956348-61-1

Usage

Uses

Used in Bioconjugation:
Alkyne-PEGn-NH2 2K, 5K, 10K, 20K is used as a bioconjugation agent for the attachment of biomolecules to other molecules or surfaces. The propargyl group reacts with azide-containing biomolecules through click chemistry, while the amine group can be used to form amide bonds with carboxylic acid-containing molecules.
Used in Drug Delivery Systems:
In the pharmaceutical industry, Alkyne-PEGn-NH2 2K, 5K, 10K, 20K is used as a component in drug delivery systems to improve the solubility, stability, and bioavailability of drugs. The PEG units provide hydrophilicity, and the amine group can be used to attach drug molecules through amide bonds.
Used in Diagnostic Imaging:
In the medical imaging industry, Alkyne-PEGn-NH2 2K, 5K, 10K, 20K is used as a contrast agent or a component in the development of imaging probes. The propargyl group can be used to attach imaging agents, such as fluorescent dyes or radionuclides, through click chemistry, while the amine group can be used to attach targeting moieties.
Used in Material Science:
In the material science industry, Alkyne-PEGn-NH2 2K, 5K, 10K, 20K is used as a building block for the synthesis of functional polymers and materials. The propargyl group and amine group can be used to create a variety of polymer architectures, while the PEG units provide hydrophilicity and tunable properties.

Upstream product

• 932741-18-9 3-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)-prop-1-yne 
• 5197-62-6 2-[2-(chloroethoxy)ethoxy]ethanol 
• 86520-52-7 2-[2-(2-azidoethoxy)ethoxy]ethanol 
• 75001-08-0 2-{2-[2-(2-hydroxyethoxy)ethoxy]ethyl}isoindole-1,3-dione 
• 1408059-52-8 2-(2-(2-(2-(prop-2-yn-1-yloxy)ethoxy)ethoxy)ethyl)isoindoline-1,3-dione 
• 112-27-6 2,2'-[1,2-ethanediylbis(oxy)]bisethanol 
• 77544-68-4 8-tosyloxy-3,6-dioxaoctanol 
• 208827-90-1 O-propargyl triethylene glycol 
• 139115-92-7 tert-butyl 2-(2-(2-hydroxyethoxy)ethoxy)ethylcarbamate 
• 1333880-60-6 tert-butyl (2-(2-(2-(prop-2-yn-1-yloxy)ethoxy)ethoxy)ethyl)carbamate 
• 6338-55-2 2-(2-(2-aminoethoxy)ethoxy)ethan-1-ol 
• 888009-94-7 2-[2-(2-(prop-2-yn-1-yloxy)ethoxy)ethoxy]ethyl 4-methylbenzene-1-sulfonate 
• 430430-57-2 2,2-dimethyl-4-oxo-3,8,11-trioxa-5-azatridecane-13-yl methanesulfonate 
• 1013921-33-9 N-(3,6,9,12-tetraoxapentadec-14-ynyl)-4,5,6,7-tetrachloroisoindoline-1,3-dione 

Downstream Products

• 1245285-73-7 C₂₈H₃₄N₈O₈ 
• 1609374-67-5 2-(6-(diethylamino)-3-(diethyliminio)-3H-xanthen-9-yl)-5-(N-(2-(2-(2-(prop-2-yn-1-yl oxy)ethoxy)ethoxy)ethyl)sulfamoyl)benzenesulfonate 
• 1219810-90-8 tert-butyl N-[2-[2-[2-(2-prop-2-ynoxyethoxy)ethoxy]ethoxy]ethyl]carbamate 

Relevant academic research and scientific papers

Facial Synthesis and Bioevaluation of Well‐Defined OEGylated Betulinic Acid‐Cyclodextrin Conjugates for Inhibition of Influenza Infection

Betulinic acid (BA) and its derivatives exhibit a variety of biological activities, especially their anti‐HIV‐1 activity, but generally have only modest inhibitory potency against influenza virus. The entry of influenza virus into host cells can be competitively inhibited by multivalent derivatives targeting hemagglutinin. In this study, a series of hexa‐, hepta‐ and octavalent BA derivatives based on α-, β-and γ-cyclodextrin scaffolds, respectively, with varying lengths of flexible oligo(ethylene glycol) linkers was designed and synthesized using a microwave‐assisted copper‐catalyzed 1,3‐di-polar cycloaddition reaction. The generated BA‐cyclodextrin conjugates were tested for their in vitro activity against influenza A/WSN/33 (H1N1) virus and cytotoxicity. Among the tested com-pounds, 58, 80 and 82 showed slight cytotoxicity to Madin‐Darby canine kidney cells with viabilities ranging from 64 to 68% at a high concentration of 100 μM. Four conjugates 51 and 69–71 showed significant inhibitory effects on influenza infection with half maximal inhibitory concentration val-ues of 5.20, 9.82, 7.48 and 7.59 μM, respectively. The structure‐activity relationships of multivalent BA‐cyclodextrin conjugates were discussed, highlighting that multivalent BA derivatives may be potential antiviral agents against influenza infection.

COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION

The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.

HETEROCYCLIC DERIVATIVES

Compounds of the formula (I): Q1-Q2-Q3, in which Q1, Q2 and Q3 have the meanings indicated in Claim 1, degrade target proteins, and can be employed, inter alia, for the treatment of diseases such as cancer, multiple sclerosis, cardiovascular diseases, central nervous system injury and different forms of inflammation.

ANTIBODY COMPOUNDS WITH REACTIVE ARGININE AND RELATED ANTIBODY DRUG CONJUGATES

The present invention provides antibody compounds that contain a substitution of arginine for the reactive lysine residue (Lys99) in the hydrophobic cleft (38C2_Arg). The invention also provides antibody drug conjugate compounds (ADCs) that contain cargo

Disulfide dimannose-gold nanoprobe as well as preparation method and application thereof

The invention belongs to the field of carbohydrate chemistry biology, and particularly relates to a disulfide dimannose-gold nanoprobe, a preparation method and application of the disulfide dimannose-gold nanoprobe in the aspect of virus receptor DC-SIGN/R recognition. The disulfide dimannose-gold nanoprobe is characterized in that a ligand exchange method is adopted, and disulfide dimannose ligands are modified on the surfaces of gold nanoparticles. The method is based on click chemistry and ligand exchange, modifies the surface of the gold nanoparticle with a mannose ligand to construct a novel dithiodimannose-gold nanoprobe, a sugar binding mechanism of tetramer lectin DC-SIGN and DC-SIGNR is researched on the basis of a fluorescence quenching strategy, and a foundation is laid for establishing a rapid and sensitive method and researching binding affinity and thermodynamics between protein-sugar multivalent interactions.

Glycan-Gold Nanoparticles as Multifunctional Probes for Multivalent Lectin-Carbohydrate Binding: Implications for Blocking Virus Infection and Nanoparticle Assembly

Multivalent lectin-glycan interactions are widespread in biology and are often exploited by pathogens to bind and infect host cells. Glycoconjugates can block such interactions and thereby prevent infection. The inhibition potency strongly depends on matching the spatial arrangement between the multivalent binding partners. However, the structural details of some key lectins remain unknown and different lectins may exhibit overlapping glycan specificity. This makes it difficult to design a glycoconjugate that can potently and specifically target a particular multimeric lectin for therapeutic interventions, especially under the challenging in vivo conditions. Conventional techniques such as surface plasmon resonance (SPR) and isothermal titration calorimetry (ITC) can provide quantitative binding thermodynamics and kinetics. However, they cannot reveal key structural information, e.g., lectin's binding site orientation, binding mode, and interbinding site spacing, which are critical to design specific multivalent inhibitors. Herein we report that gold nanoparticles (GNPs) displaying a dense layer of simple glycans are powerful mechanistic probes for multivalent lectin-glycan interactions. They can not only quantify the GNP-glycan-lectin binding affinities via a new fluorescence quenching method, but also reveal drastically different affinity enhancing mechanisms between two closely related tetrameric lectins, DC-SIGN (simultaneous binding to one GNP) and DC-SIGNR (intercross-linking with multiple GNPs), via a combined hydrodynamic size and electron microscopy analysis. Moreover, a new term, potential of assembly formation (PAF), has been proposed to successfully predict the assembly outcomes based on the binding mode between GNP-glycans and lectins. Finally, the GNP-glycans can potently and completely inhibit DC-SIGN-mediated augmentation of Ebola virus glycoprotein-driven cell entry (with IC50 values down to 95 pM), but only partially block DC-SIGNR-mediated virus infection. Our results suggest that the ability of a glycoconjugate to simultaneously block all binding sites of a target lectin is key to robust inhibition of viral infection.

PYRROLOBENZODIAZEPINE DIMER PRECURSOR AND LIGAND-LINKER CONJUGATE COMPOUND THEREOF

The present invention relates to a pyrrolobenzodiazepine dimer prodrug and a ligand-linker conjugate compound thereof, a composition containing these, and therapeutic use thereof particularly as an anticancer drug. The stability of the compounds themselves and the stability thereof in plasma are excellent and the compounds are advantageous in terms of manifestation of toxicity, and thus the compounds are industrially useful in that it is possible to target proliferative diseases such as cancer, to perform a specific treatment, to maximize the drug efficacy, and to minimize the occurrence of side effects.

A multimeric MRI contrast agent based on a: Closo -borane scaffold bearing modified AAZTA chelates on the periphery

A multimeric MRI contrast agent based on the closo-borane motif is reported. Twelve copies of a modified AAZTA chelate with an alkyne end group are appended on an azide-functionalized closo-borane motif using Cu(i) catalyzed click chemistry. The presence of two water molecules on the Gd-bound AAZTA chelate results in high relaxivity for the closomer in vitro/in vivo.

A MedChem toolbox for cereblon-directed PROTACs

A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.