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Pharmacological Inhibitors

" in MedChemExpress (MCE) Product Catalog:

49

Inhibitors & Agonists

3

Screening Libraries

1

Biochemical Assay Reagents

3

Peptides

13

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-B0103A
    Fluvoxamine maleate
    5+ Cited Publications

    DU-23000 maleate

    Serotonin Transporter Neurological Disease Cancer
    Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
    Fluvoxamine maleate
  • HY-B0103
    Fluvoxamine
    5+ Cited Publications

    DU-23000

    Serotonin Transporter Neurological Disease
    Fluvoxamine (DU-23000) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
    Fluvoxamine
  • HY-107622

    Others Metabolic Disease
    (E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
    (E/Z)-BIX02188
  • HY-B0103AS1

    DU-23000-d4 (maleate)

    Serotonin Transporter Neurological Disease
    Fluvoxamine-d4 (maleate) is the deuterium labeled Fluvoxamine maleate. Fluvoxamine maleate (DU-23000 maleate) is an antidepressant which functions pharmacologically as a selective serotonin reuptake inhibitor.
    Fluvoxamine-d4 maleate
  • HY-106456

    GP 31406

    Cholinesterase (ChE) Neurological Disease
    Depramine (GP 31406) is a tricyclic antidepressant with pharmacologically activity. Depramine inhibits acetylcholinesteraseMg 2+-ATPase,and Na+/K+ ATPase activity .
    Depramine
  • HY-105917
    Emidurdar
    2 Publications Verification

    Endovion; NS3728

    Chloride Channel Others
    Endovion is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor .
    Emidurdar
  • HY-Y1891
    Tween 80
    40+ Cited Publications

    Polysorbate 80

    Biochemical Assay Reagents Others
    Tween 80 (Polysorbate 80), a surfactant, has been widely used as a solvent for pharmacological experiments. Tween 80 can also reduce bacterial attachment and inhibit biofilm formation.
    Tween 80
  • HY-N6054

    Parasite Topoisomerase Infection Inflammation/Immunology
    Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
    Niranthin
  • HY-N1422

    Hecogenin is a steroid saponin isolated from Agave sisalana and is a selective inhibitor of human UDP-glucuronosyltransferases. Hecogenin has a wide spectrum of pharmacological activities, including anti-inflammatory, antifungal and gastroprotective effects .
    Hecogenin
  • HY-P0142

    Guanylate Cyclase Inflammation/Immunology
    DT-3 is a membrane-permeable protein kinase G Iα inhibitory peptide. DT-3 is a guanylyl cyclase? inhibitor and shows pharmacological blockade of the cGMP–PKG signalling .
    DT-3
  • HY-N2575
    Hypocrellin A
    1 Publications Verification

    PKC Bacterial Parasite Infection Cancer
    Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT) .
    Hypocrellin A
  • HY-13633
    Exisulind
    1 Publications Verification

    Aldose Reductase Metabolic Disease
    Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac . Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications .
    Exisulind
  • HY-132882

    Others Inflammation/Immunology
    ARN19689 is a potent, selective, orally active and non-covalent inhibitor of N‑Acylethanolamine-Hydrolyzing Acid Amidase (NAAA), with an IC50 of 42 nM. ARN19689 is a promising pharmacological tool to be further investigated in the field of inflammatory conditions .
    ARN19689
  • HY-114412A

    Angiotensin Receptor Neprilysin Inflammation/Immunology
    TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP .
    TD-0212 TFA
  • HY-N7765

    HCV Bacterial Apoptosis Fungal Infection Inflammation/Immunology Cancer
    Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase .
    Oenothein B
  • HY-114412

    Angiotensin Receptor Neprilysin Inflammation/Immunology Endocrinology
    TD-0212 (compound 35) is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP .
    TD-0212
  • HY-N1377

    Bacterial Infection Metabolic Disease Inflammation/Immunology
    Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive .
    Nevadensin
  • HY-12345
    ML365
    3 Publications Verification

    Potassium Channel Cardiovascular Disease
    ML365 is a selective two-pore domain potassium channel KCNK3/TASK1 inhibitor, with an IC50 of 4 nM. ML365 acts as a pharmacological tool that can be used to examine the specific roles of TASK1 channels .
    ML365
  • HY-19675

    LT-NS 001; MX 1094

    COX Inflammation/Immunology
    Naproxen etemesil is a lipophilic, non-acidic, inactive proagent of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
    Naproxen etemesil
  • HY-13991
    CCG-1423
    5+ Cited Publications

    Ras Apoptosis Cancer
    CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
    CCG-1423
  • HY-117426

    Others Cancer
    MO-I-500 is a pharmacological of FTO inhibitor with an IC50 of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer .
    MO-I-500
  • HY-119917

    p38 MAPK MEK Bacterial Infection Cancer
    Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities .
    Gossypetin
  • HY-160624

    Polo-like Kinase (PLK) Cancer
    CD 10899 is a hydroxylated metabolite of Volasertib (HY-12137). CD 10899 is pharmacologically active against Polo-like kinase 1 (PLK1) (IC50: 6 nM). Volasertib is an orally active, highly potent and ATP-competitive PLK1 inhibitor. CD 10899 can be used for research of cancer .
    CD 10899
  • HY-116211

    WIN-25978

    Biochemical Assay Reagents Neurological Disease
    Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
    Amfonelic acid
  • HY-N0005S

    Diferuloylmethane-d6; Natural Yellow 3-d6; Turmeric yellow-d6

    Keap1-Nrf2 Ferroptosis Autophagy Histone Acetyltransferase Epigenetic Reader Domain Mitophagy Influenza Virus Infection Metabolic Disease Inflammation/Immunology
    Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
    Curcumin-d6
  • HY-12445
    Asnuciclib
    2 Publications Verification

    CDKI-73; LS-007

    CDK Apoptosis Inflammation/Immunology Cancer
    Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion .
    Asnuciclib
  • HY-114372

    Lipoxygenase Caspase Apoptosis Cancer
    Lycopodine, a pharmacologically important bioactive component derived from Lycopodium clavatumspores, triggers apoptosis by modulating 5-lipoxygenase, and depolarizing mitochondrial membrane potential in refractory prostate cancer cells without modulating p53 activity . Lycopodine inhibits proliferation of HeLa cells through induction of apoptosis via caspase-3 activation .
    Lycopodine
  • HY-N0240
    Herbacetin
    4 Publications Verification

    Others Cancer
    Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects . Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis .
    Herbacetin
  • HY-106975

    Neprilysin Cardiovascular Disease
    SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the proagent SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity .
    SCH-42354
  • HY-100359
    CL-82198
    4 Publications Verification

    MMP Inflammation/Immunology Cancer
    CL-82198 is a selective inhibitor of MMP-13. CL-82198 binds to the entire S1’ pocket of MMP-13, which is the basis for its selectivity towards MMP-13 and the lack of inhibitory activities against other MMPs . CL-82198 is a pharmacologic treatment for preventing osteoarthritis (OA) progression .
    CL-82198
  • HY-124745

    MAP4K Wnt Apoptosis Cancer
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity .
    KY-05009
  • HY-N7255

    p38 MAPK Apoptosis Cancer
    Cycloartenol, a phytosterol compound, is one of the key precusor substances for biosynthesis of numerous sterol compounds. Cycloartenol inhibits the migration of glioma cells and suppresses the phosphorylation of the p38 MAP kinase. Cycloartenol has a variety of pharmacological activities such as anti-inflammatory, anti-tumor, antioxidant, antibiosis and anti-alzheimer's disease. Cycloartenol also plays an important role in the process of plant growth and development .
    Cycloartenol
  • HY-101293

    CID-53361951; ML-270

    Phospholipase Fungal Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases .
    VU0359595
  • HY-135774

    Drug Metabolite Phosphatase Cardiovascular Disease
    6-Hydroxybenzbromarone is the major metabolite of Benzbromarone with a longer half-life and greater pharmacological potency than the parent compound. 6-Hydroxybenzbromarone is a protein Eyes Absent 3 (EYA3) inhibitor with an IC50 value of 21.5 μM. 6-Hydroxybenzbromarone is an anti-angiogenic agent, has strong inhibitory effects on cell migration, tubulogenesis, and angiogenic sprouting .
    6-Hydroxybenzbromarone
  • HY-P1410
    GsMTx4
    25+ Cited Publications

    TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4
  • HY-P1410A
    GsMTx4 TFA
    25+ Cited Publications

    TRP Channel Piezo Channel Cardiovascular Disease Neurological Disease Inflammation/Immunology
    GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
    GsMTx4 TFA
  • HY-107802

    Breviscapinun

    Others Cardiovascular Disease
    Breviscapine is a crude flavonoid extract of Breviscapine, which is more than 85% of the active ingredient, Breviscapine. Breviscapine has a wide range of cardiovascular pharmacological activities, such as increasing blood flow, improving microcirculation, dilating blood vessels, reducing blood viscosity, promoting fibrinolysis, inhibiting platelet aggregation and thrombosis. Breviscapine has been used in the study of cerebral infarction and its sequelae, cerebral thrombosis, coronary heart disease and angina pectoris .
    Breviscapine
  • HY-N0005
    Curcumin
    Maximum Cited Publications
    62 Publications Verification

    Diferuloylmethane; Natural Yellow 3; Turmeric yellow

    Histone Acetyltransferase Epigenetic Reader Domain Keap1-Nrf2 Autophagy Mitophagy Influenza Virus Ferroptosis Cancer
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin
  • HY-N1940
    β-Anhydroicaritin
    1 Publications Verification

