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human whole blood

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56

Inhibitors & Agonists

1

Natural
Products

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-137892

    Epigenetic Reader Domain Inflammation/Immunology
    GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood .
    GSK620
  • HY-153440

    JAK Cancer
    JAK-IN-25 (compound 19) is a potent JAK inhibitor with IC50s of 6 nM, 21 nM, 8 nM, 1051 nM for TYK2, JAK1, JAK2, JAK3, respectively. JAK-IN-25 inhibits human whole blood IL-12 (HEB IL-12) with an IC50 of 28 nM. JAK-IN-25 has the potential for cancer research .
    JAK-IN-25
  • HY-13344A
    PF-8380 hydrochloride
    5 Publications Verification

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380 hydrochloride
  • HY-13344
    PF-8380
    5 Publications Verification

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380
  • HY-107275

    Cholinesterase (ChE) Neurological Disease
    Ebeiedinone, a steroidal alkaloid from Fritillaria species, inhibits the bioactivity of human whole blood cholinesterase (ChE) at the concentration of 0.1 mM, with the inhibitory effects of 69.0% .
    Ebeiedinone
  • HY-153673

    IRAK PROTACs Cancer
    PROTAC IRAK4 degrader-8 (Compound 2) is a PROTAC IRAK4 degrader (IC50: 15.5 nM). PROTAC IRAK4 degrader-8 degrades IRAK4 in THP-1 cells (DC50: 1.8 nM)。PROTAC IRAK4 degrader-8 also inhibits L-6 production in human whole blood and LPS-induced human PBMC cells, with IC50s of 246 nM and 2.2 nM respectively .
    PROTAC IRAK4 degrader-8
  • HY-U00170

    U66858

    Leukotriene Receptor Prostaglandin Receptor Lipoxygenase Inflammation/Immunology Endocrinology
    Bunaprolast (U66858) is a potent inhibitor of LTB4 production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB2 release.
    Bunaprolast
  • HY-172195

    p38 MAPK Inflammation/Immunology
    FS-694 is the inhibitor for p38α with an IC50 of 0.2 nM. FS-694 inhibits the TNFα release in human whole blood with an IC50 of 35.0 nM .
    FS-694
  • HY-10437A

    MK-0633 tosylate

    Lipoxygenase Inflammation/Immunology
    Setileuton tosylate is an inhibitor for 5-lipoxygenase, that inhibits the oxidation of arachidonic acid by recombinant human 5-LO, and the production of LTB4 in calcium ionophore-stimulated human whole blood, with IC50 of 3.9 and 52 nM, respectively .
    Setileuton tosylate
  • HY-162457

    DNA/RNA Synthesis Infection
    Mn007 is a potent inhibitor of bovine pancreatic DNase I, with the IC50 of 45 μM, by forming molecular aggregation. Mn007 shows suppression of S. pyogenes growth in human whole blood .
    Mn007
  • HY-169908

    STAT Cancer
    STAT3-IN-37 (Compound 101) is the inhibitor for STAT3 with an IC50 of 15 nM (measuring by DNA-HTRF assay) or 2 nM (measuring by human whole blood SOCS3 qPCR assay) .
    STAT3-IN-37
  • HY-10437

    MK-0633

    Lipoxygenase Inflammation/Immunology
    Setileuton (MK-0633) is an inhibitor for 5-lipoxygenase, that inhibits the oxidation of arachidonic acid by recombinant human 5-LO, and the production of LTB4 in calcium ionophore-stimulated human whole blood, with IC50 of 3.9 and 52 nM, respectively .
    Setileuton
  • HY-106093

    COX Inflammation/Immunology
    Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood .
    Eltenac
  • HY-18725

    P2X Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    P2X7-IN-2 (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 can be used for the research of autoimmunity, inflammation and cardiovascular disease .
    P2X7-IN-2
  • HY-18725A

    P2X Receptor Interleukin Related Cardiovascular Disease Inflammation/Immunology
    P2X7-IN-2 TFA (compound 58) is a P2X7 receptor inhibitor. P2X7-IN-2 TFA inhibits IL-Iβ release with an IC50 value of 0.01 nM. P2X7-IN-2 TFA can be used for the research of autoimmunity, inflammation and cardiovascular disease .
    P2X7-IN-2 TFA
  • HY-132248

