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Direct Inhibitors

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278

Inhibitors & Agonists

5

Screening Libraries

4

Fluorescent Dyes

3

Biochemical Assay Reagents

12

Peptides

13

Inhibitory Antibodies

30

Natural
Products

23

Isotope-Labeled Compounds

2

Click Chemistry

2

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-164789

    SKB264; MK-2870

    Antibody-Drug Conjugates (ADCs) TROP2 Cancer
    Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2 EC50 of 2.787 ng/ml, TROP2 Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer .
    Sacituzumab tirumotecan
  • HY-B0375
    Argatroban
    5 Publications Verification

    MD-805; MCI-9038

    Thrombin Cardiovascular Disease Cancer
    Argatroban (MD-805) is a direct, selective thrombin inhibitor.
    Argatroban
  • HY-10274
    Dabigatran etexilate
    4 Publications Verification

    BIBR 1048

    Thrombin Cardiovascular Disease
    Dabigatran etexilate (BIBR 1048) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
    Dabigatran etexilate
  • HY-50903
    Rivaroxaban
    15+ Cited Publications

    BAY 59-7939

    Factor Xa Cardiovascular Disease Cancer
    Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM) .
    Rivaroxaban
  • HY-10163
    Dabigatran
    5+ Cited Publications

    BIBR 953; BIBR 953ZW

    Thrombin Cardiovascular Disease Cancer
    Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
    Dabigatran
  • HY-102084
    LMT-28
    10+ Cited Publications

    Interleukin Related Inflammation/Immunology
    LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130 .
    LMT-28
  • HY-11005
    BX-912
    5+ Cited Publications

    PDK-1 Apoptosis Cancer
    BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis .
    BX-912
  • HY-103334
    MAFP
    5 Publications Verification

    Methyl Arachidonyl Fluorophosphonate

    Phospholipase Cardiovascular Disease Neurological Disease Metabolic Disease
    MAFP (Methyl Arachidonyl Fluorophosphonate) is an selective, active-site directed and irreversible inhibitor of cPLA2 and iPLA2. MAFP is also a potent irreversible inhibitor of anandamide amidase.
    MAFP
  • HY-103666
    CY-09
    Maximum Cited Publications
    50 Publications Verification

    NOD-like Receptor (NLR) Inflammation/Immunology
    CY-09 is a selective and direct NLRP3 inhibitor. CY-09 directly binds to the ATP-binding motif of NLRP3 NACHT domain and inhibits NLRP3 ATPase activity, resulting in the suppression of NLRP3 inflammasome assembly and activation .
    CY-09
  • HY-B1099
    Hycanthone
    2 Publications Verification

    DNA/RNA Synthesis Topoisomerase Parasite Infection
    Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent .
    Hycanthone
  • HY-15724
    Vercirnon
    3 Publications Verification

    GSK-1605786; CCX282-B; Traficet-EN

    CCR Ligands for Target Protein for PROTAC Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
    Vercirnon
  • HY-D0939
    Direct Blue 1
    2 Publications Verification

    Chicago Sky Blue 6B

    Amyloid-β NF-κB Inflammation/Immunology
    Direct Blue 1 (Chicago Sky Blue 6B) is a complex dye for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1 is a potent and competitive VGLUT inhibitor. Direct Blue 1 can inhibit the Aβ-binding small molecule PrP ligand. Direct Blue 1 has anti-inflammatory activity .
    Direct Blue 1
  • HY-171689

    AZD 8205; P-Sam

    Antibody-Drug Conjugates (ADCs) Topoisomerase Cancer
    Puxitatug samrotecan (AZD 8205) is a B7-H4-directed antibody-drug conjugate (ADC) bearing a Topoisomerase I inhibitor (TOP1i) payload. Puxitatug samrotecan improves HR +/HER2 - breast cancer .
    Puxitatug samrotecan
  • HY-119711

    MMP Cancer
    NNGH is a stromelysin-1 (MMP-3) inhibitor. MMP-3 is both a direct transcriptional target and a necessary contributor of the Wnt/β-catenin signaling pathway. Matrix metalloproteinases (MMPs) play a well-defined role in later stages of tumor progression .
    NNGH
  • HY-N6961
    Lapachol
    3 Publications Verification

    Dihydroorotate Dehydrogenase DNA/RNA Synthesis Parasite Infection Inflammation/Immunology Cancer
    Lapachol, a natural naphthoquinone, is an orally active, potent DHODH inhibitor. Lapachol has immunosuppressive activity on lymphocytes through its direct ability to block DHODH activity and inhibit pyrimidine synthesis. Lapachol is a vitamin K antagonist with antitumor activity and can inhibit DNA and RNA synthesis in neoplastic cells. Lapachol has anti-Leishmania activity .
    Lapachol
  • HY-B0375A
    Argatroban monohydrate
    5 Publications Verification

