287174-32-7

Usage

Uses

Used in Bioconjugation and Drug Delivery:
Hydroxy-PEG1-CH2CO2tBu serves as a versatile linker in bioconjugation processes, where it can be used to attach biologically active molecules, such as peptides, proteins, or nucleic acids, to other molecules or surfaces. The hydroxyl group facilitates these attachments, while the PEG spacer provides steric stabilization and improved solubility.
Used in Chemical Synthesis:
In chemical synthesis, Hydroxy-PEG1-CH2CO2tBu can be employed as an intermediate to produce a variety of PEGylated compounds. The t-butyl protected carboxyl group allows for selective deprotection, enabling the introduction of different functional groups or the formation of specific chemical bonds.
Used in Pharmaceutical Formulation:
Hydroxy-PEG1-CH2CO2tBu can be utilized in the formulation of pharmaceuticals to improve the solubility and stability of drug molecules. The PEG spacer can also provide a means to control the release of the drug, potentially enhancing the therapeutic efficacy and reducing side effects.
Used in Material Science:
In the field of material science, Hydroxy-PEG1-CH2CO2tBu can be incorporated into the design of hydrogels, polymers, or other materials to enhance their properties, such as biocompatibility, water solubility, and mechanical strength.
Used in Diagnostics:
Hydroxy-PEG1-CH2CO2tBu can be employed in the development of diagnostic tools, where it can be used to modify the surface of sensors or to create PEGylated contrast agents for imaging techniques, improving their performance and reducing non-specific interactions.
Overall, Hydroxy-PEG1-CH2CO2tBu is a multifunctional molecule with applications across various industries, including pharmaceuticals, diagnostics, material science, and chemical synthesis, due to its unique combination of properties and functional groups.

Upstream product

• 5292-43-3 bromoacetic acid tert-butyl ester 
• 107-21-1 ethylene glycol 
• 35059-50-8 t-butyl diazoacetate 
• 1309451-06-6 2-(2-(benzyloxy)ethoxy)acetic acid tert-butyl ester 

Downstream Products

• 287174-35-0 {2-[(1-azido-2-phenyl-ethyl)-(4-methanesulfonyl-benzyloxy)-phosphinoyloxy]-ethoxy}-acetic acid tert-butyl ester 
• 2100306-71-4 tert-butyl 2-(2-(2-(2-bromoethoxy)ethoxy)ethoxy)acetate 
• 1820717-35-8 2-azidoethoxyacetic acid tert-butyl ester 
• 1155811-37-2 tert-butyl 2-(2-aminoethoxy)acetate 
• 1643957-24-7 tert-butyl 2-(2-[[(4-methylbenzene)sulfonyl]oxy]ethoxy)acetate 

Relevant academic research and scientific papers

Oseltamivir PROTAC compound as well as preparation method and application thereof in anti-influenza virus medicines

The invention discloses an oseltamivir PROTAC compound as well as a preparation method and application thereof in anti-influenza virus medicines, and belongs to the technical field of medicines. The oseltamivir PROTAC compound is shown as a general formula (I) or (II), and in the general formula, E3 ligase is a VHL or CRBN ligand, and Linker is a linking group. The compound provided by the invention can effectively degrade influenza virus neuraminidase so as to exert the activity of inhibiting influenza virus replication, not only has inhibitory activity on wild influenza viruses, but also hasa very good inhibitory effect on oseltamivir drug-resistant strains, and has low toxicity to cells. The compound or the pharmacologically or physiologically acceptable salt thereof can be used for preparing anti-influenza virus medicines.

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Traditional EZH2 inhibitors are developed to suppress the enzymatic methylation activity, and they may have therapeutic limitations due to the nonenzymatic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation. Two best degraders, YM181 and YM281, induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.

Protein degradation targeting chimera for degrading androgen receptor

The invention relates to a novel difunctional molecule compound based on VHL ligand induction and application of the difunctional molecule compound in synthesis of the compounds and pharmaceutical compositions thereof. The compound is shown as a formula I. The compound can selectively induce AR protein degradation and can be used for treating cancers such as prostatic cancer and breast cancer.

DNA POLYMERASE IIIC INHIBITORS AND USE THEREOF

The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.

BIFUNCTIONAL SUBSTITUED PYRIMIDINES AS MODULATORS OF FAK PROTEOLYSE

The present disclosure relates to bifunctional compounds, which find utility as modulators of focal adhesion kinase (FAK) or protein tyrosine kinase 2 (PTK2). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

Protection of all cleavable sites of DNA with the multiple CGCG or continuous CGG sites from the restriction enzyme, indicative of simultaneous binding of small ligands

The anthracenone ligands (1–12) with a keto-phenol and a hydroxamic acid unit were synthesized and evaluated by a restriction enzyme inhibition assay. DNA substrates composed of multiple CGCG or CGG sites are fully hydrolyzed by a restriction enzyme that is selective for each sequence. Under such conditions, the full-length DNA substrate remains only when the ligand binds to all binding sites and protects it from hydrolysis by the restriction enzymes. In the assay using AccII and the 50-mer DNA substrates containing a different number of CGCG sites at different non-binding AT base pair intervals, the more the CGCG sites, the more the full-length DNA increased. Namely, simultaneous binding of the ligand (5) to the CGCG sites increased in the order of (CGCG)5>(CGCG)2>(CGCG)1. Furthermore, the length of the spacer of the hydroxamic acid to the anthracenone skeleton played an important role in the preference for the number of the d(A/T) base pairs between the CGCG sites. The long spacer-ligand (5) showed a preference to the CGCG sites with five AT pairs, and the short spacer-ligand (10) to that with two AT pairs. The ligand (12) with the shortest spacer showed a preference in simultaneous binding to the 54-mer DNA composed of 16 continuous CGG sites in the assay using the restriction enzyme Fnu4HI that hydrolyzes the d(GCGGC)/d(CGCCG) site. Application of these ligands to biological systems including the repeat DNA sequence should be of significant interest.

POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES

The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.

Compound for targeted ubiquitination degradation of ERRalpha protein and pharmaceutical composition and application thereof

The invention provides a compound with a structure shown as a formula (I), which has the effects of inhibiting ERRalpha protein activity and degrading ERRalpha protein activity, has relatively strongsubtype selectivity and can also effectively inhibit tri

METHODS OF SYNTHESIZING LABELED NUCLEOSIDES

Disclosed herein, inter alia, are compounds, compositions, and methods of synthesizing labeled nucleosides.

COMPOUNDS, COMPOSITIONS AND METHODS

The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.