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whole blood

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51

Inhibitors & Agonists

1

Fluorescent Dye

1

Inhibitory Antibodies

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Natural
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4

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-135674

    p38 MAPK TNF Receptor Inflammation/Immunology Cancer
    SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
    SR-318
  • 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-32018
    Cot inhibitor-2
    2 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-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-113209A

    Endogenous Metabolite Metabolic Disease
    Ent-8-Iso-15(S)-prostaglandin F2α is an isomer of 8-Isoprostaglandin F2α, with a better inhibiting activity in the whole blood platelet aggregation inhibition assay .
    ent-8-Iso-15(S)-prostaglandin F2α
  • 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-120878
    CXCR2-IN-2
    1 Publications Verification

    CXCR Inflammation/Immunology
    CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM .
    CXCR2-IN-2
  • 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-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-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-134820

    MALT1 Inflammation/Immunology
    MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research .
    MLT-943
  • 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-B2158S

    Estrogen Receptor/ERR COX Cardiovascular Disease Endocrinology
    Chlorotrianisene-d9 is the deuterium labeled Chlorotrianisene. Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood[1][2][3].
    Chlorotrianisene-d9
  • HY-U00037

    PLA 725

    Phospholipase Inflammation/Immunology
    Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
    Ecopladib
  • HY-B2158

    Chlorotrianisene is a long-acting non-steroidal estrogen and an orally active estrogen receptor modulator. Chlorotrianisene exhibits antiestrogenic activity. Chlorotrianisene potently inhibits the enzyme COX-1 and inhibits platelet aggregation in whole blood .
    Chlorotrianisene
  • HY-15321S2

    MK-0663-d3; L-791456-d3

    COX
    Etoricoxib-d3 is the deuterium labeled Etoricoxib[1]. 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[2][3][4].
    Etoricoxib-d3
  • 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-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-145884

    Btk Inflammation/Immunology
    BTK-IN-8 is a potent and selective peripheral covalent BTK inhibitor (IC50=0.22 nM; Kd=0.91 nM). BTK-IN-8 has good whole blood CD69 cellular potency (IC50=0.029 µM) .
    BTK-IN-8
  • 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-113854

    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-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-14166
    MK-886
    Maximum Cited Publications
    7 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-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-15321R

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

    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-B0883
    Proflavine hemisulfate
    1 Publications Verification

    Proflavin hemisulfate; 3,6-Diaminoacridine hemisulfate

    Bacterial Potassium Channel Autophagy Infection Cancer
    Proflavine hemisulfate, an acridine dye, is a known DNA intercalating agent. Anti-microbial agent . Proflavine hemisulfate behaves as a pore blocker for Kir3.2. Proflavine hemisulfate is a potential lead compound for Kir3.2-associated neurological diseases .
    Proflavine hemisulfate
  • 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-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-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-128342

    Complement System Inflammation/Immunology
    Complement C5-IN-1 (Compound 7) is a small-molecule inhibitor of complement component 5 protein (C5). Complement C5-IN-1 interacts with C5 to prevent its cleavage by the C5 convertase and blocks zymosan-induced the membrane-attack complex (MAC) deposition in 50% human whole blood with an IC50 of 0.77 µM .
    Complement C5-IN-1
  • 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-101448

    WAY-171318

    TMI-1 is a potent inhibitor of disintegrin metalloenzyme 17 (ADAM17) and other MMPs. TMI-1 inhibits LPS-induced TNF-α secretion in human primary monocytes, and human whole blood . TMI-1 selectively induces caspase-dependent apoptosis in triple negative (TN) and ERBB2-overexpressing breast tumor cell lines .
    TMI-1
  • HY-153480

    BAX499

    Factor Xa Others
    ARC19499 is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
    ARC19499
  • HY-160067

    Others Infection
    T18.3 aptamer sodium is an anticoagulant RNA aptamer targeting FV/Va and eliminates the interaction of FV/FVa with phospholipid membranes. T18.3 aptamer sodium exhibits clinically relevant anticoagulant activity in plasma and whole blood and acts synergistically with low molecular weight heparin. The anticoagulant activity of T18.3 aptamer sodium is effectively and rapidly reversed by protamine sulfate .
    T18.3 aptamer sodium
  • HY-153480A

    BAX499 sodium

    Factor Xa Others
    ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.
    ARC19499 sodium
  • HY-102064
    SR 57227A
    1 Publications Verification

    5-HT Receptor Neurological Disease
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects .
    SR 57227A
  • 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-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-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-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-18862

    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-15425
    PF-543
    Maximum Cited Publications
    7 Publications Verification

    Sphingosine Kinase 1 Inhibitor II

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
    PF-543
  • HY-15425B

    Sphingosine Kinase 1 Inhibitor II hydrochloride

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
    PF-543 hydrochloride
  • 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-10797
    CJ-42794
    1 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-15425A
    PF-543 Citrate
    Maximum Cited Publications
    7 Publications Verification

    Sphingosine Kinase 1 Inhibitor II Citrate

    SphK LPL Receptor Apoptosis Autophagy Cardiovascular Disease Inflammation/Immunology Cancer
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
    PF-543 Citrate
  • HY-108642

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
    AMG-548
  • HY-108642B

    p38 MAPK Casein Kinase Inflammation/Immunology
    AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
    AMG-548 dihydrochloride

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