Tag: M.W=200-250

Bryson, David I. published the artcileContinuous directed evolution of aminoacyl-tRNA synthetases, Name: H-Lys(Boc)-OH, the publication is Nature Chemical Biology (2017), 13(12), 1253-1260, database is CAplus and MEDLINE.

Directed evolution of orthogonal aminoacyl-tRNA synthetases (AARSs) enables site-specific installation of noncanonical amino acids (ncAAs) into proteins. Traditional evolution techniques typically produce AARSs with greatly reduced activity and selectivity compared to their wild-type counterparts. We designed phage-assisted continuous evolution (PACE) selections to rapidly produce highly active and selective orthogonal AARSs through hundreds of generations of evolution. PACE of a chimeric Methanosarcina spp. pyrrolysyl-tRNA synthetase (PylRS) improved its enzymic efficiency (k_cat/K_M^tRNA) 45-fold compared to the parent enzyme. Transplantation of the evolved mutations into other PylRS-derived synthetases improved yields of proteins containing noncanonical residues up to 9.7-fold. Simultaneous pos. and neg. selection PACE over 48 h greatly improved the selectivity of a promiscuous Methanocaldococcus jannaschii tyrosyl-tRNA synthetase variant for site-specific incorporation of p-iodo-L-phenylalanine. These findings offer new AARSs that increase the utility of orthogonal translation systems and establish the capability of PACE to efficiently evolve orthogonal AARSs with high activity and amino acid specificity.

Nature Chemical Biology published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Name: H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Li, Yue published the artcileAn in-line capillary electrophoresis assay for the high-throughput screening of histone deacetylase inhibitors, Safety of H-Lys(Boc)-OH, the publication is Journal of Chromatography A (2019), 171-177, database is CAplus and MEDLINE.

Histone deacetylases (HDACs) are important enzymes that cause chromatin structure contraction and transcription repression, which can downregulate some cancer-suppression genes and lead to the occurrence of cancer. HDAC-specific inhibition is an effective approach to cancer therapy. Hence, a method with which to investigate HDAC activity is needed. We developed an in-line capillary electrophoresis method based on electrophoretically mediated microanal. The optimized conditions were thoroughly validated, and the method was applied to determine the enzyme’s kinetic parameters and the inhibition characteristics of three potent probe inhibitors. The obtained values were comparable to the literature data. Hence, the presented method, with its advantages of miniaturization and full automation, could be used for kinetic and inhibition studies of HDACs, which are targets for drug discovery, in the early stages of new drug development.

Journal of Chromatography A published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Safety of H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Vincent, Christelle published the artcile5-LOX, 12-LOX and 15-LOX in immature forms of human leukemic blasts, Application In Synthesis of 321673-30-7, the publication is Leukemia Research (2008), 32(11), 1756-1762, database is CAplus and MEDLINE.

Several reports have demonstrated an important role of leukotriene B₄ (LTB₄) in the immune system. We investigated whether leukemic blasts from acute myeloid leukemic (AML) and acute lymphoid leukemic (ALL) patients produced LTB₄, 12- and 15-hydroxyeicosatetraenoic acids (12-HETE and 15-HETE) and whether these compounds affected blast proliferation and apoptosis. Leukemic blasts from AML M_0-2 and ALL patients expressed 5-LOX, 12-LOX and 15-LOX transcripts. Quant. polymerase chain reaction indicated that 5-LOX transcripts were far more abundant than 12-LOX and 15-LOX ones. Leukemic blasts expressed 5-LOX activating protein (FLAP) transcripts and produced LTB₄ in response to calcium ionophore. In contrast no 15-HETE production was found. Calcium ionophore-stimulated leukemic blasts produced 12-HETE but also released thromboxane A₂ suggesting that contaminating platelets accounted for the release of these compounds No significant effect of LTB₄, 12-HETE or 15-HETE could be documented on leukemic blast growth and on their apoptose rate. Results of the present study indicate that immature form of leukemic blasts produce LTB₄. However, the three major lipoxygenase metabolites of arachidonic acid; i.e., LTB₄, 12-HETE or 15-HETE, had no evident effect on their growth and apoptosis. We may speculate that LTB₄-derived blast cells might initiate, augment or prolong tissue inflammation and damages by affecting the marrow and blood cytokine network.

Leukemia Research published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C14H20BNO4, Application In Synthesis of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Tomlinson, Matthew L. published the artcileXenopus as a model organism in developmental chemical genetic screens, Name: [(2-Hexylcyclopentylidene)amino]thiourea, the publication is Molecular BioSystems (2005), 1(3), 223-228, database is CAplus and MEDLINE.

Chem. genetics is a potentially powerful tool for studying developmental processes in vertebrate systems. The authors present data showing X. laevis as a model organism in which systematic chem. genetic screens can be carried out. Previous forward chem. genetic screens, including those with developing zebrafish embryos, have demonstrated the nature and value of biol. information gained with this approach. The authors show how amenable Xenopus is to chem. genetics by investigating a series of compounds either with known biochem. effects, or previously identified to give developmental phenotypes, on a range of biol. functions, including the development of pigmentation, the heart, and the central nervous system in zebrafish. The authors have found that the compounds give comparable phenotypes when applied to developing Xenopus embryos. The authors have also studied the penetrance and expressivity of these chem. genetic phenotypes in relation to genetic variation and the developmental window during which the compound is present. Finally, the authors assess the feasibility and the potential throughput of a screen in this vertebrate species.

