Tag: 200-300

Safety of H-Lys(Boc)-OHOn June 1, 2020, Vangala, Venugopal; Nimmu, Narendra Varma; Khalid, Sara; Kuncha, Madhusudana; Sistla, Ramakrishna; Banerjee, Rajkumar; Chaudhuri, Arabinda published an article in Molecular Pharmaceutics. The article was 《Combating Glioblastoma by Codelivering the Small-Molecule Inhibitor of STAT3 and STAT3siRNA with α5β1 Integrin Receptor-Selective Liposomes》. The article mentions the following:

Glioblastoma multiforme (GBM) is one of the most aggressive tumors with a median survival of only 15 mo. Effective therapeutics need to overcome the formidable challenge of crossing the blood-brain barrier (BBB). Receptors and transporters overexpressed on BCECs are being used for designing liposomes, polymers, polymeric micelles, peptides, and dendrimer-based drug carriers for combating brain tumors. Herein, using the orthotopic mouse glioblastoma model, we show that codelivering a small-mol. inhibitor of the JAK/STAT pathway (WP1066) and STAT3siRNA with nanometric (100-150 nm) α5β1 integrin receptor-selective liposomes of RGDK-lipopeptide holds therapeutic promise in combating glioblastoma. Rh-PE (red)-labeled liposomes of RGDK-lipopeptide were found to be internalized in GL261 cells via integrin α5β1 receptors. I.v. administered near-IR (NIR)-dye-labeled α5β1 integrin receptor-selective liposomes of RGDK-lipopeptide were found to be accumulated preferentially in the mouse brain tumor tissue. Importantly, we show that iv injection of WP1066 (a com. sold small-mol. inhibitor of the JAK/STAT pathway) and STAT3siRNA cosolubilized within the liposomes of RGDK-lipopeptide leads to significant inhibition (>350% compared to the untreated mice group) of orthotopically growing mouse glioblastoma. The present strategy may find future use in combating GBM. After reading the article, we found that the author used H-Lys(Boc)-OH(cas: 2418-95-3Safety of H-Lys(Boc)-OH)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Safety of H-Lys(Boc)-OH

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Chakraborty, Moubani; Haag, Stephanie L.; Bernards, Matthew T.; Waynant, Kristopher V. published an article in 2021. The article was titled 《Synthesis of a zwitterionic N-Ser-Ser-C dimethacrylate cross-linker and evaluation in polyampholyte hydrogels》, and you may find the article in Biomaterials Science.Name: tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

Polyampholyte hydrogels are attractive materials for tissue engineering scaffolds as they offer a wide variety of features including nonfouling, selective protein delivery, and tunable phys. characteristics. However, to improve the potential performance of these materials for in vivo applications, there is a need for a higher diversity of zwitterionic cross-linker species to replace commonly used ethylene glycol (EG) based chemistries. Toward this end, the synthesis of a dipeptide based zwitterionic cross-linker, N-Ser-Ser-C dimethacrylate (S-S) from N-Boc-L-serine is presented. The strategy utilized a convergent coupling of methacrylated serine partners followed by careful global deprotection to yield the zwitterionic cross-linker with good overall yields. This novel cross-linker was incorporated into a polyampholyte hydrogel and its phys. properties and biocompatibility were compared against a polyampholyte hydrogel synthesized with an EG-based cross-linker. The S-S cross-linked hydrogel demonstrated excellent nonfouling performance, while promoting enhanced cellular adhesion to fibrinogen delivered from the hydrogel. Therefore, the results suggest that the S-S cross-linker will demonstrate superior future performance for in vivo applications. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Name: tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Name: tert-Butyl N,N’-diisopropylcarbamimidate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2016,Yang, Xing; Mease, Ronnie C.; Pullambhatla, Mrudula; Lisok, Ala; Chen, Ying; Foss, Catherine A.; Wang, Yuchuan; Shallal, Hassan; Edelman, Hannah; Hoye, Adam T.; Attardo, Giorgio; Nimmagadda, Sridhar; Pomper, Martin G. published 《[18F]Fluorobenzoyllysinepentanedioic Acid Carbamates: New Scaffolds for Positron Emission Tomography (PET) Imaging of Prostate-Specific Membrane Antigen (PSMA)》.Journal of Medicinal Chemistry published the findings.Product Details of 71432-55-8 The information in the text is summarized as follows:

