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Results for "

Macrocycle

" in MedChemExpress (MCE) Product Catalog:

By Targets:	ADC Linker (2) Adenosine Receptor (1) CDK (1) HCV (2) LRRK2 (1) MDM-2/p53 (1) Radionuclide-Drug Conjugates (RDCs) (1) STING (2)
By Research Areas:	Cancer (6) Infection (2) Inflammation/Immunology (1) Neurological Disease (2)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Click Chemistry

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111999A

E7766 diammonium salt 1 Publications Verification	STING	Cancer
E7766 diammonium salt is a macrocycle-bridged STING agonist with a K_d of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities .

HY-100138

2-Aminoethyl-mono-amide-DOTA-tris(tBu ester)	Radionuclide-Drug Conjugates (RDCs) ADC Linker	Cancer
2-Aminoethyl-mono-amide-DOTA-tris(tBu ester) is a macrocycle DOTA derivative for tumor pretargeting .

HY-P4210

Sulanemadlin ALRN-6924; MP-4897	MDM-2/p53	Cancer
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .

HY-15591A

TMC647055 Choline salt 1 Publications Verification	HCV	Infection
TMC647055 (Choline salt) is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 Choline salt has potent HCV combine activity with an IC₅₀ value of 82 nM. TMC647055 Choline salt can be used for the research of Hepatitis C virus (HCV) .

HY-111999B

E7766 disodium	STING	Cancer
E7766 disodium is a macrocycle-bridged STING agonist with a K_d of 40 nM. E7766 disodium shows potent pan-genotypic and antitumor activities .

HY-146152

ASGPR modulator-1	Others	Others
ASGPR modulator-1 (Compound 5TJX) is a macrocycle compound that can be uesd for protein-protein interaction study .

HY-155184

A3AR agonist 2	Adenosine Receptor	Neurological Disease Inflammation/Immunology Cancer
A3AR agonist 2 (Compound 19) a selective A3AR agonist (K_i: 22.1 nM). A3AR agonist 2 stimulates β-arrestin2 recruitment, with EC₅₀ value of 4.36 nM. A3AR agonist 2 can be used for research of inflammatory diseases, ischemia, cancer, neuropathic pain, liver diseases, and other chronic conditions . A3AR agonist 2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-15591

TMC647055	HCV	Infection
TMC647055 is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 has potent HCV combine activity with an IC₅₀ value of 82 nM. TMC647055 can be used for the research of Hepatitis C virus (HCV) .

HY-161463

CDK2-IN-28	CDK	Cancer
CDK2-IN-28 (compound 22) is a CDK2 inhibitor with good selectivity and cellular effects against other CDKs. CDK2-IN-28 has anti-proliferative effects on MKN1 cells (EC50: 0.31 μM) .

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-151738

Fmoc-Aeg(N3)-OH	ADC Linker	Others
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

Cat. No.	Product Name

HY-L0116V

Asinex Macrocycles for RNA Library	1,065 compounds
Macrocycles are promising scaffolds for the design of novel RNA targeting molecules. This collection of macrocycles for RNA consists of very diverse, drug-like molecules which incorporate certain known RNA-recognition elements (e.g. nucleobase ring systems and analogs) distributed within macrocyclic rings or peripheral fragments. As macrocyclic molecules tend to be larger than traditional screening molecules, it is vital to carefully assess and control their physicochemical properties. All macrocycles have been tested for aqueous and DMSO solubility with cutoffs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4); PAMPA permeability has also been tested for representative set of macrocycles.

Asinex Macrocycles for RNA Library

1,065 compounds

Macrocycles are promising scaffolds for the design of novel RNA targeting molecules. This collection of macrocycles for RNA consists of very diverse, drug-like molecules which incorporate certain known RNA-recognition elements (e.g. nucleobase ring systems and analogs) distributed within macrocyclic rings or peripheral fragments. As macrocyclic molecules tend to be larger than traditional screening molecules, it is vital to carefully assess and control their physicochemical properties. All macrocycles have been tested for aqueous and DMSO solubility with cutoffs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4); PAMPA permeability has also been tested for representative set of macrocycles.

HY-L0115V

Asinex Macrocycles Library	10,091 compounds
ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks. Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.

Asinex Macrocycles Library

10,091 compounds

ASINEX has elaborated a library of diverse macrocycles using an effective tool box of synthetic methods. The resulting scaffolds are novel, tremendously diverse, medchem-relevant, macrocyclic frameworks.

Macrocyles tend to be larger than traditional screening molecules which make them perfect discovery tools for targets with shallow or extended binding sites. At the same time, their unique character based on restricted flexibility and ability to form intra-molecular hydrogen bonds allows for design approaches effectively optimizing properties such asaqueous solubility and membrane permeability. Many of these macrocycles have been tested for aqueous and DMSO solubility with cut-offs applied at 10 mM in DMSO and 50 µM in PBS (pH 7.4) followed by PAMPA permeability assay.

HY-L0118V

Asinex Covalent Inhibitors Library	942 compounds
A unique set of molecules containing mild electrophilic moieties that covalently interact with amino acid residues in the target protein. The diversity of our compounds for covalent drug discovery ranges from natural product-like scaffolds to macrocycles, creating multiple opportunities in hit generation for a selected target.

HY-L041

Macrocyclic Compound Library	385 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 385 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.

Macrocyclic Compound Library

385 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 385 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-L0122V

Asinex CNS Macrocycles Library	1,122 compounds
Several CNS multi-parameter scoring approaches have been reported: CNS-MPO, CNS-MPO V.2, CNS-TEMPO, which suggesting an algorithm to predict CNS-ike properties of new chemical entities. We have applied these scoring algorithms to select macrocycles satisfying multiple cut-offs and structural desirability criteria. The resulting set consists of 1,122 macrocyclic compounds with CNS-MPO > 4, CNS-MPO.v2 > 4, and CNS-TEMPO < 4 for CNS-related drug discovery and research.

Asinex CNS Macrocycles Library

1,122 compounds

Several CNS multi-parameter scoring approaches have been reported: CNS-MPO, CNS-MPO V.2, CNS-TEMPO, which suggesting an algorithm to predict CNS-ike properties of new chemical entities. We have applied these scoring algorithms to select macrocycles satisfying multiple cut-offs and structural desirability criteria. The resulting set consists of 1,122 macrocyclic compounds with CNS-MPO > 4, CNS-MPO.v2 > 4, and CNS-TEMPO < 4 for CNS-related drug discovery and research.

HY-L0117V

Asinex Macrocycles for Glycomimetics Library	1,412 compounds
Glycomimetics are designed to mimic the structure of natural carbohydrates and modulate their disease-related functions. Macrocyclic glycomimetics are an extremely interesting class of glycomimetics as they occupy space between small and macro molecules. Macrocyclic glycomimetics are mostly represented by naturally occurring molecules derived from marine microorganisms and bacterial or fungal metabolites.

Asinex Macrocycles for Glycomimetics Library

1,412 compounds

Glycomimetics are designed to mimic the structure of natural carbohydrates and modulate their disease-related functions. Macrocyclic glycomimetics are an extremely interesting class of glycomimetics as they occupy space between small and macro molecules. Macrocyclic glycomimetics are mostly represented by naturally occurring molecules derived from marine microorganisms and bacterial or fungal metabolites.

Cat. No.	Product Name	Target	Research Area

HY-P4210

Sulanemadlin ALRN-6924; MP-4897	MDM-2/p53	Cancer
Sulanemadlin (ALRN-6924) is a potent and cell-permeating p53-based peptidomimetic macrocycles. Sulanemadlin is a inhibitor of the p53-MDM2, p53-MDMX, or both p53 and MDM2 and MDMX protein-protein interactions. Sulanemadlin can be used for cancers research .

HY-P3566

(D-Lys16)-ACTH (1-24) (human, bovine, mouse, ovine, porcine, rabbit, rat)	Peptides	Others
(D-Lys16)-ACTH (1-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the reaction product with gadolinium tetraazacyclododecanetriacetate derivative. (D-Lys16)-ACTH (1-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) involves in preparation of tetraazacyclododecane macrocycle metal complexes for production of conjugates with biomolecules and for use as NMR contrast agents, radiodiagnostic agents and for radioresearch .

Cat. No.	Product Name		Classification

HY-151738

Fmoc-Aeg(N3)-OH		Azide
Fmoc-Aeg(N3)-OH is a click chemistry reagent containing an Azide. Alkylating the Nitrogen of an amide bond results in peptoid structures, which leads to conformational restrains, like N-methylation and allows backbone derivatisation. Altering cytotoxicity, bacterial cell selectivity and receptor pharmacology through formation of peptoid derivatives have been published for Cilengitide, Piscidin 1, and MC3, MC4 and MC5 receptor agonist. This building block enables design of macrocycles through intermolecular crosslinking or backbone stabilization through intermolecular ring-closure. This compound is a potential building block for the construction of (customized) peptide nucleic acids (PNAs) and for peptoid synthesis . Fmoc-Aeg(N3)-OH is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

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