Molecular BioSystems published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C5H10Cl3O3P, Name: [(2-Hexylcyclopentylidene)amino]thiourea.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Giliomee, Johnel published the artcileEvaluation of composition effects on the physicochemical and biological properties of polypeptide-based hydrogels for potential application in wound healing, Recommanded Product: H-Lys(Boc)-OH, the publication is Polymers (Basel, Switzerland) (2021), 13(11), 1828, database is CAplus and MEDLINE.

In this study, the effect of crosslinking and concentration on the properties of a new library of low-concentration poly(Lys₆₀-ran-Ala₄₀)-based hydrogels for potential application in wound healing was investigated in order to correlate the hydrogel composition with the desired physicochem. and biofunctional properties to expand the assortment of poly-L-lysine (PLL)-based hydrogels suitable for wound healing. Controlled ring-opening polymerization (ROP) and precise hydrogel compositions were used to customize the physicochem. and biofunctional properties of a library of new hydrogels comprising poly(L-lysine-ran-L-alanine) and four-arm poly(ethylene glycol) (P(KA)/4-PEG). The chem. composition and degree of crosslinking via free amine quantification were analyzed for the P(KA)/4-PEG hydrogels. In addition, the rheol. properties, pore morphol., swelling behavior and degradation time were characterized. Subsequently, in vitro cell studies for evaluation of the cytotoxicity and cell adhesion were performed. The 4 wt% 1:1 functional molar ratio hydrogel with P(KA) concentrations as low as 0.65 wt% demonstrated low cytotoxicity and desirable cell adhesion towards fibroblasts and thus displayed a desirable combination of properties for wound healing application.

Polymers (Basel, Switzerland) published new progress about 2418-95-3. 2418-95-3 belongs to amides-buliding-blocks, auxiliary class Chiral,Carboxylic acid,Amine,Aliphatic hydrocarbon chain,Ester,Amino acide derivatives, name is H-Lys(Boc)-OH, and the molecular formula is C11H22N2O4, Recommanded Product: H-Lys(Boc)-OH.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Hua, Guoxiong published the artcileSynthesis and Structural Study of Novel Selenation Derivatives of N, N-Dialkylcyanamides, Quality Control of 2451-91-4, the publication is ChemistrySelect (2016), 1(21), 6810-6817, database is CAplus.

The reaction of 2,4-bis(phenyl)-1,3-diselenadiphosphetane-2,4-diselenide {[PhP(Se)(μ-Se)]₂, Woollins’ reagent, WR} with N, N-dialkylcyanamides 1–3 in refluxing toluene solution led to the corresponding [2+3] cycloaddition products 4-dialkylamino-2,5-diphenyl-1,3,2,5-selenazadiphosphole 2,5-diselenides 4–6 in good yields, the latter were further treated with water resulting in the corresponding hydrolysis derivatives dialkyl-selenoureas 7–9, and phosphinodiselenoates 10 and 11. Selenourea 7 could be transferred into 1,3-selenazol-2-amines 12–15 in excellent yields by further cyclization with four different α-haloketones. All new compounds have been characterized by IR spectroscopy, multi-NMR (¹H, ¹³C, ³¹P, ⁷⁷Se) spectroscopy and accurate mass measurement. The single crystal X-ray structural features of nine new compounds are also discussed.

ChemistrySelect published new progress about 2451-91-4. 2451-91-4 belongs to amides-buliding-blocks, auxiliary class Nitrile,Amine,Benzene, name is N,N-Dibenzylcyanamide, and the molecular formula is C15H14N2, Quality Control of 2451-91-4.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Salives, Richard published the artcileSolid-phase syntheses of 6-arylpyridazin-3(2H)-ones, COA of Formula: C11H16BNO3, the publication is Journal of Combinatorial Chemistry (2005), 7(3), 414-420, database is CAplus and MEDLINE.

The 3-chloropyridazine moiety was immobilized on a Wang resin, using two different methodologies. The first of these involved direct nucleophilic substitution of 3,6-dichloropyridazine with the alcoholate of Wang resin. The exptl. conditions were optimized. The second method involved a Mitsunobu reaction between the Wang resin and 6-chloropyridazin-3-ol during which a problem of regioselectivity was observed The so-obtained chloropyridazine-containing resins were subsequently reacted with various arylboronic acids under Suzuki conditions. Acid cleavage yielded 6-arylpyridazin-3(2H)-ones, e.g., I, with high chem. purity.

