 binds tightly to the active site cavity of G9a, thereby improving the binding firmness and prolonging the residence time of the compound, further enhancing the inhibitory effect of G9a. CSV0C018875 has the potential to improve its ADME (absorption, distribution, metabolism and excretion) and pharmacodynamic properties through further optimization .
    CSV0C018875 hydrochloride
  • HY-103607
    (S,R,S)-AHPC-PEG2-C4-Cl
    1 Publications Verification

    VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    (S,R,S)-AHPC-PEG2-C4-Cl
  • HY-P5372
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2

    		Protease Activated Receptor (PAR) Others
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2 is a biological active peptide. (Protease activated receptor 1 (PAR-1) belongs to a subfamily of G-protein coupled receptors and is known to mediate the cellular effects of thrombin. This peptide is a PAR-1 selective agonist displaying a high level of specificity to PAR-1 over PAR-2. The specificity of peptide was evaluated in cell-based calcium signaling assay using HEK293 cells. PAR-1 selective agonists can be used to study PAR-1 activation in vivo. In addition to its varied cellular effects of thrombin, PAR-1 has also been shown to coordinate with PAR-4 and regulate thrombin-induced hepatocellular carcinoma harboring thrombin formation within the tumor environment classified as 'coagulation type'.)
    Ala-parafluoroPhe-Arg-Cha-Cit-Tyr-NH2
  • HY-103605
    (S,R,S)-AHPC-C6-PEG3-C4-Cl
    1 Publications Verification

    VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8

    		 E3 Ligase Ligand-Linker Conjugates Cancer
    (S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
    (S,R,S)-AHPC-C6-PEG3-C4-Cl
  • HY-105253
    PARP-2/1-IN-2

    		PARP Neurological Disease
    PARP-2/1-IN-2 (Compound 4a), the enantiomer of Veliparib (HY-10129), is a potent PARP inhibitor with Kis of 2 and 5 nM against PARP-2 and PARP-1, respectively. PARP-2/1-IN-2 has an EC50 of 3 nM in a cell based assay of PARP activity .
    PARP-2/1-IN-2
  • HY-139504
    Gamcemetinib

    CC-99677

    		 MAPKAPK2 (MK2) Inflammation/Immunology
    Gamcemetinib (CC-99677) is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). Gamcemetinib is extracted from patent WO2020236636, compound 1 .
    Gamcemetinib

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