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Results for "

Macrocyclic inhibitors

" in MedChemExpress (MCE) Product Catalog:

61

Inhibitors & Agonists

2

Screening Libraries

3

Biochemical Assay Reagents

16

Peptides

12

Natural
Products

3

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-I0179
    ITMN 4077

    		HCV Protease Infection
    ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC50: 2131 nM) .
    ITMN 4077
  • HY-15739
    Ansamitocin P-3
    5+ Cited Publications

    Antibiotic C 15003P3; Maytansinol isobutyrate

    		 Microtubule/Tubulin ADC Cytotoxin Bacterial Antibiotic Infection Cancer
    Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.
    Ansamitocin P-3
  • HY-162234
    PKCTheta-IN-1

    		PKC Others
    PKCTheta-IN-1 (Compound 19) is a selective macrocyclic PKCTheta inhibitor with IC50 value of 0.1 nM .
    PKCTheta-IN-1
  • HY-161079
    TDI-8304

    		Parasite Infection
    TDI-8304, a macrocyclic peptide, is a potent, species selective, and noncovalent Plasmodium falciparum (Pf20S) inhibitor. TDI-8304 shows highly selective for Pf20S over human proteasomes .
    TDI-8304
  • HY-176417
    Antifungal agent 132

    		Fungal Antibiotic Infection
    Antifungal agent 132 (compound 25) is a selective and potent antifungal agent. Antifungal agent 132 inhibits Cryptococcus neoformans May1 with a Ki of 180 pM .
    Antifungal agent 132
  • HY-147429A
    Zosurabalpin TFA

    Abx MCP TFA; RG6006 TFA

    		 Antibiotic Bacterial Infection
    Zosurabalpin TFA is a tethered macrocyclic peptide antibiotic, acting specifically on A. baumannii. Zosurabalpin TFA inhibits lipopolysaccharide-transport .
    Zosurabalpin TFA
  • HY-P3356
    Cyclotheonellazole A

    		Elastase Proteasome Inflammation/Immunology
    Cyclotheonellazole A is a natural macrocyclic peptide and a potent elastase inhibitor (IC50=0.034 nM). Cyclotheonellazole A inhibits chymotrypsin with an IC50 value of 0.62 nM .
    Cyclotheonellazole A
  • HY-156105
    8304-vs

    		Parasite Proteasome Infection
    8304-vs is a macrocyclic anti-Plasmodial agent that covalently and irreversibly targets the Plasmodium proteasome. 8304-vs effectively inhibits the growth of Plasmodium falciparum .
    8304-vs
  • HY-P3270
    Capreomycin

    		Bacterial Antibiotic Infection
    Capreomycin is a macrocyclic peptide antibiotic. Capreomycin can be used for anti-multidrug-resistant-tuberculosis research. Capreomycin can inhibit phenylalanine synthesis in in mycobacterial ribosomes translation
    Capreomycin
  • HY-P2331
    Actagardin

    Antibiotic A 3802-IV-3; Gardimycin

    		 Antibiotic Infection
    Actagardin is a tetracyclic lantibiotic produced by several species of Actinoplanes. It is composed of macrocyclic rings formed by thioether bridges. Actagardin preferably targets Gram-positive bacteria, inhibiting the synthesis of peptidoglycan.
    Actagardin
  • HY-145263
    VD2173

    		Ser/Thr Protease Cancer
    VD2173 is a side chain cyclized macrocyclic peptide inhibitor of HGF-activating serine proteases. VD2173 potently inhibits matriptase and hepsin. VD2173 can be used for the research of lung cancer .
    VD2173
  • HY-139105
    20-O-Demethyl-AP3

    		Microtubule/Tubulin Infection Cancer
    20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. Ansamitocin P-3, a microtubule inhibitor, is a macrocyclic antitumor antibiotic .
    20-O-Demethyl-AP3
  • HY-158150
    20S Proteasome-IN-5

    		Proteasome Cancer
    20S Proteasome-IN-5 (Compound 5) is a macrocyclic inhibitor of the 20S Proteasome, with IC50 values of 0.19 and 52.5 μM for ChT-L and PGPH-L activity, respectively .
    20S Proteasome-IN-5
  • HY-13756A
    Tacrolimus monohydrate
    Maximum Cited Publications
    83 Publications Verification

    FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate

    		 Phosphatase FKBP Autophagy Bacterial Antibiotic Infection Inflammation/Immunology Cancer
    Tacrolimus monohydrate (FK506 monohydrate), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex and inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
    Tacrolimus monohydrate
  • HY-13756
    Tacrolimus
    Maximum Cited Publications
    83 Publications Verification

    FK506; Fujimycin; FR900506

    		 Phosphatase FKBP Bacterial Autophagy Antibiotic Infection Inflammation/Immunology Cancer
    Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
    Tacrolimus
  • HY-P3502
    Zilucoplan

    RA101495; RA3193

    		 Complement System Inflammation/Immunology
    Zilucoplan (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan can be used in research of immune-mediated necrotising myopathy (IMNM) .
    Zilucoplan
  • HY-172320
    BMS-986238

    		PD-1/PD-L1 Cancer
    BMS-986238, a second-generation macrocyclic peptide, is a potent PD-L1 inhibitor. BMS-986238 has the potential for the study of solid tumours and lymphomas (cancer of the lymphatic system) .
    BMS-986238
  • HY-19628A
    OD36 hydrochloride

    		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
  • HY-19628
    OD36

    		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-P3502A
    Zilucoplan TFA

    RA101495 TFA; RA3193 TFA

    		 Complement System Inflammation/Immunology
    Zilucoplan TFA (RA101495), a 15-amino acid macrocyclic peptide, is a potent complement component 5 (C5) inhibitor. Zilucoplan TFA can be used in research of immune-mediated necrotising myopathy (IMNM) .
    Zilucoplan TFA
  • HY-P5963
    Lib2-1

    		Interleukin Related Inflammation/Immunology
    Lib2-1, a macrocyclic peptide, is an IL-17C/IL-17RE interaction inhibitor. Lib2-1 can be used for autoimmune and inflammatory diseases research .
    Lib2-1
  • HY-N7765
    Oenothein B

    		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-173076
    HDAC11-IN-1

    		HDAC YAP Inflammation/Immunology
    HDAC11-IN-1 (Compound 14-N C6OH) is a selective macrocyclic inhibitor of HDAC11 with a Ki of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .
    HDAC11-IN-1
  • HY-P10375
    BMS-986189

    		PD-1/PD-L1 Inflammation/Immunology Cancer
    BMS-986189 is a macrocyclic peptide PD-1/PD-L1 interaction with an IC50 of 1.03 nM inhibitor. BMS-986189 can be used for cancer research, such as human lung carcinoma cells L2987 .
    BMS-986189
  • HY-133015
    Mcl-1 inhibitor 3

    		Bcl-2 Family Cancer
    Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity .
    .
    Mcl-1 inhibitor 3
  • HY-15739R
    Ansamitocin P-3 (Standard)

    Antibiotic C 15003P3 (Standard); Maytansinol isobutyrate (Standard)

    		 Microtubule/Tubulin ADC Cytotoxin Bacterial Antibiotic Infection Cancer
    Ansamitocin P-3 (Standard) is the analytical standard of Ansamitocin P-3. This product is intended for research and analytical applications. Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.
    Ansamitocin P-3 (Standard)
  • HY-107486
    Nosiheptide

    Multhiomycin; RP 9671

    		 Bacterial Antibiotic Infection
    Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth .
    Nosiheptide
  • HY-144614
    JH-XVII-10

    		DYRK Apoptosis Neurological Disease Cancer
    JH-XVII-10 is a potent, selective and orally active DYRK1A and DYRK1B inhibitor with IC50s of 3 nM and 5 nM for DYRK1A and DYRK1B, respectively. JH-XVII-10 shows antitumor efficacy in neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XVII-10
  • HY-13756R
    Tacrolimus (Standard)

    		Phosphatase FKBP Bacterial Autophagy Antibiotic Infection Inflammation/Immunology Cancer
    Tacrolimus (Standard) is the analytical standard of Tacrolimus. This product is intended for research and analytical applications. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
    Tacrolimus (Standard)
  • HY-107212
    Selamectin

    		Parasite Chloride Channel P-glycoprotein Bacterial Infection
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
    Selamectin
  • HY-13756S2
    Tacrolimus-d3

    FK506-d3; Fujimycin-d3; FR900506-d3

    		 Isotope-Labeled Compounds Autophagy FKBP Bacterial Antibiotic Phosphatase Infection Inflammation/Immunology Cancer
    Tacrolimus-d3 (FK506-d3) is deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
    Tacrolimus-d3
  • HY-13756S
    Tacrolimus-13C,d2

    FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2

    		 Phosphatase FKBP Bacterial Autophagy Antibiotic Infection Inflammation/Immunology Cancer
    Tacrolimus- 13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties .
    Tacrolimus-13C,d2
  • HY-168902
    Proteasome-IN-7

    		Proteasome Cancer
    Proteasome-IN-7 (Compound 6f) is an epoxyketone macrocyclic peptidyl proteasome inhibitor (IC50 value of 37.92 nM for 20S proteasome ChT-L subunit). Proteasome-IN-7 displays robust antiproliferative effects against multiple myeloma, acute lymphoblastic leukemia and non-small cell lung cancer .
    Proteasome-IN-7
  • HY-P10700
    RO7196472

    		Antibiotic Infection
    RO7196472 is a potent and selective macrocyclic peptide antibiotic that targets Acinetobacter strains. RO7196472 inhibits Acinetobacter strain activity by specifically binding to the Lipopolysaccharide (LPS) binding site on the LptB2FG complex located on the inner membrane of Acinetobacter strains, thereby blocking LPS transport and suppressing Acinetobacter strain activity .
    RO7196472
  • HY-17580
    Fidaxomicin
    5+ Cited Publications

    OPT-80; PAR-101

    		 DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Infection
    Fidaxomicin (OPT-80), a macrocyclic antibiotic, is an orally active and potent RNA polymerase inhibitor. Fidaxomicin has a narrow spectrum of antibacterial activity and a good anti-Clostridium difficile activity (MIC90=0.12 μg/mL). Fidaxomicin can be used for Clostridium difficile infection (CDI) research .
    Fidaxomicin
  • HY-17566
    Capreomycin sulfate
    2 Publications Verification

    		 Antibiotic Bacterial Infection Neurological Disease Metabolic Disease
    Capreomycin sulfate is a macrocyclic peptide antibiotic that inhibits phenylalanine synthesis in mycobacterial ribosomal translation. Capreomycin sulfate has anti-amyloidogenic and pro-fibrinolytic activities, reducing amyloid-induced cytotoxicity by inhibiting the occurrence of amyloid fibrillation. Capreomycin sulfate can be used in the study of multidrug-resistant tuberculosis, type 2 diabetes, Alzheimer's disease and Parkinson's disease .
    Capreomycin sulfate
  • HY-P10855
    S1b3inL1

    		SARS-CoV Infection
    S1b3inL1 is a SARS-CoV-2 spike protein macrocyclic peptide inhibitor. S1b3inL1 can bind the conserved site of spike protein with high affinity and inhibit the infection of various SARS-CoV-2 variant strains. S1b3inL1 has antiviral activity .
    S1b3inL1
  • HY-144068
    Cap-dependent endonuclease-IN-25

    		Influenza Virus Infection
    Cap-dependent endonuclease-IN-25 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-25 is a macrocyclic pyridotriazine derivative. Cap-dependent endonuclease-IN-25 has the potential for the research of viral infections caused by viruses belonging to the Orthomyxoviridae family (extracted from patent WO2020075080A1, compound 4) .
    Cap-dependent endonuclease-IN-25
  • HY-N0750
    Monocrotaline
    30+ Cited Publications

    Crotaline

    		 Others Metabolic Disease Cancer
    Monocrotaline is an 11-membered macrocyclic pyrrolizidine alkaloid. Monocrotaline inhibits OCT-1 and OCT-2 with IC50s of 36.8 µM and 1.8 mM, respectively. Monocrotaline has antitumor activity and is cytotoxic to hepatocellular carcinoma cells. Monocrotaline is used to induce a model of pulmonary hypertension in rodents. [2][6][8].
    Monocrotaline
  • HY-W034576
    Hexacyclen hexahydrochloride

    Hexaaza-18-crown-6 hexahydrochloride; 1,4,7,10,13,16-Hexaazacyclooctadecane hexahydrochloride

    		 Biochemical Assay Reagents Cancer
    Hexacyclen (Cycloalkene) is an organic compound with a unique macrocyclic structure composed of six nitrogen-containing rings. Hexacyclen is commonly used as a chelating agent in chemistry and biochemistry due to its ability to bind metal ions, and is often used to selectively bind metal ions in proteins or enzymes to study their structure and function. Hexacyclen also acts as an inhibitor of cancer .
    Hexacyclen hexahydrochloride
  • HY-107426
    Verrucarin A

    Muconomycin A

    		 Apoptosis Reactive Oxygen Species Cancer
    Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
    Verrucarin A
  • HY-161370
    VD4162

    		Ser/Thr Protease Cancer
    VD4162 (Compound 8b) is a macrocyclic inhibitor of serine proteases. VD4162 can significantly improve potency for all four target enzymes TMPRSS2 (IC50 = 3.7 nM), HGFA(IC50 = 3.3 nM), matriptase (IC50 = 2.9 nM), and hepsin (IC50 = 0.54 nM). VD4162 can be used for the research of cancer .
    VD4162
  • HY-17580S
    Fidaxomicin-d7

    		Isotope-Labeled Compounds Bacterial Apoptosis Antibiotic Infection
    Fidaxomicin-d7 (OPT-80-D7) is the deuterium labeled Fidaxomicin. Fidaxomicin (OPT-80), a macrocyclic RNA polymerase inhibitor, has a narrow spectrum of activity. Fidaxomicin selectively eradicates pathogenic Clostridium difficile with minimal disruption to the multiple species of bacteria that make up the normal, healthy intestinal flora .
    Fidaxomicin-d7
  • HY-107486R
    Nosiheptide (Standard)

    		Bacterial Antibiotic Infection
    Nosiheptide (Standard) is the analytical standard of Nosiheptide. This product is intended for research and analytical applications. Nosiheptide (Multhiomycin), a thiopeptide antibiotic produced by Streptomyces actuosus, inhibits bacterial protein synthesis and bears a unique indole side ring system and regiospecific hydroxyl groups on the characteristic macrocyclic core. Nosiheptide has been widely used as a feed additive for animal growth .
    Nosiheptide (Standard)
  • HY-107212R
    Selamectin (Standard)

    		Parasite Chloride Channel P-glycoprotein Bacterial Infection
    Selamectin (Standard) is the analytical standard of Selamectin. This product is intended for research and analytical applications. Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM .
    Selamectin (Standard)
  • HY-144617
    JH-XIV-68-3

    		DYRK Cancer
    JH-XIV-68-3 is a selective macrocyclic inhibitor of DYRK1A/B. JH-XIV-68-3 displays selectivity for DYRK1A and close family member DYRK1B in biochemical and cellular assays. JH-XIV-68-3 demonstrates antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines .
    JH-XIV-68-3
  • 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 .
    BACE1-IN-8
  • 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 .
    BACE1-IN-9
  • HY-17580R
    Fidaxomicin (Standard)

    		DNA/RNA Synthesis Bacterial Apoptosis Antibiotic Infection
    Fidaxomicin (Standard) is the analytical standard of Fidaxomicin. This product is intended for research and analytical applications. Fidaxomicin (OPT-80), a macrocyclic antibiotic, is an orally active and potent RNA polymerase inhibitor. Fidaxomicin has a narrow spectrum of antibacterial activity and a good anti-Clostridium difficile activity (MIC90=0.12 μg/mL). Fidaxomicin can be used for Clostridium difficile infection (CDI) research .
    Fidaxomicin (Standard)
  • HY-P3143
    BMSpep-57

    		PD-1/PD-L1 Cancer
    BMSpep-57 is a potent and competitive macrocyclic peptide inhibitor of PD-1/PD-L1 interaction with an IC50 of 7.68 nM. BMSpep-57 binds to PD-L1 with Kds of 19 nM and 19.88 nM in MST and SPR assays, respectively. BMSpep-57 facilitates T cell function by in creasing IL-2 production in PBMCs .
    BMSpep-57

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