Radiolabeled urea-based low-mol. weight inhibitors of the prostate-specific membrane antigen (PSMA) are under intense investigation as imaging and therapeutic agents for prostate and other cancers. In an effort to provide agents with less nontarget organ uptake than the ureas, we synthesized four 18F-labeled inhibitors of PSMA based on carbamate scaffolds. 4-Bromo-2-[18F]fluorobenzoyllysineoxypentanedioic acid (OPA) carbamate and 4-iodo-2-[18F]fluorobenzoyllysine OPA carbamate (I) in particular exhibited high target-selective uptake in PSMA+ PC3 PIP tumor xenografts, with tumor-to-kidney ratios of >1 by 4 h postinjection, an important benchmark. Because of its high tumor uptake (90% injected dose per g of tissue at 2 h postinjection) and high tumor-to-organ ratios, I (X=Br) is promising for clin. translation. Prolonged tumor-specific uptake demonstrated by I (X=I), which did not reach equilibrium during the 4 h study period, suggests carbamates as alternative scaffolds for mitigating dose to nontarget tissues. The results came from multiple reactions, including the reaction of tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Product Details of 71432-55-8)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Product Details of 71432-55-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2013,Zeller, Wayne E. published 《Synthesis of (+)- and (-)-Phaselic Acid》.Synthetic Communications published the findings.Reference of tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

The syntheses of both enantiomers of phaselic acid (2-O-caffeoylmalate) are described. The previously unreported acetate-protected caffeic acid anhydride was used with appropriately protected malic acid derivatives as coupling partners to provide fully protected phaselic acid. Sequential unmasking of the protecting groups afforded phaselic acid in an acceptable overall yield. Supplemental materials are available for this article. Go to the publisher’s online edition of Synthetic Communications to view the free supplemental file. In the experiment, the researchers used many compounds, for example, tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Reference of tert-Butyl N,N’-diisopropylcarbamimidate)

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Reference of tert-Butyl N,N’-diisopropylcarbamimidate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Soley, Jacob; Taylor, Scott D. published an article on February 21 ,2020. The article was titled 《Mild, Rapid, and Chemoselective Procedure for the Introduction of the 9-Phenyl-9-fluorenyl Protecting Group into Amines, Acids, Alcohols, Sulfonamides, Amides, and Thiols》, and you may find the article in Journal of Organic Chemistry.Recommanded Product: H-Lys(Boc)-OH The information in the text is summarized as follows:

The 9-phenyl-9-fluorenyl (PhF) group has been used as an Nα protecting group of amino acids and their derivatives mainly as a result of its ability to prevent racemization. However, installing this group using the standard protocol, which employs 9-bromo-9-phenylfluorene/K3PO4/Pb(NO3)2, often takes days and yields can be variable. Here, we demonstrate that the PhF group can be introduced into the amino group of Weinreb’s amides and Me esters of amino acids, as well as into alcs. and carboxylic acids, rapidly and in excellent yields, using 9-chloro-9-phenylfluorene (PhFCl)/N-methylmorpholine (NMM)/AgNO3. Nα-PhF-protected amino acids can be prepared from unprotected α-amino acids, rapidly and often in near quant. yields, by treatment with N,O-bis(trimethylsilyl)acetamide (BSA) and then PhFCl/NMM/AgNO3. Primary alcs. can be protected with the PhF group in the presence of secondary alcs. in moderate yield. Using PhFCl/AgNO3, a primary alc. can be protected in good yield in the presence of a primary ammonium salt or a carboxylic acid. Primary sulfonamides and amides can be protected in moderate to good yields using phenylfluorenyl alc. (PhFOH)/BF3·OEt2/K3PO4, while thiols can be protected in good to excellent yield using PhFOH/BF3·OEt2 even in the presence of a carboxylic acid or primary ammonium group. The results came from multiple reactions, including the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Recommanded Product: H-Lys(Boc)-OH)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. In addition to subunits of proteins, amino acids have many other functions as well, including osmoregulation (proline), neurotransmitters (gamma-aminobutyric acid), metabolic intermediates (ornithine and citrulline), and inhibitors (dehydroproline).Recommanded Product: H-Lys(Boc)-OH

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Bohnstedt, Adolph C.; Prasad, J. V. N. Vara; Rich, Daniel H. published their research in Tetrahedron Letters on August 13 ,1993. The article was titled 《Synthesis of E- and Z-alkene dipeptide isosteres》.Name: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide The article contains the following contents:

The syntheses of MeLeu-Leu and MeLeu-D-Leu alkene dipeptide isosteres (E)-I and (E)-II (Boc = Me3CO2C, R = H), and (Z)-I and (Z)-II (R = Me) are described. (E)-I and (E)-II were synthesized stereoselectively by employing the [2,3]-Wittig rearrangement to control double bond geometry and C-2 configuration. (Z)-I and (Z)-II were obtained as an easily separable mixture of diastereomers via alkylation of a Z-alkene MeLeu-Gly isostere that was obtained using a Z-selective Wittig reaction as the key step. All isosteres are isolated with high stereochem. purity. In the experimental materials used by the author, we found (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Name: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides. Because of the greater electronegativity of oxygen, the carbonyl (C=O) is a stronger dipole than the N–C dipole.Name: (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide The presence of a C=O dipole and, to a lesser extent a N–C dipole, allows amides to act as H-bond acceptors. In primary and secondary amides, the presence of N–H dipoles allows amides to function as H-bond donors as well.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Electric Literature of C13H26N2O4On March 31, 1999, Llinares, M.; Devin, C.; Chaloin, O.; Azay, J.; Noel-Artis, A.-M.; Bernad, N.; Fehrentz, J.-A.; Martinez, J. published an article in Journal of Peptide Research. The article was 《Syntheses and biological activities of potent bombesin receptor antagonists》. The article mentions the following:

Bombesin receptor antagonists are potential therapeutic agents due to their ability to act as inhibitors of cellular proliferation. On the basis of our hypothesis concerning the mechanism of action of gastrin associating an activating enzyme to the receptor and on the results reported in the literature, we have synthesized bombesin analogs which have been modified in the C-terminal part. Potent bombesin receptor antagonists were obtained by replacement of Leu-13 with a statyl residue or with a residue bearing an hydroxyl group in place of the carbonyl function of Leu-13. Several inhibitors were able to recognize the bombesin receptor on rat pancreatic acini and antagonized bombesin stimulated amylase secretion in the nano-molar range. These compounds were also able to recognize the bombesin receptor and to inhibit [3H] thymidine incorporation in 3T3 cells with the same potency. The experimental process involved the reaction of (S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6Electric Literature of C13H26N2O4)

(S)-N-Methyl-N-methoxy-2-(tert-butoxycarbonylamino)-4-methylpentanamide(cas: 87694-50-6) belongs to amides.Electric Literature of C13H26N2O4 Amides include many other important biological compounds, as well as many drugs like paracetamol, penicillin and LSD. Low-molecular-weight amides, such as dimethylformamide, are common solvents.

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Electric Literature of C9H7ClF3NOOn March 10, 2015, Gantenbein, Markus; Hellstern, Manuel; Le Pleux, Loic; Neuburger, Markus; Mayor, Marcel published an article in Chemistry of Materials. The article was 《New 4,4′-Bis(9-carbazolyl)-Biphenyl Derivatives with Locked Carbazole-Biphenyl Junctions: High-Triplet State Energy Materials》. The article mentions the following:

We synthesized a series of 4,4′-bis(9-carbazolyl)-biphenyl (CBP) derivatives, using Me groups as spatially demanding groups, locking the angle between the carbazole subunit and the biphenyl backbone as potential matrix material for blue organic light-emitting diodes (OLEDs). The locked rotation was achieved by four Me groups either in positions 1 and 8 of the carbazole subunit (1) or in positions 3, 5, 3′, and 5′ of the biphenyl subunit (2), and the fixed spatial arrangement was confirmed by X-ray anal. The phys. properties of CBP derivatives based on parent structure 2 were further tailored by electron-withdrawing CF3 groups in positions 3 and 6 (3) or positions 2 and 7 of the carbazole subunits (4) or alternatively by electron-donating CH3O groups in positions 2 and 7 (5) of the same building blocks. Increased triplet energies (ET) compared to that of the parent compound CBP were found for all synthesized CBP derivatives 1-5. Enhanced glass transition temperatures ranging between 129 and 202 °C further corroborate the application potential of these derivatives for matrix material in blue OLEDs. In the experiment, the researchers used N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0Electric Literature of C9H7ClF3NO)

N-(2-Chloro-4-(trifluoromethyl)phenyl)acetamide(cas: 247170-19-0) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Electric Literature of C9H7ClF3NO

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Reference of H-Lys(Boc)-OHOn May 17, 2019 ,《Genetic incorporation of noncanonical amino acids using two mutually orthogonal quadruplet codons》 appeared in ACS Synthetic Biology. The author of the article were Hankore, Erome Daniel; Zhang, Linyi; Chen, Yan; Liu, Kun; Niu, Wei; Guo, Jiantao. The article conveys some information:

Genetic incorporation of noncanonical amino acids has emerged as a powerful tool for the study of protein structure and function. While the three triplet nonsense codons have been widely explored, quadruplet codons have attracted attention for the potential of creating addnl. blank codons for noncanonical amino acid mutagenesis. Here we demonstrated for the first time that two orthogonal quadruplet codons could be used to simultaneously encode two different noncanonical amino acids within a single protein in bacterial cells. To achieve this, we fine-tuned the interaction between aminoacyl-tRNA synthetase and tRNA, which afforded up to 21-fold improvement in quadruplet codon decoding efficiency. This work represents a significant step toward the use of multiple quadruplet codons for noncanonical amino acid mutagenesis. Simultaneous incorporation of two or more noncanonical amino acids is of significant importance for biol. applications that can benefit from multiple unique functional groups, such as fluorescence resonance energy transfer and NMR studies, and ultimately for the synthesis of completely unnatural biopolymers as new biomaterials. After reading the article, we found that the author used H-Lys(Boc)-OH(cas: 2418-95-3Reference of H-Lys(Boc)-OH)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Reference of H-Lys(Boc)-OH

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Formula: C11H22N2O4On May 20, 2022 ,《Exploration of Methanomethylophilus alvus pyrrolysyl-tRNA synthetase activity in yeast》 appeared in ACS Synthetic Biology. The author of the article were Stieglitz, Jessica T.; Lahiri, Priyanka; Stout, Matthew I.; Van Deventer, James A.. The article conveys some information:

Archaeal pyrrolysyl-tRNA synthetases (PylRSs) have been used to genetically encode over 200 distinct noncanonical amino acids (ncAAs) in proteins in Escherichia coli and mammalian cells. This vastly expands the range of chem. functionality accessible within proteins produced in these organisms. Despite these clear successes, explorations of PylRS function in yeast remain limited. In this work, we demonstrate that the Methanomethylophilus alvus PylRS (MaPylRS) and its cognate tRNACUAMaPyl support the incorporation of ncAAs into proteins produced in Saccharomyces cerevisiae using stop codon suppression methodologies. Addnl., we prepared three MaPylRS mutants originally engineered in E. coli and determined that all three were active with one or more ncAAs, although with low efficiencies of ncAA incorporation in comparison to the parent MaPylRS. Alongside MaPylRS variants, we evaluated the activity of previously reported Methanosarcina mazei, Methanosarcina barkeri, and chimeric M. mazei and M. barkeri PylRSs. Using S. cerevisiae RJY100 and pairing these PylRSs with the M. mazei tRNACUA, we did not observe any detectable stop codon suppression activity under the same conditions that produced moderately efficient ncAA incorporation with MaPylRS. The addition of MaPylRS/tRNACUAMaPyl to the orthogonal translation machinery toolkit in S. cerevisiae potentially opens the door to hundreds of ncAAs that have not previously been genetically encodable using other aminoacyl-tRNA synthetase/tRNA pairs. Extending the scope of ncAA incorporation in yeast could powerfully advance chem. and biol. research for applications ranging from basic biol. discovery to enzyme engineering and therapeutic protein lead discovery. The experimental process involved the reaction of H-Lys(Boc)-OH(cas: 2418-95-3Formula: C11H22N2O4)

H-Lys(Boc)-OH(cas: 2418-95-3) belongs to amino acids. Amino acids are not generally considered to be electrochemically active because products of the oxidation accumulate on the electrode surface and prevent it from participating in any further electrochemical processes.Formula: C11H22N2O4

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics