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Results for "

macrocyclic inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Payload (2) Antibiotic (17) Apoptosis (8) Autophagy (5) Bacterial (20) Bcl-2 Family (2) Beta-secretase (2) Biochemical Assay Reagents (3) Caspase (1) CDK (2) Chloride Channel (2) Complement System (2) DNA/RNA Synthesis (4) Drug Intermediate (1) DYRK (2) E1/E2/E3 Enzyme (1) Elastase (1) FKBP (5) Fungal (3) HBV (1) HCV (4) HCV Protease (4) HDAC (2) Influenza Virus (2) Interleukin Related (1) Isotope-Labeled Compounds (2) LRRK2 (1) Microtubule/Tubulin (3) P-glycoprotein (2) Parasite (5) PCSK9 (1) PD-1/PD-L1 (6) PERK (1) Phosphatase (5) PKC (1) Proteasome (4) Ras (4) Reactive Oxygen Species (ROS) (1) Reference Standards (6) RIP kinase (2) SARS-CoV (2) Ser/Thr Kinase (1) Ser/Thr Protease (2) TAM Receptor (1) TGF-β Receptor (2) Trk Receptor (1) YAP (2)
By Research Areas:	Cancer (39) Infection (35) Inflammation/Immunology (16) Metabolic Disease (4) Neurological Disease (6)

By Targets:

ADC Payload (2)

Antibiotic (17)

Apoptosis (8)

Autophagy (5)

Bacterial (20)

Bcl-2 Family (2)

Beta-secretase (2)

Biochemical Assay Reagents (3)

Caspase (1)

CDK (2)

Chloride Channel (2)

Complement System (2)

DNA/RNA Synthesis (4)

Drug Intermediate (1)

DYRK (2)

E1/E2/E3 Enzyme (1)

Elastase (1)

FKBP (5)

Fungal (3)

HBV (1)

HCV (4)

HCV Protease (4)

HDAC (2)

Influenza Virus (2)

Interleukin Related (1)

Isotope-Labeled Compounds (2)

LRRK2 (1)

Microtubule/Tubulin (3)

P-glycoprotein (2)

Parasite (5)

PCSK9 (1)

PD-1/PD-L1 (6)

PERK (1)

Phosphatase (5)

PKC (1)

Proteasome (4)

Ras (4)

Reactive Oxygen Species (ROS) (1)

Reference Standards (6)

RIP kinase (2)

SARS-CoV (2)

Ser/Thr Kinase (1)

Ser/Thr Protease (2)

TAM Receptor (1)

TGF-β Receptor (2)

Trk Receptor (1)

YAP (2)

By Research Areas:

Cancer (39)

Infection (35)

Inflammation/Immunology (16)

Metabolic Disease (4)

Neurological Disease (6)

Inhibitors & Agonists

Screening Libraries

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-13756

Tacrolimus Maximum Cited Publications 101 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 .

HY-N0750

Monocrotaline 40+ Cited Publications Crotaline	Others	Infection 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].

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 .

HY-15739

Ansamitocin P-3 5+ Cited Publications Antibiotic C 15003P3; Maytansinol isobutyrate	Microtubule/Tubulin ADC Payload Bacterial Antibiotic	Infection Cancer
Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.

HY-13756A

Tacrolimus monohydrate Maximum Cited Publications 101 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 .

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) .

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 .

HY-17566

Capreomycin sulfate 5 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 .

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 .

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 .

HY-13756S

Tacrolimus-13C,d2 1 Publications Verification 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 .

HY-172320

BMS-986238	PD-1/PD-L1	Cancer
BMS-986238 is an orally active macrocyclic peptide PD-L1 inhibitor. BMS-986238 can be used in the research of tumors such as solid tumors and lymphomas .

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 .

HY-107426

Verrucarin A 1 Publications Verification Muconomycin A	Apoptosis Reactive Oxygen Species (ROS)	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 .

HY-W034566

Hexacyclen Hexaaza-18-crown-6; 1,4,7,10,13,16-Hexaazacyclooctadecane	Biochemical Assay Reagents	Others
Hexacyclen is an organic compound with a unique macrocyclic structure composed of six nitrogen-containing rings. It is commonly used as a chelating agent in chemistry and biochemistry due to its ability to bind metal ions. Inhibitors of certain diseases such as cancer. In biochemistry, Hexacyclen is often used to selectively bind metal ions in proteins or enzymes to study their structure and function. Due to its large size and complex structure, Hexacyclen is not widely used in daily products or applications .

HY-125728

Micrococcin P1	Bacterial Parasite HCV	Infection
Micrococcin P1 is a macrocyclic peptide antibiotic and is a potent hepatitis C virus (HCV) inhibitor with an EC₅₀ range of 0.1-0.5 μM . Micrococcin P1 has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Micrococcin P1 against *S. aureus* 1974149, E. faecalis 1674621 and S. pyogenes 1744264 are 2 μg/mL, 1 μg/mL and 1 μg/mL, respectively . Micrococcin P1 is also a potent inhibitor of the malaria parasite Plasmodium falciparum .

HY-13756R

Tacrolimus (Standard) FK506 (Standard); Fujimycin (Standard); FR900506 (Standard)	Reference Standards 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 .

HY-17580S

Fidaxomicin-d7	Isotope-Labeled Compounds DNA/RNA Synthesis 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 .

HY-10242

Ciluprevir BILN 2061; BILN 2061ZW	HCV HCV Protease DNA/RNA Synthesis	Infection
Ciluprevir (BILN 2061; BILN 2061ZW) is an orally active macrocyclic peptide inhibitor of hepatitis C virus (HCV)NS3 protease, with an IC₅₀ of 3 nM. Ciluprevir has Kᵢ values of 0.66 nM and 0.30 nM against genotypes 1b and 1a, respectively. Ciluprevir inhibits HCV RNA replication with an EC₅₀ of 1.2 nM, and its EC50 values against genotypes 1b and 1a are 3 nM and 4 nM, respectively. Ciluprevir shows no significant inhibition against human leukocyte elastase and hepatic cathepsin B. Ciluprevir can be used for genotype 1 HCV infection .

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 K_Ds of 37 nM .

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 K_ds 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 .

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 .

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 .

HY-P11020

p27 Analogue CP2	E1/E2/E3 Enzyme	Cancer
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (K_d = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .

HY-W004812

BOC-(1R,3S)-3-aminocyclopentane carboxylic acid (1S,3S)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid	Drug Intermediate SARS-CoV	Infection
BOC-(1R,3S)-3-aminocyclopentane carboxylic acid ((1S,3S)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid) is a conformationally constrained peptide building block and a key component of SARS-CoV-2 main protease (Mpro) inhibitors. When incorporated into macrocyclic peptides, BOC-(1R,3S)-3-aminocyclopentane carboxylic acid not only helps generate high-affinity Mpro inhibitors by preorganizing the secondary structure of peptides, but also exerts sequence-dependent functional inhibition on the hydrolytic activity of Mpro. BOC-(1R,3S)-3-aminocyclopentane carboxylic is widely used in COVID-19-related research .

HY-103048A

PD-1/PD-L1-IN 3 TFA	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC₅₀s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases .

HY-I0179

ITMN 4077	HCV Protease	Infection
ITMN 4077 is a macrocyclic inhibitor against Hepatitis C Virus (HCV) NS3 protease (EC₅₀: 2131 nM) .

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

HY-173076A

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

HY-107486R

Nosiheptide (Standard) Multhiomycin (Standard); RP 9671 (Standard)	Reference Standards 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 .

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 .

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 K_Ds of 37 nM .

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 .

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-103048

PD-1/PD-L1-IN 3	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC₅₀s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases .

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 .

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 .

HY-14404

MK-1220	HBV HCV Protease	Infection
MK-1220 is a covalently reversible inhibitor of the hepatitis C virus (HCV) NS3/4A protease (NS3/4A protease) with a K_i of 0.02 nM. MK-1220 in cell models simulating viral replication exhibits EC₅₀s of 4 (with 10% fetal bovine serum) and 11 nM (50% normal human serum). MK-1220 can be used for the study of chronic hepatitis C virus infection .

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 .

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) .

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 (K_i= 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 . .

HY-178501

KRAS-IN-45	Ras	Cancer
KRAS-IN-45 (Compound 1.019) is a KRAS inhibitor. KRAS-IN-45 can be used for the study of cancers .

