Category: 139115-91-6

《Macropinocytosis as a key determinant of peptidomimetic uptake in cancer cells》 was written by Yoo, Daniel Y.; Barros, Stephanie A.; Brown, Gordon C.; Rabot, Christian; Bar-Sagi, Dafna; Arora, Paramjit S.. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate And the article was included in Journal of the American Chemical Society in 2020. The article conveys some information:

Peptides and peptidomimetics represent the middle space between small mols. and large proteins-they retain the relatively small size and synthetic accessibility of small mols. while providing high binding specificity for biomol. partners typically observed with proteins. During the course of our efforts to target intracellular protein-protein interactions in cancer, we observed that the cellular uptake of peptides is critically determined by the cell line-specifically, we noted that peptides show better uptake in cancer cells with enhanced macropinocytic indexes. Here, we describe the results of our anal. of cellular penetration by different classes of conformationally stabilized peptides. We tested the uptake of linear peptides, peptide macrocycles, stabilized helixes, β-hairpin peptides, and cross-linked helix dimers in 11 different cell lines. Efficient uptake of these conformationally defined constructs directly correlated with the macropinocytic activity of each cell line: high uptake of compounds was observed in cells with mutations in certain signaling pathways. Significantly, the study shows that constrained peptides follow the same uptake mechanism as proteins in macropinocytic cells, but unlike proteins, peptide mimics can be readily designed to resist denaturation and proteolytic degradation Our findings expand the current understanding of cellular uptake in cancer cells by designed peptidomimetics and suggest that cancer cells with certain mutations are suitable mediums for the study of biol. pathways with peptide leads. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2018,Rubner, Stefan; Scharow, Andrej; Schubert, Sabine; Berg, Thorsten published 《Selective Degradation of Polo-like Kinase 1 by a Hydrophobically Tagged Inhibitor of the Polo-Box Domain》.Angewandte Chemie, International Edition published the findings.Product Details of 139115-91-6 The information in the text is summarized as follows:

Hydrophobic tagging (HT) of bioactive compounds can induce target degradation via the proteasomal pathway. The first application of hydrophobic tagging to an existing inhibitor of protein-protein interactions is now presented. We developed Poloxin-2HT by fusing an adamantyl tag to Poloxin-2, an inhibitor of the polo-box domain (PBD) of the protein kinase Plk1, which is a target for tumor therapy. Poloxin-2HT selectively reduced the protein levels of Plk1 in HeLa cells and had a significantly stronger effect on cell viability and the induction of apoptosis than the untagged PBD inhibitor Poloxin-2. The change in cellular phenotype associated with the addition of the hydrophobic tag to Poloxin-2 demonstrated that Poloxin-2HT targets Plk1 in living cells. Our data validate hydrophobic tagging of selective inhibitors of protein-protein interactions as a novel strategy to target and destroy disease-relevant proteins.tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Product Details of 139115-91-6) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Ethers do have nonbonding electron pairs on their oxygen atoms, and they can form hydrogen bonds with other molecules (alcohols, amines, etc.) that have O―H or N―H bonds. Product Details of 139115-91-6 The ability to form hydrogen bonds with other compounds makes ethers particularly good solvents for a wide variety of organic compounds and a surprisingly large number of inorganic compounds.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2018,Spaeth, Andreas; Graeler, Andre; Maisch, Tim; Plaetzer, Kristjan published 《CureCuma-cationic curcuminoids with improved properties and enhanced antimicrobial photodynamic activity》.European Journal of Medicinal Chemistry published the findings.Related Products of 139115-91-6 The information in the text is summarized as follows:

The naturally occurring photosensitizer curcumin has excellent biocompatibility, but its antimicrobial photodynamic efficacy is limited by (i) weak adherence to Gram(-) cell walls, (ii) low (photo-)stability and (iii) limited solubility in water. In this study novel curcuminoids bearing cationic substituents were prepared by different synthetic routes. The derivatives exhibit excellent water solubility, improved photostability and low aggregation. All novel curcuminoids showed antibacterial photodynamic effects (>3 log10 reduction of CFU) against Escherichia coli and Staphylococcus aureus upon blue light illumination. In contrast to natural curcumin, effective photokilling of E. coli was possible without the addition of permeabilizing agents. Ten micromolar of the most active compound achieved a 7 log10 decrease of E. coli after light activation with a fluence of 33.8 J/cm2, whereas S. aureus was inactivated by more than 4 log10 at a fluence of 5.3 J/cm2. Overall the reduction in bacterial count was at least 100-fold more effective with these new curcuminoids in comparison to natural curcumin. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Related Products of 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. Related Products of 139115-91-6 They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2014,Skouta, Rachid; Dixon, Scott J.; Wang, Jianlin; Dunn, Denise E.; Orman, Marina; Shimada, Kenichi; Rosenberg, Paul A.; Lo, Donald C.; Weinberg, Joel M.; Linkermann, Andreas; Stockwell, Brent R. published 《Ferrostatins Inhibit Oxidative Lipid Damage and Cell Death in Diverse Disease Models》.Journal of the American Chemical Society published the findings.SDS of cas: 139115-91-6 The information in the text is summarized as follows:

Ferrostatin-1 (Fer-1) inhibits ferroptosis, a form of regulated, oxidative, nonapoptotic cell death. We found that Fer-1 inhibited cell death in cellular models of Huntington’s disease (HD), periventricular leukomalacia (PVL), and kidney dysfunction; Fer-1 inhibited lipid peroxidation, but not mitochondrial reactive oxygen species formation or lysosomal membrane permeability. We developed a mechanistic model to explain the activity of Fer-1, which guided the development of ferrostatins with improved properties. These studies suggest numerous therapeutic uses for ferrostatins, and that lipid peroxidation mediates diverse disease phenotypes. In the experiment, the researchers used many compounds, for example, tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6SDS of cas: 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Ethers do have nonbonding electron pairs on their oxygen atoms, and they can form hydrogen bonds with other molecules (alcohols, amines, etc.) that have O―H or N―H bonds. The ability to form hydrogen bonds with other compounds makes ethers particularly good solvents for a wide variety of organic compounds and a surprisingly large number of inorganic compounds.SDS of cas: 139115-91-6

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Macropinocytosis as a key determinant of peptidomimetic uptake in cancer cells》 was written by Yoo, Daniel Y.; Barros, Stephanie A.; Brown, Gordon C.; Rabot, Christian; Bar-Sagi, Dafna; Arora, Paramjit S.. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate And the article was included in Journal of the American Chemical Society in 2020. The article conveys some information:

Peptides and peptidomimetics represent the middle space between small mols. and large proteins-they retain the relatively small size and synthetic accessibility of small mols. while providing high binding specificity for biomol. partners typically observed with proteins. During the course of our efforts to target intracellular protein-protein interactions in cancer, we observed that the cellular uptake of peptides is critically determined by the cell line-specifically, we noted that peptides show better uptake in cancer cells with enhanced macropinocytic indexes. Here, we describe the results of our anal. of cellular penetration by different classes of conformationally stabilized peptides. We tested the uptake of linear peptides, peptide macrocycles, stabilized helixes, β-hairpin peptides, and cross-linked helix dimers in 11 different cell lines. Efficient uptake of these conformationally defined constructs directly correlated with the macropinocytic activity of each cell line: high uptake of compounds was observed in cells with mutations in certain signaling pathways. Significantly, the study shows that constrained peptides follow the same uptake mechanism as proteins in macropinocytic cells, but unlike proteins, peptide mimics can be readily designed to resist denaturation and proteolytic degradation Our findings expand the current understanding of cellular uptake in cancer cells by designed peptidomimetics and suggest that cancer cells with certain mutations are suitable mediums for the study of biol. pathways with peptide leads. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2012,Tamura, Tomonori; Tsukiji, Shinya; Hamachi, Itaru published 《Native FKBP12 Engineering by Ligand-Directed Tosyl Chemistry: Labeling Properties and Application to Photo-Cross-Linking of Protein Complexes in Vitro and in Living Cells》.Journal of the American Chemical Society published the findings.Application of 139115-91-6 The information in the text is summarized as follows:

The ability to modify target native (endogenous) proteins selectively in living cells with synthetic mols. should provide powerful tools for chem. biol. To this end, the authors recently developed a novel protein labeling technique termed ligand-directed tosyl (LDT) chem. This method uses labeling reagents in which a protein ligand and a synthetic probe are connected by a tosylate ester group. The authors previously demonstrated its applicability to the selective chem. labeling of several native proteins in living cells and mice. However, many fundamental features of this chem. remain to be studied. In this work, the authors investigated the relation between the LDT reagent structure and labeling properties by using native FK506-binding protein 12 (FKBP12) as a target protein. In vitro experiments revealed that the length and rigidity of the spacer structure linking the protein ligand and the tosylate group have significant effects on the overall labeling yield and labeling site. In addition to histidine, which the authors reported previously, tyrosine and glutamate residues were identified as amino acids that are modified by LDT-mediated labeling. Through the screening of various spacer structures, piperazine was optimal for FKBP12 labeling in terms of labeling efficiency and site specificity. Using a piperazine-based LDT reagent containing a photoreactive probe, the authors successfully demonstrated the labeling and UV-induced covalent crosslinking of FKBP12 and its interacting proteins in vitro and in living cells. This study not only furthers the understanding of the basic reaction properties of LDT chem. but also extends the applicability of this method to the investigation of biol. processes in mammalian cells. The results came from multiple reactions, including the reaction of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Application of 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers. Ethers lack the hydroxyl groups of alcohols. Application of 139115-91-6 Without the strongly polarized O―H bond, ether molecules cannot engage in hydrogen bonding with each other.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2013,El-Gendy, Bahaa El-Dien M.; Zadeh, Ebrahim H. Ghazvini; Sotuyo, Ania C.; Pillai, Girinath G.; Katritzky, Alan R. published 《α-substitution effects on the ease of S → N-acyl transfer in aminothioesters》.Chemical Biology & Drug Design published the findings.Product Details of 139115-91-6 The information in the text is summarized as follows:

