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Results for "

Cyclic inhibitor

" in MCE Product Catalog:

91

Inhibitors & Agonists

1

Screening Libraries

23

Peptides

18

Natural
Products

6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-N6717
    Tentoxin

    Others Infection
    Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
  • HY-111673
    8-CPT-Cyclic AMP sodium

    8-CPT-cAMP sodium; 8-(p-Chlorophenylthio)-cAMP sodium

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50Cyclic AMP sodium is a very high affinity for Epac and is a potent Epac activator.
  • HY-108974
    Drotaverine hydrochloride

    Phosphodiesterase (PDE) Calcium Channel
    Drotaverine (hydrochloride) is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
  • HY-P1789
    CTTHWGFTLC, CYCLIC

    MMP Cancer Inflammation/Immunology
    CTTHWGFTLC, CYCLIC is a cyclic peptide inhibitor for matrix metalloproteinases MMP-2 and MMP-9. The IC50 value for MMP-9 is ~8 μM.
  • HY-P1789A
    CTTHWGFTLC, CYCLIC TFA

    MMP Cancer Inflammation/Immunology
    CTTHWGFTLC, CYCLIC TFA is a cyclic peptide inhibitor for matrix metalloproteinases MMP-2 and MMP-9. The IC50 value for MMP-9 is ~8 μM.
  • HY-123076
    Pifithrin-α, p-Nitro, Cyclic

    PFN-α

    MDM-2/p53 Neurological Disease
    Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
  • HY-108623
    Atizoram

    CP-80,633

    Phosphodiesterase (PDE) Inflammation/Immunology
    Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice.
  • HY-B1730
    Phensuximide

    Others Metabolic Disease Neurological Disease
    Phensuximide is an orally active succinimide antiepileptic and anticonvulsant agent. Phensuximide inhibits cyclic AMP and cyclic GMP accumulation in depolarized brain tissue. Phensuximide can be used for the study of seizure and petit mal.
  • HY-108974S
    Drotaverine-d10 hydrochloride

    Phosphodiesterase (PDE) Calcium Channel
    Drotaverine-d10 hydrochloride is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects.
  • HY-19930
    Vaborbactam

    RPX7009

    Bacterial Infection
    Vaborbactam (RPX7009) is a cyclic boronic acid pharmacophore β-lactamase inhibitor.
  • HY-101661
    Win 58237

    Phosphodiesterase (PDE) Cardiovascular Disease
    Win 58237 is a cyclic nucleotide phosphodiesterase (PDE) inhibitor, with Ki of 170 nM for PDE V, possessing vasorelaxant activity.
  • HY-146127
    Grb2 SH2 domain inhibitor 1

    Others Others
    Hy-146127 is a conformationally restricted cyclic cell penetrating peptide (CPP) containing d-pro-l-pro motif ring (AF Φ Rpprrfq) (where Φ It is L-naphthylalanine, R is D-arginine, P is D-proline), which is mainly used as a cyclic peptide inhibitor.
  • HY-N0113
    Hordenine

    Ordenina; Peyocactine

    Bacterial Antibiotic Infection Cardiovascular Disease
    Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production.
  • HY-147946
    PDE1-IN-4

    Phosphodiesterase (PDE) Calcium Channel Inflammation/Immunology
    PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.
  • HY-P1975
    Aureobasidin A

    Basifungin

    Fungal Infection Inflammation/Immunology
    Aureobasidin A (Basifungin), a cyclic depsipetide, is an antifungal antibiotic. Aureobasidin A (Basifungin) A is an inhibitor of the inositolphosphorylceramide synthase AUR1.
  • HY-134482
    PCSK9-IN-1

    Ser/Thr Protease Cardiovascular Disease
    PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a Ki value of 1.46 nM.
  • HY-33900
    Dihydrofuran-3(2H)-one

    3-Oxotetrahydrofuran

    Others Others
    Dihydrofuran-3(2H)-one (3-Oxotetrahydrofuran) is used for synthesizing cyclic ketone inhibitors that inhibits the serine protease plasmin.
  • HY-N6793
    Phomopsin A

    Microtubule/Tubulin Cancer
    Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin.
  • HY-50723
    3-Methylxanthine

    Endogenous Metabolite Others
    3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.
  • HY-U00136
    Win-62005

    Phosphodiesterase (PDE) Cardiovascular Disease
    Win-62005 is a cyclic AMP phosphodiesterase III (PDE III) inhibitor with Kis of 25 and 26 nM for rat heart and canine aorta, respectively.
  • HY-131900
    Protein kinase inhibitor H-7

    PKC Cancer
    Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC.
  • HY-131083
    ε-Amanitin

    DNA/RNA Synthesis ADC Cytotoxin Cancer
    ε-Amanitin, a cyclic peptide isolated from a variety of mushroom species, potently binds to and inhibits the activity of RNA polymerase II.
  • HY-115732
    PKA-IN-1

    PKA Inflammation/Immunology
    PKA-IN-1 is a potent and selective cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor with an IC50 of 0.03 μM.
  • HY-N6781
    Ophiobolin A

    Phosphodiesterase (PDE) Cancer Infection
    Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
  • HY-N1469
    Kaurenoic acid

    Others Inflammation/Immunology Neurological Disease
    Kaurenoic acid is a diterpene from Sphagneticola trilobata, inhibits Inflammatory Pain by the inhibition of cytokine production and activation of the NO–cyclic GMP–PKG–ATP-sensitive potassium channel signaling pathway.
  • HY-126856
    HC-Toxin

    HDAC Apoptosis Cancer
    HC-Toxin, a cyclic tetrapeptide, is a potent HDAC inhibitor with an IC50 of 30 nM. HC-Toxin induces tumor cell apoptosis and has anticancer effects.
  • HY-14841
    Gisadenafil

    UK-369003

    Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
  • HY-144752
    cSPM

    Cyclic spermine

    Others Neurological Disease
    cSPM (Cyclic spermine) is a Aβ42 inhibitor. cSPM could suppress the aggregation of three different peptides, Aβ42, amylin and insulin, and decreases cytotoxicity.
  • HY-128583
    G150

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    G150 is a potent and highly selective human cyclic GMP-AMP synthase (h-cGAS) inhibitor for repression of dsDNA-triggered interferon expression, with an IC50 of 10.2 nM.
  • HY-15979
    H-89

    PKA Autophagy Neurological Disease
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
  • HY-108619
    Gisadenafil besylate

    UK 369003-26

    Phosphodiesterase (PDE) Neurological Disease
    Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
  • HY-N0113S
    Hordenine-d6

    Ordenina-d6; Peyocactine-d6

    Bacterial Antibiotic Infection Cardiovascular Disease
    Hordenine-d6 (Ordenina-d6) is the deuterium labeled Hordenine. Hordenine, an alkaloid found in plants, inhibits melanogenesis by suppression of cyclic adenosine monophosphate (cAMP) production.
  • HY-108952
    17,17-(Ethylenedioxy)androst-4-en-3-one

    Others Endocrinology
    17,17-(Ethylenedioxy)androst-4-en-3-one (4-​androstene-​3,​17-​dione-​17-​cyclic ethylene ketal) is an effective ingredient in cosmetics, which can be used for acne and promote hair growth research. 17,17-(Ethylenedioxy)androst-4-en-3-one can inhibit the reductase activity and inhibit the bond of a receptor protein and 5α-DHT.
  • HY-12085
    Apremilast

    CC-10004

    Phosphodiesterase (PDE) Apoptosis TNF Receptor Inflammation/Immunology
    Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-114182
    PF-06928215

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ. PF-06928215 has a high binding affinity of 0.2 μM (Kd).
  • HY-101962
    HNMPA

    Insulin Receptor Metabolic Disease
    HNMPA is a membrane impermeable insulin receptor tyrosine kinase inhibitor. HNMPA inhibits serine and tyrosine autophosphorylation by the human insulin receptor. HNMPA has no effect on protein kinase C or cyclic AMP-dependent protein kinase activities
  • HY-100164
    SDZ-MKS 492

    MKS 492

    Phosphodiesterase (PDE) Inflammation/Immunology
    SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
  • HY-133916
    G140

    Cyclic GMP-AMP Synthase Inflammation/Immunology
    G140 is a potent and selective inhibitor of cyclic GMP-AMP synthase (cGAS), with IC50s of 14.0 nM and 442 nM for h-cGAS and m-cGAS, respectively. G140 has anti-inflammatory activity.
  • HY-146075
    β-Lactamase-IN-8