HY-178502

KRAS-IN-46	Ras	Cancer
KRAS-IN-46 (Compound 1.013) is a KRAS inhibitor. KRAS-IN-46 can be used for the study of cancers .

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 .

HY-161571

LRRK2-IN-13	LRRK2	Neurological Disease
LRRK2-IN-13 (Compound 13) is an inhibitor of LRRK2 (IC₅₀=0.57 nM). LRRK2-IN-13 has brain penetrating properties .

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 .

HY-17580R

Fidaxomicin (Standard) OPT-80 (Standard); PAR-101 (Standard)	Reference Standards 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 .

HY-P3143A

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

HY-N8280

IKD-8344	Fungal	Infection
IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties. It is cytotoxic to L5178Y murine leukemia cells (IC₅₀=0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC=6.25 μg/mL) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.

HY-153221

QR-6401	CDK	Cancer
QR-6401 is an orally active and selective macrocyclic CDK2 inhibitor with IC₅₀ values of 0.37, 10, 22, 34 and 45 nM for CDK2/E1, CDK9/T1, CDK1/A2, CDK6/D3 and CDK4/D1, respectively. QR-6401 has potent antitumor activity in an OVCAR3 ovarian cancer xenograft model. QR-6401 has the potential to be used in the study of cancer .

Cat. No.	Product Name

HY-L041

Macrocyclic Compound Library

448 compounds

Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity.

MCE offers a unique collection of 448 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.

HY-L0119V

Asinex PPI Pre-Plated Library

3,253 compounds

Protein protein interactions (PPI) have pivotal roles in life processes. The studies showed that aberrant PPI are associated with various diseases. However, the design of modulators targeting PPI still faces tremendous challenges, such the difficult PPI interfaces for the drug design, lack of ligands reference, lack of guidance rules for the PPI modulators development and high-resolution PPI proteins structures.

The PPI Library comprises molecules of various sizes, frameworks, and shapes ranging from fragment-like entities to macrocyclic derivatives designed as secondary structure mimetics or as epitope mimetics. The designs cover β-turn / loop mimetics and α-helix mimetics. Since helices present at the interface in 62% of all protein-protein interactions. This library focused on designs including mimics with the substitution geometry of an a-helices, as well as designs that mimic the location of “hot-spot” side chains in helix-mediated PPIs.

HY-L932V0

Kinase Macrocyclic Compound Virtual Library

2,000,000 compounds

Macrocyclic compounds (≥12-atom cyclic small molecules/peptides) have unique physicochemical properties. They form preorganized conformations with high binding affinity/selectivity, target traditional small-molecule-inaccessible proteins, and bridge small-molecule drugs and biological agents. As key protein phosphorylation enzymes, kinases are linked to tumors, COPD, etc., and are critical therapeutic targets. Traditional small-molecule kinase inhibitors lack selectivity, causing off-target toxicity, low bioavailability, and acquired resistance. Macrocycles’ semi-rigid structure restricts conformations, boosts binding selectivity, optimizes pharmacokinetics, and makes macrocyclization a core kinase inhibitor optimization strategy.

Thousands of bioactive macrocycles were curated from ChEMBL. Via Transformer, macrocyclization was converted into a chemical language translation task, enabling end-to-end macrocycle generation from linear precursors with simplified inputs. Macformer achieves efficient, automated linear molecule macrocyclization via deep learning; generated macrocycles have diversity, novelty, biocompatibility, and cover broader chemical space.

MCE collected thousands of marketed/clinical kinase inhibitors, using their fragments for macrocyclization to generate derivatives. After evaluating synthetic accessibility and physicochemical properties, a million-scale virtual macrocyclic library was built for kinase-related virtual and AI-driven screening.

HY-L932V

Kinase Macrocyclic Compound Virtual Library

2,000,000 compounds

Cat. No.	Product Name	Type

HY-W034566

Hexacyclen

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

Biochemical Assay Reagents

Hexacyclen is an organic compound with a unique macrocyclic structure composed of six nitrogen-containing rings. It is commonly used as a chelating agent in chemistry and biochemistry due to its ability to bind metal ions. Inhibitors of certain diseases such as cancer. In biochemistry, Hexacyclen is often used to selectively bind metal ions in proteins or enzymes to study their structure and function. Due to its large size and complex structure, Hexacyclen is not widely used in daily products or applications .

HY-W034576

Hexacyclen hexahydrochloride

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

Biochemical Assay Reagents

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 .

HY-W034566A

Hexacyclen trisulfate

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

Biochemical Assay Reagents

Hexacyclen, also known as cycloalkene, is an organic compound with a unique macrocyclic structure composed of six nitrogen-containing rings. It is commonly used as a chelating agent in chemistry and biochemistry due to its ability to bind metal ions. Inhibitors of certain diseases such as cancer. In biochemistry, Hexacyclen is often used to selectively bind metal ions in proteins or enzymes to study their structure and function. Due to its large size and complex structure, Hexacyclen is not widely used in daily products or applications.

Cat. No.	Product Name	Target	Research Area

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) .

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 .

HY-172320

BMS-986238	PD-1/PD-L1	Cancer
BMS-986238 is an orally active macrocyclic peptide PD-L1 inhibitor. BMS-986238 can be used in the research of tumors such as solid tumors and lymphomas .

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 K_ds 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 .

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 .

HY-P11020

p27 Analogue CP2	E1/E2/E3 Enzyme	Cancer
p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the Cks1-Skp2-Skp1 complex (K_d = 32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer .

HY-103048A

PD-1/PD-L1-IN 3 TFA	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN 3 TFA, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 TFA interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC₅₀s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 TFA can be used for the research of various diseases, including cancer and infectious diseases .

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

HY-173076A

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

HY-103048

PD-1/PD-L1-IN 3	PD-1/PD-L1	Cancer
PD-1/PD-L1-IN 3, a macrocyclic peptide, is a potent and selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions extracted from patent WO2014151634A1, compound No.1. PD-1/PD-L1-IN 3 interferes with PD-L1 binding to PD-1 and CD80 by binding to PD-L1, with IC₅₀s of 5.60 nM and 7.04 nM, respectively. PD-1/PD-L1-IN 3 can be used for the research of various diseases, including cancer and infectious diseases .

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) .

HY-P3143A

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

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.

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 .

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 K_i of 40 nM. HDAC11-IN-1 exhibits good cell permeability and can inhibit the expression of YAP1 and SOX2 .

HY-P10700

RO7196472	Antibiotic Bacterial	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 .

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 .

HY-P10477

CT-08	Peptides	Cancer
CT-08 (CT8, Compound 3) is a macrocyclic Sec61 modulator, blocks protein secretion in a signal sequence-dependent manner. CT-08 blocks Sec61-mediated translocation of VCAMss-GLuc into the ER, resulting in a loss of luciferase activity. CT-08 inhibits VCAM expression in transfected cells .

HY-149034

Influenza A virus-IN-8 S5	Influenza Virus	Infection Cancer
Influenza A virus-IN-8 (S5) is a macrocyclic peptide with no cytotoxic. Influenza A virus-IN-8 is also a potent Influenza A Virus (IAV) inhibitor (with sufficient protease stability) with IC₅₀s of 6.7 and 6.6 nM for H1 and H5 variants, respectively. Influenza A virus-IN-8 shows good affinitiescan to H1 variants, binds to a conserved region in the HA stem with a K_d of 1.0 nM .

HY-P10676

cMCF02A	Peptides	Cancer
cMCF02A is a potent inhibitory peptide of the MAGE-A4 binding axis and can be used in melanoma-related research .

HY-W1126955

Enlicitide (decanoate) MK-0616 (decanoate)	PCSK9	Metabolic Disease Inflammation/Immunology
Enlicitide (MK-0616) decanoate is an orally active macrocyclic peptide PCSK9 inhibitor. Enlicitide decanoate binds to PCSK9, blocks its interaction with low-density lipoprotein receptor (LDLR), and enhances hepatic clearance of LDL-C. Enlicitide decanoate reduces atherogenic lipoproteins, including non-HDL cholesterol, apolipoprotein B, and lipoprotein (a). Enlicitide decanoate is applicable to research related to hypercholesterolemia, heterozygous familial hypercholesterolemia, and atherosclerotic cardiovascular disease .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-13756

Tacrolimus Maximum Cited Publications 101 Publications Verification FK506; Fujimycin; FR900506	Infection Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Animals Classification of Application Fields Antibiotics Disease Research Inflammation/Immunology Disease Research Fields Source Classification	Phosphatase FKBP Bacterial Autophagy Antibiotic
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 .