    β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
    β-Anhydroicaritin
  • HY-N3127

    Casein Kinase PI3K VEGFR Metabolic Disease
    Orobol is one of the major soy isoflavones and has various pharmacological activities, including anti-skin-aging and anti-obesity effects. Orobol inhibits CK1ε, VEGFR2, MAP4K5, MNK1, MUSK, TOPK, and TNIK (IC50=1.24-4.45 μM). Orobol also inhibits PI3K isoforms (IC50=3.46-5.27 μM for PI3K α/β/γ/K/δ) .
    Orobol
  • HY-103160A
    EHNA hydrochloride
    3 Publications Verification

    Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Infection Cardiovascular Disease Neurological Disease Cancer
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
    EHNA hydrochloride
  • HY-136726

    CINK4

    CDK Cancer
    GP-82996 (CINK4) is a pharmacological inhibitor of CDK4/6. GP-82996 has IC50s of 1.5, 5.6 and 25 μM for CDK4/cyclin D1, CDK6/cyclin D1 and Cdk5/p35, respectively. GP-82996 induces the apoptosis of cancer cells U2OS. GP-82996 can be used in the research of cancer .
    CGP-82996
  • HY-N0408
    Picroside II
    1 Publications Verification

    NF-κB Reactive Oxygen Species Apoptosis Influenza Virus Infection Neurological Disease Inflammation/Immunology Cancer
    Picroside II, an iridoid compound extracted from Picrorhiza, exhibits anti-inflammatory and anti-apoptotic activities. picroside II alleviates the inflammatory response in sepsis and enhances immune function by inhibiting the activation of NLRP3 inflammasome and NF-κB pathways . Picroside II is an antioxidant, exhibits a significant neuroprotective effect through reducing ROS production and protects the blood-brain barrier (BBB) after cerebral ischemia-reperfusion (CI/R) injury. Picroside II has antioxidant, anti-inflammatory, immune regulatory, anti-virus and other pharmacological activities .
    Picroside II
  • HY-N0103
    Sophocarpine
    5 Publications Verification

    Autophagy Apoptosis PI3K Akt Influenza Virus Infection Inflammation/Immunology Cancer
    Sophocarpine is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer .
    Sophocarpine
  • HY-N0103A
    Sophocarpine monohydrate
    5 Publications Verification

    Autophagy Apoptosis PI3K Akt Influenza Virus Infection Inflammation/Immunology Cancer
    Sophocarpine (monohydrate) is one of the significant alkaloid extracted from the traditional herb medicine Sophora flavescens which has many pharmacological properties such as anti-virus, anti-tumor, anti-inflammatory. Sophocarpine (monohydrate) significantly inhibits the growth of gastric cancer (GC) cells through multiple mechanisms such as induction of autophagy, activation of cell apoptosis and down-regulation of cell survival PI3K/AKT signaling pathway. Sophocarpine (monohydrate) has been demonstrated to have anti-tumor activity in various cancer cells, including hepatocellular carcinoma, prostate cancer and colorectal cancer .
    Sophocarpine monohydrate
  • HY-112499

    Vitamin K2-7; Vitamin K2(35); Vitamin MK-7

    Others Cardiovascular Disease
    Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .
    Menaquinone-7
  • HY-124322

    Beta-secretase Neurological Disease Inflammation/Immunology
    NB-360 is a potent, brain penetrable, and orally bioavailable dual BACE1/BACE2 inhibitor (IC50: mouse and human BACE1=5 nM; BACE2=6 nM). NB-360 shows a superior pharmacological profile and robust reduction of amyloid-β and neuroinflammation in amyloid precursor protein(APP) transgenic mice. NB-360 can completely block the progression of Aβ deposition in the brains of APP transgenic mice. NB-360 shows excellent selectivity over the related aspartyl proteases pepsin, cathepsin D and cathepsin E .
    NB-360
  • HY-149008

    Amylases Metabolic Disease Cancer
    α-Amylase-IN-3 (Compound 4) is a none-competitive type of α-Amylase inhibitor with an IC50 value of 18.04 μM, which also has radical scavenging activities (DPPH and ABTS) with IC50 values of 16.04 μM (DPPH) and 16.99 μM (ABTS), respectively. α-Amylase-IN-3 has good protein–ligand interactions profile against α-Amylase. α-Amylase-IN-3 may have pharmacological activities such as anti-oxidative, anti-inflammatory inhibitory, which is helpful for the development of diabetes and oxidative stress associated disease .
    α-Amylase-IN-3
  • HY-112499R

    Vitamin K2-7(Standard); Vitamin K2(35)(Standard); Vitamin MK-7 (Standard)

    Others Cardiovascular Disease
    Menaquinone-7 (Standard) is the analytical standard of Menaquinone-7. This product is intended for research and analytical applications. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .
    Menaquinone-7 (Standard)

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