89346-82-7

Usage

Uses

Benzyl-PEG4-Ots is a PEG-based PROTAC linker that can be used to synthesize PROTACs.

in vitro

PROTAC contains two distinct ligands linked by a linker; one is a ligand for the E3 ubiquitin ligase and the other is a ligand for the target protein. PROTAC utilizes the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

Upstream product

• 112-60-7 Tetraethylene glycol 
• 86259-87-2 1-phenyl-2,5,8,11-tetraoxatridecan-13-ol 
• 4792-15-8 Pentaethylene glycol 
• 100-39-0 benzyl bromide 
• 98-59-9 p-toluenesulfonyl chloride 
• 111-77-3 2-(2-methoxyethoxy)ethyl alcohol 
• 100-44-7 benzyl chloride 

Downstream Products

• 129086-17-5 [2-(2-{2-[2-(2,2,3,3,4,4,5,5,6,6,7,7,8,8,8-Pentadecafluoro-octyloxy)-ethoxy]-ethoxy}-ethoxy)-ethoxymethyl]-benzene 
• 129086-20-0 [2-(2-{2-[2-(2,2,3,3,4,4,5,5,6,6,7,7-Dodecafluoro-heptyloxy)-ethoxy]-ethoxy}-ethoxy)-ethoxymethyl]-benzene 
• 129086-22-2 [2-(2-{2-[2-(2,2,3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,11,11-Icosafluoro-undecyloxy)-ethoxy]-ethoxy}-ethoxy)-ethoxymethyl]-benzene 
• 142723-25-9 2-(2-{2-[2-(2-Benzyloxy-ethoxy)-ethoxy]-ethoxy}-ethoxy)-5-decyl-benzoic acid methyl ester 
• 86770-71-0 ((2-(2-(2-(2-azidoethoxy)ethoxy)ethoxy)ethoxy)methyl)benzene 
• 134881-75-7 1,4-bis<2-<2-<2-<2-(benzyloxy)ethoxy>ethoxy>ethoxy>ethoxy>benzene 
• 1050202-41-9 octaethylene glycol benzyl trityl ether 
• 1144113-13-2 octaethylene glycol benzyl tert-butyl ether 
• 361543-06-8 C₄₀H₆₆O₁₄ 
• 17598-96-8 poly(ethylene glycol) 600 
• 477775-73-8 1-phenyl-2,5,8,11,14,17,20,23-octaoxapenta-cosan-25-ol 
• 89346-73-6 2-<2-<2-<2-<(diazonium tetrafluoroborate)benzoyloxy>ethoxy>ethoxy>ethoxy>ethoxybenzene 
• 89346-84-9 2-<2-<2-<2-(nitrobenzoyloxy)ethoxy>ethoxy>ethoxy>ethoxybenzene 

Relevant academic research and scientific papers

TARGET PROTEIN EED DEGRADATION-INDUCING DEGRADUCER, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING DISEASES RELATED TO EED, EZH2, OR PRC2, COMPRISING SAME AS ACTIVE INGREDIENT

The present invention relates to a target protein degradation-inducing Degraducer, a preparation method thereof, and a pharmaceutical composition for preventing or treating diseases related to EED, EZH2, or PRC2 comprising same as an active ingredient. A novel compound represented by formula 1, according to the present invention is a Degraducer compound that induces degradation of a target protein, i.e., embryonic ectoderm development (EED) or polycomb repressive complex 2 (PRC2), utilizing cereblon E3 ubiquitin ligase, von Hippel-Lindau tumor suppressor (VHL) E3 ubiquitin ligase, mouse double minute 2 homolog (MDM2) E3 ubiquitin ligase, and cellular inhibitor of apoptosis protein 1 (cIAP) E3 ubiquitin ligase, wherein the compound has an aspect of remarkably achieving target protein degradation-inducing activity through a ubiquitin proteasome system (UPS), and therefore there is a useful effect in that it is possible to provide a pharmaceutical composition for preventing or treating diseases or conditions related to a target protein, and a functional health food composition for preventing or improving same, comprising said compound as an active ingredient.

SMALL-MOLECULE INHIBITORS FOR THE Β-CATENIN/B-CELL LYMPHOMA 9 PROTEIN?PROTEIN INTERACTION

Disclosed are inhibitors for the β-catenin/B-cell lymphoma 9 interaction. The inhibitors are selective for β-catenin/B-cell lymphoma 9 over β-catenin/ E-cadherin PPI interaction. Methods of using the disclosed compounds to treat cancer are also disclosed.

Effects of 18F-fluorinated neopentyl glycol side-chain on the biological characteristics of stilbene amyloid-β PET ligands

Introduction: The 2,2-dihydroxymethyl-1-[18F]fluoropropane group, also called 18F-labelled neopentyl glycol side-chain, is a novel 18F-labelling group for positron emission tomography (PET) imaging agents. The aim of using this group is to develop simple purification with solid-phase extraction without high-performance liquid chromatography. However, the effects of the neopentyl 18F-labelling group on the characteristics of brain imaging agents are unknown. Here, we added this side-chain to compounds with an aminostilbene structure to evaluate their effects on the biological properties of aminostilbene as an amyloid-β (Aβ) radioligand. Methods: Biodistributions of four novel 18F-labelled stilbene compounds with different lengths of polyethylene glycol (PEG) linkers, called [18F]Cpd-0, -1, -2, and -4, (PEG = 0, 1, 2, and 4), and [18F]AV-1 in normal mice were evaluated. Metabolite analysis of [18F]Cpd-0 and -1 was performed with mouse plasma and brain. A competitive binding assay of [18F]AV-1 binding to Aβ1–42 fibrils was performed to determine the binding properties of the compounds. Results: [18F]Cpd-0, -1, and -2 demonstrated moderate initial brain uptake in mice (3.1–4.2% injected dose/g at 2 min post-injection) followed by fast clearance, and in vivo defluorination of these compounds was negligible. [18F]Cpd-4 exhibited low brain uptake and high bone uptake. Compared with [18F]Cpd-1, the percentage of [18F]Cpd-0 in mouse brain was high at 10 min post-injection. A competitive binding assay revealed partial interference effects by the neopentyl glycol side-chain on binding of stilbene compounds to Aβ1–42 fibrils. Conclusions: Aminostilbene compounds with two or fewer PEG linkers containing an 18F-labelled neopentyl glycol side-chain demonstrated preferable pharmacokinetic properties as a brain imaging radioligand in normal mice. These side-chains can be used as an alternative labelling group for imaging agents targeting the brain.

HETEROCYCLIC COMPOUND

One of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity. Another of the purposes of the present invention is to provide a heterocyclic derivative that has an IAP (particularly XIAP) binding (inhibiting) activity and exhibits a protein degradation induction activity. The present invention provides a compound represented by formula (I) (the symbols in the formula are as defined in the present Description) and salts thereof.

Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction

The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.

CALCIUM OXALATE CRYSTALLIZATION INHIBITORS FOR RENAL DISORDERS

The present invention relates to inositol derivatives comprising two or more cyclohexanolpentakisester moieties linked by a common central linker and their use in therapy or prevention of a condition related to pathological crystallization. The invention

Templated Formation of Luminescent Virus-like Particles by Tailor-Made Pt(II) Amphiphiles

Virus-like particles (VLPs) have been created from luminescent Pt(II) complex amphiphiles, able to form supramolecular structures in water solutions, that can be encapsulated or act as templates of cowpea chlorotic mottle virus capsid proteins. By virtue

TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE

The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.

Solid Phase Stepwise Synthesis of Polyethylene Glycols

Polyethylene glycol (PEG) and derivatives with eight and twelve ethylene glycol units were synthesized by stepwise addition of tetraethylene glycol monomers on a polystyrene solid support. The monomer contains a tosyl group at one end and a dimethoxytrityl group at the other. The Wang resin, which contains the 4-benzyloxy benzyl alcohol function, was used as the support. The synthetic cycle consists of deprotonation, Williamson ether formation (coupling), and detritylation. Cleavage of PEGs from solid support was achieved with trifluoroacetic acid. The synthesis including monomer synthesis was entirely chromatography-free. PEG products including those with different functionalities at the two termini were obtained in high yields. The products were analyzed with ESI and MALDI-TOF MS and were found close to monodispersity.

Precursor for preparing micelle

The present invention refers to linker, polar material and two aliphatic hydrocarbon chain comprised of precursor for micellar formation, said precursor manufacturing method, including micelles and including said precursor of said micelle relates to drug delivery. In the present invention number the use of precursor for forming micelle under public affairs, two game machine included in same, non-polar tail due to, than micelles of the existing method a relatively high stability of the insertion part and the holder under trillion number micelle, micelles including drug delivery or the like and can be widely used for the development of.. (by machine translation)