HY-N0750

Monocrotaline 40+ Cited Publications Crotaline	Structural Classification Alkaloids Pyrrole Alkaloids Classification of Application Fields Leguminosae Crotalaria pallida Ait. Plants Disease Research Fields Cancer	Others
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].

HY-17580

Fidaxomicin 5+ Cited Publications OPT-80; PAR-101	Infection Structural Classification Microorganisms Macrolide Antibiotics Classification of Application Fields Antibiotics Phenols Polyphenols Antibacterial Disease Research Disease Research Fields Source Classification	DNA/RNA Synthesis Bacterial Apoptosis Antibiotic
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 .

HY-15739

Ansamitocin P-3 5+ Cited Publications Antibiotic C 15003P3; Maytansinol isobutyrate	Infection Microorganisms Classification of Application Fields Antibiotics Disease Research Anticancer Disease Research Fields Other Antibiotics Source Classification	Microtubule/Tubulin ADC Payload Bacterial Antibiotic
Ansamitocin P-3 (Antibiotic C 15003P3) is a microtubule inhibitor. Ansamitocin P-3 is a macrocyclic antitumor antibiotic.

HY-13756A

Tacrolimus monohydrate Maximum Cited Publications 101 Publications Verification FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate	Infection Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Classification of Application Fields Antibiotics Disease Research Inflammation/Immunology Disease Research Fields Source Classification	Phosphatase FKBP Autophagy Bacterial Antibiotic
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 .

HY-17566

Capreomycin sulfate 5 Publications Verification	Infection Microorganisms Classification of Application Fields Antibiotics Mammalian Cell Culture Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	Antibiotic Bacterial
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 .

HY-N7765

Oenothein B	Infection other families Classification of Application Fields Phenols Polyphenols Plants Inflammation/Immunology Disease Research Fields Source Classification	HCV Bacterial Apoptosis Fungal
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 .

HY-107486

Nosiheptide Multhiomycin; RP 9671	Infection Microorganisms Antibiotics Animal Husbandry Antibacterial Disease Research Disease Research Fields Other Antibiotics Source Classification	Bacterial Antibiotic
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 .

HY-13756R

Tacrolimus (Standard) FK506 (Standard); Fujimycin (Standard); FR900506 (Standard)	Structural Classification Microorganisms Anti-inflammation/Immunoregulatory Macrolide Antibiotics Animals Antibiotics Disease Research Source Classification	Reference Standards Phosphatase FKBP Bacterial Autophagy Antibiotic
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 .

HY-107486R

Nosiheptide (Standard) Multhiomycin (Standard); RP 9671 (Standard)	Structural Classification Microorganisms Antibiotics Animal Husbandry Antibacterial Disease Research Other Antibiotics Source Classification	Reference Standards Bacterial Antibiotic
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 .

HY-17580R

Fidaxomicin (Standard) OPT-80 (Standard); PAR-101 (Standard)	Structural Classification Microorganisms Macrolide Antibiotics Antibiotics Phenols Polyphenols Antibacterial Disease Research Source Classification	Reference Standards DNA/RNA Synthesis Bacterial Apoptosis Antibiotic
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 .

HY-15739R

Ansamitocin P-3 (Standard) Antibiotic C 15003P3 (Standard); Maytansinol isobutyrate (Standard)	Structural Classification Microorganisms Antibiotics Disease Research Anticancer Other Antibiotics Source Classification	Reference Standards Microtubule/Tubulin ADC Payload Bacterial Antibiotic
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.

HY-N0750R

Monocrotaline (Standard) Crotaline (Standard)	Structural Classification Alkaloids Pyrrole Alkaloids Leguminosae Crotalaria pallida Ait. Plants	Reference Standards Others
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. .

Cat. No.	Product Name	Chemical Structure

HY-13756S

Tacrolimus-13C,d2 1 Publications Verification
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 .

HY-17580S

Fidaxomicin-d7
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 .

HY-13756S2

Tacrolimus-d3
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 .

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