    Lenalidomide 5'-amine

    TNF Receptor Inflammation/Immunology
    C5 Lenalidomide (Lenalidomide 5'-amine) (Compound 8a) is a thalidomide analog and is a potent inhibitor of TNF-α production (IC50 = 100 μM in LPS stimulated human PBMC and IC50 = 480 nM in whole blood) .
    C5 Lenalidomide
  • HY-13344AR

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    PF-8380 (hydrochloride) (Standard) is the analytical standard of PF-8380 (hydrochloride). This product is intended for research and analytical applications. PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380 hydrochloride (Standard)
  • HY-13344R

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    PF-8380 (Standard) is the analytical standard of PF-8380. This product is intended for research and analytical applications. PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
    PF-8380 (Standard)
  • HY-120606

    Lipoxygenase Inflammation/Immunology
    A-78773 is a 5-lipoxygenase inhibitor. A-78773 can inhibit the formation of LTB4 in human whole blood and human neutrophils, with IC50 values of 85 nM and 20 nM, respectively. A-78773 can be used in the study of inflammation-related diseases .
    A-78773
  • HY-151894

    Epigenetic Reader Domain Cancer
    I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases .
    I-BET432
  • HY-156961

    GLPG3667

    JAK Inflammation/Immunology
    Cadefrecitinib (GLPG3667) is a reversible, ATP-competitive and orally active TYK2 inhibitor with an IC50 of 2.3 nM. Cadefrecitinib inhibits IFNα/pSTAT1, and the IC50 values ​​in human peripheral blood mononuclear cell (PBMC) and whole blood assays are 70 nM and 623 nM, respectively. Cadefrecitinib has the potential for the study of inflammatory and autoimmune diseases .
    Cadefrecitinib
  • HY-113854
    AZD2906
    1 Publications Verification

    Glucocorticoid Receptor Cardiovascular Disease Endocrinology
    AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
    AZD2906
  • HY-15321

    MK-0663; L-791456

    COX Inflammation/Immunology Cancer
    Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib
  • HY-32015
    Cot inhibitor-1
    2 Publications Verification

    MAP3K Inflammation/Immunology
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM .
    Cot inhibitor-1
  • HY-12159A

    Integrin Inflammation/Immunology
    MK-0668 mesylate is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 mesylate exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
    MK-0668 mesylate
  • HY-12159

    Integrin Inflammation/Immunology
    MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
    MK-0668
  • HY-15321S
    Etoricoxib-d4
    1 Publications Verification

    MK-0663-d4; L-791456-d4

    COX Others
    Etoricoxib-d4 is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib-d4
  • HY-153254

    Toll-like Receptor (TLR) Inflammation/Immunology
    BMS905 is an orally active TLR7 and TLR8 dual inhibitor (IC50s: 0.7 and 3.2 nM respectively). BMS905 inhibits TLR7 or TLR8 induced IL-6 production in human/mouse whole blood. BMS905 can be used for research of lupus .
    BMS905
  • HY-W419570

    P2Y Receptor Cardiovascular Disease
    (Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
    (Rac)-BX 048
  • HY-170364

    NOD-like Receptor (NLR) Pyroptosis Inflammation/Immunology
    NLRP3-IN-60 (Compound 39) is the orally active inhibitor for NLRP3. NLRP3-IN-60 inhibits pyroptosis with an IC50 of 13 nM in THP-1 cell. NLRP3-IN-60 inhibits IL-1β release with an IC50 of 225 nM in human whole blood .
    NLRP3-IN-60
  • HY-14166
    MK-886
    Maximum Cited Publications
    9 Publications Verification

    L 663536

    FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
    MK-886
  • HY-14166A

    L 663536 sodium salt

    PPAR Apoptosis Leukotriene Receptor FLAP Cancer
    MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis .
    MK-886 sodium salt
  • HY-32018
    Cot inhibitor-2
    4 Publications Verification

    MAP3K Cancer
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM .
    Cot inhibitor-2
  • HY-150508

    CD38 Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    MK-0159 is an orally active, potent and selective CD38 inhibitor, with IC50 values of 22, 3, and 70 nM for human, mouse and rat CD38, respectively. MK-0159 also shows good microsomal stability for human and rodent liver microsomes. MK-0159 increases NAD + (nicotinamide adenine dinucleotide) and reduces ADPR (adenosine diphosphate ribose) in whole blood and heart .
    MK-0159
  • HY-100864

    PGE synthase Inflammation/Immunology
    mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM) .
    mPGES1-IN-3
  • HY-15321S2