The present work investigates the ease of ligations in compounds with all carbon/oxygen (but no amidic group) backbones as compared with those found in peptide sequences with 5-, 6-, and 8-membered cyclic TSs, aiming initially to examine the differential effect of cysteine-free acid, α-ester, and α-amide groups on transition state conformation during the ligation process. In S-acylcysteines and homocysteines the efficacy and rate of S → N-acyl transfer (5 and 6 cyclic TSs) vary with the size of S-acyl group. Conformational and quantum chem. calculations indicate that the spatial distance, b(N-C), between the terminal amine and the thioester carbon is shortened by α-C(O)X (X = OH, OMe, NH2) substituents. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Product Details of 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes. Product Details of 139115-91-6

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

《Novel anti-Alzheimer phenol-lipoyl hybrids: synthesis, physico-chemical characterization, and biological evaluation》 was published in European Journal of Medicinal Chemistry in 2020. These research results belong to Pagoni, Aikaterini; Marinelli, Lisa; Di Stefano, Antonio; Ciulla, Michele; Turkez, Hasan; Mardinoglu, Adil; Vassiliou, Stamatia; Cacciatore, Ivana. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate The article mentions the following:

To date, drugs that hit a single target are inadequate for the treatment of neurodegenerative diseases, such as Alzheimer’s or Parkinson’s diseases. The development of multitarget ligands, able to interact with the different pathways involved in the progression of these disorders, represents a great challenge for medicinal chemists. In this context, we report here the synthesis and biol. evaluation of phenol-lipoyl hybrids (SV1-13), obtained via a linking strategy, to take advantage of the synergistic effect due to the antioxidant portions and anti-amyloid properties of the single constituents present in the hybrid mol. Biol. results showed that SV5 (I) and SV10 (II) possessed the best protective activity against Aβ1-42 induced neurotoxicity in differentiated SH-SY5Y cells. SV9 (III) and II showed remarkable antioxidant properties due to their ability to counteract the damage caused by H2O2 in SHSY-5Y-treated cells. Hovewer, I, showing moderate antioxidant and good neuroprotective activities, resulted the best candidate for further experiments since it also resulted stable both simulated and plasma fluids.tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.Although ethers resist hydrolysis, they are cleaved by hydrobromic acid and hydroiodic acid. Hydrogen chloride cleaves ethers only slowly. Recommanded Product: tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamateIn 2015 ,《Covalent Protein Labeling by Enzymatic Phosphocholination》 appeared in Angewandte Chemie, International Edition. The author of the article were Heller, Katharina; Ochtrop, Philipp; Albers, Michael F.; Zauner, Florian B.; Itzen, Aymelt; Hedberg, Christian. The article conveys some information:

We present a new protein labeling method based on the covalent enzymic phosphocholination of a specific octapeptide amino acid sequence in intact proteins. The bacterial enzyme AnkX from Legionella pneumophila has been established to transfer functional phosphocholine moieties from synthetically produced CDP-choline derivatives to N-termini, C-termini, and internal loop regions in proteins of interest. Furthermore, the covalent modification can be hydrolytically removed by the action of the Legionella enzyme Lem3. Only a short peptide sequence (eight amino acids) is required for efficient protein labeling and a small linker group (PEG-phosphocholine) is introduced to attach the conjugated cargo. In addition to this study using tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate, there are many other studies that have used tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate) was used in this study.

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers. Ethers lack the hydroxyl groups of alcohols. Safety of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate Without the strongly polarized O―H bond, ether molecules cannot engage in hydrogen bonding with each other.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

In 2012,Fujishima, Sho-hei; Yasui, Ryosuke; Miki, Takayuki; Ojida, Akio; Hamachi, Itaru published 《Ligand-Directed Acyl Imidazole Chemistry for Labeling of Membrane-Bound Proteins on Live Cells》.Journal of the American Chemical Society published the findings.SDS of cas: 139115-91-6 The information in the text is summarized as follows:

Chem.-based protein labeling in living cells is undoubtedly useful for understanding natural protein functions and for biol./pharmaceutical applications. Here, the authors report a novel approach for endogenous membrane-bound protein labeling for both in vitro and live cell conditions. A moderately reactive alkyloxyacyl imidazole (AI) assisted by ligand-binding affinity (ligand-directed AI (LDAI)) chem. allowed the authors to selectively modify natural proteins, such as dihydrofolate reductase (DHFR) and folate receptor (FR), neither of which could be efficiently labeled using the recently developed ligand-directed tosylate approach. It was clear that LDAI selectively labeled a single Lys(K32) in DHFR, proximal to the ligand-binding pocket. The authors also demonstrate that the fluorescein-labeled (endogenous, by LDAI) FR works as a fluorescent biosensor on the live KB cell surface, which allowed the authors to carry out unprecedented in situ kinetic anal. of ligand binding to FR. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6SDS of cas: 139115-91-6)

tert-Butyl (2-(2-hydroxyethoxy)ethyl)carbamate(cas: 139115-91-6) belongs to ethers.The C-O bonds that comprise simple ethers are strong. SDS of cas: 139115-91-6 They are unreactive toward all but the strongest bases. Although generally of low chemical reactivity, they are more reactive than alkanes.

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem