Coumarin-C2-exoBCN is a dye derivative of Coumarin (HY-N0709). Coumarin-C2-exoBCN contains the lyophilic bidentate macrocyclic ligand exo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to generate stable triazoles under catalyst-free conditions.
Cy3-PEG2-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 2 PEG units. Cy3-PEG2-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy5-PEG7-exo-BCN is a dye derivative of Cyanine 5 (Cy5) (HY-D0821) containing 7 PEG units. Cy5-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Verrucarin A (Muconomycin A) 是一种 D 型大环真菌毒素,来源于Myrothecium verrucaria,是一种蛋白质合成 (protein synthesis) 的抑制剂。Verrucarin A 抑制白血病细胞系生长,激活巨噬细胞 caspases、凋亡和炎症信号。Verrucarin A 能有效提高 p38 MAPK 的磷酸化,降低 ERK/Akt 的磷酸化。Verrucarin A 通过 p21 和 p53 的诱导引起细胞周期调控的解除。
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.
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.
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.
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.
Coumarin-C2-exoBCN is a dye derivative of Coumarin (HY-N0709). Coumarin-C2-exoBCN contains the lyophilic bidentate macrocyclic ligand exo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to generate stable triazoles under catalyst-free conditions.
Cy3-PEG2-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 2 PEG units. Cy3-PEG2-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy5-PEG7-exo-BCN is a dye derivative of Cyanine 5 (Cy5) (HY-D0821) containing 7 PEG units. Cy5-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Coumarin-C2-exoBCN is a dye derivative of Coumarin (HY-N0709). Coumarin-C2-exoBCN contains the lyophilic bidentate macrocyclic ligand exo-BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to generate stable triazoles under catalyst-free conditions.
Cy3-PEG2-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 2 PEG units. Cy3-PEG2-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG3-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 3 PEG units. Cy3-PEG3-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-endo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-endo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, endo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy3-PEG7-exo-BCN is a dye derivative of Cyanine 3 (Cy3) (HY-D0822) containing 7 PEG units. Cy3-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.
Cy5-PEG7-exo-BCN is a dye derivative of Cyanine 5 (Cy5) (HY-D0821) containing 7 PEG units. Cy5-PEG7-exo-BCN contains the lyophilic bidentate macrocyclic ligand BCN, which can further synthesize macrocyclic complexes. In click chemistry, exo-BCN can react with molecules containing azide groups to form stable triazoles in the absence of catalysts.