    MD-805 monohydrate; MCI-9038 monohydrate

    Thrombin Cardiovascular Disease Infection Cancer
    Argatroban (monohydrate) (MD-805 (monohydrate)) is a direct, selective thrombin inhibitor.
    Argatroban monohydrate
  • HY-10274A
    Dabigatran etexilate mesylate
    4 Publications Verification

    BIBR 1048MS; Dabigatran etexilate methanesulfonate

    Thrombin Cardiovascular Disease
    Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active proagent of Dabigatran (a direct inhibitor of thrombin). Dabigatran etexilate mesylate has anticoagulant effects and is used for the prophylaxis of venousthromboembolism and stroke due to atrial fibrillation .
    Dabigatran etexilate mesylate
  • HY-50903S
    Rivaroxaban-d4
    1 Publications Verification

    BAY 59-7939-d4

    Factor Xa Cardiovascular Disease
    Rivaroxaban-d4 (BAY 59-7939-d4) is a deuterium labeled Rivaroxaban. Rivaroxaban is a highly potent,selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM) .
    Rivaroxaban-d4
  • HY-103643

    (-)-Fumagillol

    Bacterial Infection
    Fumagillol is a direct precursor of fumagillin. Fumagillin, as an antimicrobial agent, is a potent and selective inhibitor of angiogenesis .
    Fumagillol
  • HY-167851

    CXCR Neurological Disease Cancer
    CCX662 is a selective CXCR7 inhibitor with human IC50 values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC50 of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4 +/CXCR7 + cells. CCX662 can be used for the research of glioblastoma multiforme .
    CCX662
  • HY-U00422
    K-756
    2 Publications Verification

    PARP Cancer
    K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
    K-756
  • HY-125989
    2-Methylthio-AMP
    1 Publications Verification

    2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate

    P2Y Receptor Cardiovascular Disease
    2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation .
    2-Methylthio-AMP
  • HY-126302
    DMT1 blocker 2
    3 Publications Verification

    Ferroportin Metabolic Disease
    DMT1 blocker 2 is a direct inhibitor of divalent metal transporter 1 (DMT1), with an IC50 of 0.83 μM. DMT1 blocker 2 can block iron uptake by enterocytes in vivo .
    DMT1 blocker 2
  • HY-151931

    Jasmonyl-ACC

    Phytohormone Metabolic Disease
    JA-ACC (Jasmonyl-ACC) is a derivative of 1-aminocyclopropane-1-carboxylic acid (ACC). ACC is the direct precursor of the plant hormone ethylene. JA-ACC inhibits root growth in Arabidopsis and the inhibition is independent of jasmonic acid (JA) signaling .
    JA-ACC
  • HY-19628

    RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM .
    OD36
  • HY-141487
    CLP-3094
    2 Publications Verification

    Androgen Receptor Metabolic Disease Inflammation/Immunology
    CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM) . CLP-3094 is a selective, potent GPR142 antagonist .
    CLP-3094
  • HY-112373

    Aurora Kinase Others
    Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
    Aurora kinase inhibitor-3
  • HY-156395

    E1/E2/E3 Enzyme Cancer
    MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .
    MN551
  • HY-136450

    TCBZ-SO

    Parasite BCRP Infection Cancer
    Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer .
    Triclabendazole sulfoxide
  • HY-103180

    2-Chloro-N-cyclopentyl-2′-C-methyladenosine

    Adenosine Receptor Neurological Disease
    2'-MeCCPA is a potent and selective A1 adenosine receptors (A1AR) agonist. 2'-MeCCPA efficiently inhibits cAMP modulation in both direct pathway medium spiny neurons (dMSNs) and indirect pathway medium spiny neurons (iMSNs) .
    2'-MeCCPA
  • HY-P10108

    Hxk2VBD peptide, cell-permeable

    Hexokinase Neurological Disease
    Hexokinase II VDAC binding domain peptide (Hxk2VBD peptide) is a cell-permeable hexokinase II VDAC binding domain. Hexokinase II VDAC binding domain peptide inhibits mitochondrial localization of hexokinase 2 (HXK2). Hexokinase II VDAC binding domain peptide inhibits neurotrophic factor-directed axon outgrowth .
    Hexokinase II VDAC binding domain peptide, cell-permeable
  • HY-10515

    PDK-1 Cancer
    BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect .
    BX-320
  • HY-10217

    Thrombin Cardiovascular Disease
    Thrombin Inhibitor 2 is a small molecule direct thrombin inhibitor, extracted from US8541580B2. Thrombin Inhibitor 2 has antithrombotic activity .
    Thrombin Inhibitor 2
  • HY-102076

    Adrenergic Receptor Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP .
    0990CL
  • HY-W015664

    Fungal Infection
    2-Methylheptanoic acid is a naturally occurring branched-chain medium-chain fatty acid with fumigant activity against Aspergillus flavus. 2-Methylheptanoic acid inhibits the growth of Aspergillus flavus and kills its spores via two modes of action, namely fumigation and direct contact, with its fumigant activity being stronger than its direct contact activity. 2-Methylheptanoic acid can be used in studies related to Aspergillus flavus infection .
    2-Methylheptanoic acid
  • HY-76948
    5-R-Rivaroxaban
    1 Publications Verification

    Factor Xa Cardiovascular Disease
    5-R-Rivaroxaban is (R)-enantiomer of Rivaroxaban. Rivaroxaban (BAY 59-7939) is a highly potent and selective, direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM).
    5-R-Rivaroxaban
  • HY-10163S

    BIBR 953-d4; BIBR 953ZW-d4

    Isotope-Labeled Compounds Thrombin Cardiovascular Disease
    Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
    Dabigatran-d4
  • HY-15724A
    Vercirnon sodium
    3 Publications Verification

    GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium

    CCR Inflammation/Immunology Endocrinology
    Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively .
    Vercirnon sodium
  • HY-50903R

    BAY 59-7939 (Standard)

    Reference Standards Factor Xa Cardiovascular Disease Cancer
    Rivaroxaban (Standard) is the analytical standard of Rivaroxaban. This product is intended for research and analytical applications. Rivaroxaban (BAY 59-7939) is a highly potent, selective and direct Factor Xa (FXa) inhibitor, achieving a strong gain in anti-FXa potency (IC50 0.7 nM; Ki 0.4 nM) .
    Rivaroxaban (Standard)
  • HY-110019

    Lu 19-005

    Serotonin Transporter Dopamine Transporter Neurological Disease
    Indatraline hydrochloride (Lu 19-005) is a non-selective monoamine transporter inhibitor that blocks the reuptake of neurotransmitters (dopamine, serotonin, and norepinephrine). Indatraline hydrochloride can be used for the research of antidepressive. Indatraline hydrochloride induces autophagy while simultaneously inhibiting cell proliferation. Indatraline hydrochloride may also serve to direct the development of new agents for autophagy-related diseases such as atherosclerosis or restenosis .
    Indatraline hydrochloride
  • HY-18660

    PER977

    Factor Xa Thrombin Cardiovascular Disease
    Ciraparantag (PER977) is a thrombin and factor Xa inhibitor. Ciraparantag is a broad-spectrum reversal agent for anticoagulants, including low-molecular-weight heparin, unfractionated heparin, and certain direct oral anticoagulants. It is reported to antagonize the effects of all coagulants except VKAs and agratroban .
    Ciraparantag
  • HY-108739

    BI 655075

    Thrombin Cardiovascular Disease
    Idarucizumab is a humanized monoclonal antibody fragment. Idarucizumab is first reversal agent for a direct oral anticoagulant (DOAC). Idarucizumab can specifically neutralize the effects of the oral direct thrombin inhibitor in order to restore hemostasis .
    Idarucizumab
  • HY-D1270

    SARS-CoV Infection
    Direct Violet 1, an azo dye, is a textile dye. Direct Violet 1 is also the protein-protein interaction (PPI) between the SARS-CoV-2 spike protein and ACE2 inhibitor with IC50s of 1.47-2.63 μM .
    Direct Violet 1
  • HY-114511

    Factor VIIa Cardiovascular Disease
    BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
    BMS-593214
  • HY-153493A

    Small Interfering RNA (siRNA) Metabolic Disease
    PF-04523655 sodium is a siRNA directed against RTP801 gene. RTP801 sodium is an inhibitor of the mammalian target of rampamycin complex 1 (mTORC1) and downstream transcription factor HIF-1.
    PF-04523655 sodium
  • HY-139031

    Aldehyde Dehydrogenase (ALDH) Endocrinology
    ALDH1A2-IN-1 is an active site-directed reversible ALDH1A2 inhibitor (IC50=0.91 μM; Kd=0.26 μM) with several hydrophobic interactions .
    ALDH1A2-IN-1
  • HY-10163S1

    BIBR 953-d3; BIBR 953ZW-d3

    Thrombin Cardiovascular Disease
    Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
    Dabigatran-d3
  • HY-10163R

    BIBR 953 (Standard); BIBR 953ZW (Standard)

    Reference Standards Thrombin Cardiovascular Disease Cancer
    Dabigatran (Standard) is the analytical standard of Dabigatran. This product is intended for research and analytical applications. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
    Dabigatran (Standard)
  • HY-129944

    Phospholipase Inflammation/Immunology
    MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
    MJ33-OH
  • HY-19628A

    RIP kinase TGF-β Receptor Inflammation/Immunology
    OD36hydrochloride is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 hydrochloride is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 hydrochloride shows ALK2-directed activity with KDs of 37 nM .
    OD36 hydrochloride

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