    MK-0663-d3; L-791456-d3

    COX Inflammation/Immunology
    Etoricoxib-d3 is the deuterium labeled Etoricoxib . Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood .
    Etoricoxib-d3
  • HY-15321R

    MK-0663 (Standard); L-791456 (Standard)

    Reference Standards COX Inflammation/Immunology Cancer
    Etoricoxib (Standard) is the analytical standard of Etoricoxib. This product is intended for research and analytical applications. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib (Standard)
  • HY-14165A

    (S)-BAY X 1005; (S)-DG-031

    Leukotriene Receptor FLAP Inflammation/Immunology
    (S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood .
    (S)-Veliflapon
  • HY-15321S1

    MK-0663-13C,d3; L-791456-13C,d3

    Isotope-Labeled Compounds COX Inflammation/Immunology Cancer
    Etoricoxib- 13C,d3 is the 13C- and deuterium labeled Etoricoxib. Etoricoxib (MK-0663) is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood.
    Etoricoxib-13C,d3
  • HY-10797
    CJ-42794
    2 Publications Verification

    CJ-042794

    Prostaglandin Receptor Inflammation/Immunology Endocrinology
    CJ-42794 (CJ-042794) is a potent, orally active, selective prostaglandin E receptor 4 (EP4) antagonist with an IC50 value of 10 nM, which is 200-fold more selective than EP1, EP2 and EP3. CJ-42794 can be used in research of gastric ulcers .
    CJ-42794
  • HY-136527

    ROR Interleukin Related Inflammation/Immunology
    BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis) .
    BMS-986251
  • HY-12995A

    FLAP Inflammation/Immunology
    (S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production .
    (S)-BI 665915
  • HY-156409

    JAK Inflammation/Immunology
    ABBV-712 is a selective and orally active inhibitor of Tyrosine kinase 2 (TYK2). ABBV-712 has EC50 values of 0.01, 0.19, and 0.17 μM for TYK2 JH2, TYK2 cells and human whole blood, respectively. ABBV-712 has anti-inflammatory activity and can be used in the research of autoimmune diseases .
    ABBV-712
  • HY-19443

    Histamine Receptor Lipoxygenase Inflammation/Immunology
    UCB-35440 is an orally active histamine H1 receptor antagonist and 5-lipoxygenase inhibitor. UCB-35440 inhibits LTB4 formation in human whole blood and reduces polymorphonuclear cell infiltration in mouse models. UCB-35440 inhibits histamine-stimulated bronchoconstriction and reduces skin inflammation in guinea pigs. UCB-35440 can be used for research on asthma and skin inflammation .
    UCB-35440
  • HY-150720

    JAK IFNAR Inflammation/Immunology
    TYK2-IN-12 (compound 30) is an orally active, potent and selective TYK2 (tyrosine kinase 2) inhibitor, with a Ki of 0.51 nM. TYK2-IN-12 inhibits IL-12 induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. TYK2-IN-12 can be used for psoriasis research .
    TYK2-IN-12
  • HY-14166R

    FLAP Leukotriene Receptor PPAR Apoptosis Cancer
    MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
    MK-886 (Standard)
  • HY-18862

    p38 MAPK Inflammation/Immunology
    PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
    PF-03715455
  • HY-173154

    Molecular Glues NEKs Inflammation/Immunology
    NK7-902 is a CRBN molecular glue degrader of NEK7. NK7-902 fully degrades NEK7 in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 leads to profound and long-lasting NEK7 degradation but only transiently blocks NLRP3 inflammasome activation in non-human primates by oral administration. NK7-902 shows activity in murine systems .
    NK7-902
  • HY-125975

    Lipoxygenase Inflammation/Immunology
    1-Naphthyl 3,5-dinitrobenzoate is a potent 5-lipoxygenase inhibitor with IC50 values of 1.04 µM and 3.6 µM for 5-LOX and mPGES-1, respectively. 1-Naphthyl 3,5-dinitrobenzoate has strong inhibition activity in the human whole blood (HWB) assay with an IC50 value of 8.6 μM. 1-Naphthyl 3,5-dinitrobenzoate can be used in research of inflammation .
    1-Naphthyl 3,5-dinitrobenzoate
  • HY-122144

    Teroxirone

    Endogenous Metabolite Cancer
    α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in rat liver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
    α-Triglycidyl isocyanurate

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