    Bacterial Infection
    β-Lactamase-IN-8 (compound 20) is a potent and oral bioavailable broad-spectrum cyclic boronate β-lactamase inhibitor. β-Lactamase-IN-8 can be used for researching antibacteria.
  • HY-144739
    BACE1-IN-8

    Beta-secretase Neurological Disease
    BACE1-IN-8 (compound 70b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 3.9 µM.
  • HY-144741
    BACE1-IN-9

    Beta-secretase Neurological Disease
    BACE1-IN-9 (compound 82b) is a potent BACE1 (β-site APP cleaving enzyme 1) inhibitor, with an IC50 of 1.2 µM.
  • HY-B0128
    Diphylline

    Diprophylline

    Adenosine Receptor Phosphodiesterase (PDE) Inflammation/Immunology Cardiovascular Disease
    Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclic nucleotide phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator drug and has the potential for chronic bronchitis and emphysema.
  • HY-B1294
    Amrinone

    Inamrinone

    Phosphodiesterase (PDE) Cardiovascular Disease
    Amrinone (Inamrinone) is a positive inotropic-vasodilator agent. Amrinone is a selective phosphodiesterase III inhibitor that increases cyclic adenosine monophosphate by preventing its breakdown. Amrinone is also an orally active, non-glycosidic and non-catecholamine cardiotonic agent.
  • HY-B0392
    (S)-(+)-Rolipram

    (+)-Rolipram; (S)-Rolipram

    Phosphodiesterase (PDE) Apoptosis Cancer Inflammation/Immunology Neurological Disease
    (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic AMP(cAMP)-specific phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 1100 nM. (S)-(+)-Rolipram can suppresse tumor necrosis factor-alpha (TNFα) production by human mononuclear cells.
  • HY-125586
    β-Amanitin

    DNA/RNA Synthesis ADC Cytotoxin Cancer
    β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. β-Amanitin inhibits inhibits eukaryotic RNA polymerase II and III. β-Amanitin inhibits protein synthesis. β-Amanitin can be used as a cytotoxic component of antibody-drug conjugates (ADCs).
  • HY-P1420
    TAT-cyclo-CLLFVY

    HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
  • HY-12085S
    Apremilast-d5

    CC-10004-d5

    Phosphodiesterase (PDE) TNF Receptor Apoptosis Inflammation/Immunology
    Apremilast D5 (CC-10004 D5) is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM.
  • HY-141550
    BPK-25

    Others Inflammation/Immunology
    BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
  • HY-B0764A
    Bucladesine calcium

    Dibutyryl cAMP calcium salt; DBcAMP calcium salt

    PKA Phosphodiesterase (PDE) Apoptosis Others
    Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
  • HY-P2698
    1-Alaninechlamydocin

    HDAC Apoptosis Cancer
    1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC50=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.
  • HY-100933
    MY-5445

    Phosphodiesterase (PDE) Cancer Inflammation/Immunology Cardiovascular Disease
    MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a Ki of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.
  • HY-P1420A
    TAT-cyclo-CLLFVY TFA

    HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
  • HY-B0764
    Bucladesine sodium

    Dibutyryl cAMP sodium salt; DBcAMP sodium salt

    PKA Phosphodiesterase (PDE) Inflammation/Immunology
    Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
  • HY-P1178
    Cyclotraxin B

    Trk Receptor Neurological Disease
    Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
  • HY-N6693
    Valinomycin

    NSC 122023

    Bacterial Apoptosis Antibiotic Autophagy Infection
    Valinomycin (NSC 122023), a cyclic depsipeptide antibiotic, act as a potassium selective ionophore. Valinomycin (NSC 122023) inhibits lymphocyte proliferation by its effects on the cell membrane, and induces apoptosis in CHO cells. Valinomycin induces activation of PINK1 leading to Parkin Ser65 phosphorylation.
  • HY-114181
    IRAK4-IN-4

    IRAK Cyclic GMP-AMP Synthase Inflammation/Immunology
    IRAK4-IN-4 is an interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor extracted from patent CN107163044A, Compound15, has an IC50 of 2.8 nM. IRAK4-IN-4 also inhibits cyclic GMP-AMP synthase (cGAS) with an IC50 of 2.1 nM.
  • HY-114180
    RU.521

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-P1178A
    Cyclotraxin B TFA

    Trk Receptor Neurological Disease
    Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50  of  0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects.
  • HY-B0162
    Ivabradine

    HCN Channel Cardiovascular Disease
    Ivabradine is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine reduces dose-dependently heart rate without modification of blood pressure. Ivabradine shows anticonvulsant, anti-ischaemic and anti-anginal activity.
  • HY-B0162A
    Ivabradine hydrochloride

    HCN Channel Cardiovascular Disease Endocrinology Cancer
    Ivabradine hydrochloride is a potent and orally active HCN (hyperpolarization-activated cyclic nucleotide-gated) channel blocker that inhibits the cardiac pacemaker current (If). Ivabradine hydrochloride reduces dose-dependently heart rate without modification of blood pressure. Ivabradine hydrochloride shows anticonvulsant, anti-ischaemic and anti-anginal activity.
  • HY-101402
    Cyclo(his-pro)

    Cyclo(histidyl-proline); Histidylproline diketopiperazine

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-129522
    Sulfo-ara-F-NMN

    CZ-48

    Toll-like Receptor (TLR) Neurological Disease
    Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production.
  • HY-N1074
    Warangalone

    Scandenolone

    Parasite PKA Infection Inflammation/Immunology
    Warangalone is an anti-malarial compound which can inhibit the growth of both strains of parasite 3D7 (chloroquine sensitive) and K1 (chloroquine resistant) with IC50s of 4.8 μg/mL and 3.7 μg/mL, respectively. Warangalone can also inhibit cyclic AMP-dependent protein kinase catalytic subunit (cAK) with an IC50 of 3.5 μM.
  • HY-145010
    SN-011

    STING Inflammation/Immunology
    SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease.
  • HY-P1036
    Compstatin

    Complement System Others
    Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-101402A
    Cyclo(his-pro) TFA

    Cyclo(histidyl-proline) TFA; Histidylproline diketopiperazine TFA

    NF-κB Endogenous Metabolite Inflammation/Immunology Neurological Disease
    Cyclo(his-pro) TFA (Cyclo(histidyl-proline) TFA) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) TFA could inhibit NF-κB nuclear accumulation. Cyclo(his-pro) TFA can cross the brain-blood-barrier and affect diverse inflammatory and stress responses.
  • HY-14428
    ICG-001

    β-catenin Apoptosis Cancer
    ICG-001 is an inhibitor of β-catenin/TCF mediated transcription. ICG-001 works by specifically binding to cyclic AMP response element-binding protein with an IC50 of 3 μM. ICG-001 selectively blocks the β-catenin/CBP interaction without interfering with the β-catenin/p300 interaction.
  • HY-N6704
    Enniatin A1

    ERK Apoptosis Cancer
    Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
  • HY-P1045
    187-1, N-WASP inhibitor

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-P1045A
    187-1, N-WASP inhibitor TFA

    Arp2/3 Complex Others
    187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
  • HY-B0763
    Ibudilast

    KC-404; AV-411; MN-166

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
  • HY-115745
    Calmodulin antagonist-1

    CaMK Cardiovascular Disease
    Calmodulin antagonist-1 (W-7) is a calmodulin (CaM) antagonist. Calmodulin antagonist-1 inhibits calmodulin-activated Ca 2+-phosphodiesterase (PDE) (IC50=28 μM). Calmodulin antagonist-1 also inhibits trypsin-treated Ca 2+-PDE (IC50=375 μM) in a competitive fashion with respect to cyclic GMP and the Ki value is 300 μM.
  • HY-P1036A
    Compstatin TFA

    Complement System Others
    Compstatin TFA, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin TFA binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin TFA inhibits only the activation of primates’ complement system. Compstatin TFA exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
  • HY-P2090
    Angiopeptin

    Somatostatin Receptor Adenylate Cyclase Cardiovascular Disease
    Angiopeptin, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin has the potential for coronary atherosclerosis research.
  • HY-P0178
    LXW7

    Integrin Inflammation/Immunology
    LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
  • HY-P2090A
    Angiopeptin TFA

    Somatostatin Receptor Adenylate Cyclase Cardiovascular Disease
    Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research.
  • HY-B0442C
    Vardenafil dihydrochloride

    Endogenous Metabolite Phosphodiesterase (PDE) Endocrinology Metabolic Disease Inflammation/Immunology
    Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes -.
  • HY-B0442A
    Vardenafil hydrochloride

    Phosphodiesterase (PDE) Endogenous Metabolite Endocrinology Metabolic Disease Inflammation/Immunology
    Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research like erectile dysfunction, hepatitis, diabetes[1]-[6].
  • HY-B0442S
    Vardenafil-d5

    Phosphodiesterase (PDE) Endogenous Metabolite Endocrinology
    Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction.
  • HY-P0178A
    LXW7 TFA

    Integrin Inflammation/Immunology
    LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
  • HY-P1934A
    Cyclo(L-Phe-L-Pro)

    Fungal IFNAR Reactive Oxygen Species Cancer Inflammation/Immunology Infection
    Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
  • HY-B0763S1
    Ibudilast-d7

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    Ibudilast-d7 is the deuterium labeled Ibudilast. Ibudilast (KC-404; AV-411; MN-166) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
  • HY-B0442
    Vardenafil

    Phosphodiesterase (PDE) Endogenous Metabolite Endocrinology Metabolic Disease Inflammation/Immunology
    Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
  • HY-13422
    Zatebradine hydrochloride

    UL-FS-49; UL-FS-49CL

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
  • HY-B0763S
    Ibudilast-d3

    Phosphodiesterase (PDE) Inflammation/Immunology Cancer
    Ibudilast-d3 (KC-404-d3) is the deuterium labeled Ibudilast. Ibudilast (KC-404) is a cyclic AMP phosphodiesterase (PDE) inhibitor. Ibudilast has platelet anti-aggregatory effects. Ibudilast can be used for the research of asthma for its inhibitory effects on tracheal smooth muscle contractility. Ibudilast may be a useful neuroprotective and anti-dementia agent counteracting neurotoxicity in activated microglia.
  • HY-105349
    T-0156

    Phosphodiesterase (PDE) Neurological Disease
    T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.
  • HY-N6680
    Virginiamycin S1

    Bacterial Antibiotic Infection
    Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections[1][2].
  • HY-13422A
    Zatebradine

    UL-FS-49 free base; UL-FS-49CL free base

    HCN Channel Cardiovascular Disease
    Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively.
  • HY-103160A
    EHNA hydrochloride

    Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Cancer Infection Neurological Disease Cardiovascular Disease
    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.
  • HY-12379
    NS-2028

    Guanylate Cyclase Inflammation/Immunology
    NS-2028 is a highly selective soluble Guanylyl Cyclase (sGC) inhibitor with IC50 values of 30 nM and 200 nM for basal and NO-stimulated enzyme activity. NS-2028 inhibits soluble Guanylyl Cyclase activity in homogenates of mouse cerebellum and neuronal NO synthase with IC50 values of 17 nM and 20 nM. NS-2028 inhibits 3-morpholino-sydnonimine (SIN-1)-elicited formation of cyclic GMP in human cultured umbilical vein endothelial cells with an IC50 of 30 nM. NS-2028 is commonly used in the research of nitric oxide signaling pathways, it inhibits NO-dependent relaxant responses in non-vascular smooth muscle completely (1 μM). NS-2028 reduces vascular endothelial growth factor-induced angiogenesis and permeability.
  • HY-108648
    2-Methylthioadenosine diphosphate trisodium

    2-Methylthio-ADP trisodium

    P2Y Receptor Neurological Disease
    2-Methylthioadenosine diphosphate trisodium is a potent purinergic P2Y receptors agonist, with EC50s of 19, 6.2, and 5 nM for human P2Y13, mouse P2Y13 and human P2Y12, respectively. 2-Methylthioadenosine diphosphate trisodium has pEC50s of 8.29 and 5.75 for human P2Y1 and rat P2Y6, respectively. 2-Methylthioadenosine diphosphate trisodium induces platelet aggregation and shape change, and inhibits cyclic AMP accumulation in platelets exposed to prostaglandin E1.