Journal of Combinatorial Chemistry published new progress about 146140-95-6. 146140-95-6 belongs to amides-buliding-blocks, auxiliary class Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (2-Pivalamidophenyl)boronic acid, and the molecular formula is C11H16BNO3, COA of Formula: C11H16BNO3.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Wang, Meng published the artcileDifferential contribution of BLT1 and BLT2 to leukotriene B4-induced human NK cell cytotoxicity and migration, Related Products of amides-buliding-blocks, the publication is Mediators of Inflammation (2015), 389849/1-389849/14, database is CAplus and MEDLINE.

Accumulating evidence indicates that leukotriene B4 (LTB4) via its receptors BLT1 and/or BLT2 (BLTRs) could have an important role in regulating infection, tumor progression, inflammation, and autoimmune diseases. In the present study, we showed that LTB4 not only augments cytotoxicity by NK cells but also induces their migration. We found that approx. 30% of fresh NK cells express BLT1, 36% express BLT2, and 15% coexpress both receptors.The use of selective BLTR antagonists indicated that BLT1 was involved in both LTB4-induced migration and cytotoxicity, whereas BLT2 was involved exclusively in NK cell migration, but only in response to higher concentrations of LTB4. BLT1 and BLT2 expression increased after activation of NK cells with IL-2 and IL-15.These changes of BLTR expression by cytokines were reflected in enhanced NK cell responses to LTB4. Our findings suggest that BLT1 and BLT2 play differential roles in LTB4-induced modulation of NK cell activity.

Mediators of Inflammation published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C5H5F3O2, Related Products of amides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Zhang, Shui-Juan published the artcileIntracerebroventricular injection of leukotriene B₄ attenuates antigen-induced asthmatic response via BLT1 receptor stimulating HPA-axis in sensitized rats, Synthetic Route of 321673-30-7, the publication is Respiratory Research (2010), No pp. given, database is CAplus and MEDLINE.

Basic and clin. studies suggest that hypothalamic-pituitary-adrenal (HPA) axis is the neuroendocrine-immune pathway that functionally regulates the chronic inflammatory disease including asthma. Our previous studies showed corresponding changes of cytokines and leukotriene B₄ (LTB₄) between brain and lung tissues in antigen-challenged asthmatic rats. Here, we investigated how the increased LTB₄ level in brain interacts with HPA axis in regulating antigen-induced asthmatic response in sensitized rats. Ovalbumin-sensitized rats were challenged by inhalation of antigen. Rats received vehicle, LTB₄ or U75302 (a selective LTB₄ BLT1 receptor inhibitor) was given via intracerebroventricular injection (i.c.v) 30 min before challenge. Lung resistance (R_L) and dynamic lung compliance (C_dyn) were measured before and after antigen challenge. Inflammatory response in lung tissue was assessed 24 h after challenge. Expression of CRH mRNA and protein in hypothalamus were evaluated by RT-PCR and Western Blot, and plasma levels of adrenocorticotropic hormone (ACTH) and corticosterone (CORT) were measured using the ELISA kits. Antigen challenge decreased pulmonary function and induced airway inflammation, evoked HPA axis response in sensitized rats. Administration of LTB₄ via i.c.v markedly attenuated airway contraction and inflammation. Meanwhile, LTB₄ via i.c.v markedly increased CORT and ACTH level in plasma before antigen challenge, and followed by further increases in CORT and ACTH levels in plasma after antigen challenge in sensitized rats. Expression of CRH mRNA and protein in hypothalamus were also significantly increased by LTB₄ via i.c.v in sensitized rats after antigen challenge. These effect were completely blocked by pre-treatment with BLT1 receptor antagonist U75302 (10 ng), but not by BLT2 antagonist LY255283. LTB₄ administered via i.c.v down-regulates the airway contraction response and inflammation through activation of the HPA axis via its BLT1 receptor. This study expands our concept of the regulatory role of intracranial inflammatory mediators in inflammatory diseases including asthma. The favorable effects of LTB₄ on the HPA axis may help to explain the phenomenon of self-relief after an asthmatic attack.

Respiratory Research published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C8H7ClO3, Synthetic Route of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics

Emre, Ceren published the artcileAge-related changes in brain phospholipids and bioactive lipids in the APP knock-in mouse model of Alzheimers disease, Application In Synthesis of 321673-30-7, the publication is Acta Neuropathologica Communications (2021), 9(1), 116, database is CAplus and MEDLINE.

Sustained brain chronic inflammation in Alzheimers disease (AD) includes glial cell activation, an increase in cytokines and chemokines, and lipid mediators (LMs), concomitant with decreased pro-homeostatic mediators. The inflammatory response at the onset of pathol. engages activation of pro-resolving, pro-homeostatic LMs followed by a gradual decrease. We used an APP knock-in (App KI) AD mouse that accumulates β-amyloid (Aβ) and presents cognitive deficits (at 2 and 6 mo of age, resp.) to investigate LMs, their precursors, biosynthetic enzymes and receptors, glial activation, and inflammatory proteins in the cerebral cortex and hippocampus at 2-, 4-, 8- and 18-mo-old in comparison with wild-type (WT) mice. We used LC-mass-spectrometry and MALDI mol. imaging to analyze LMs and phospholipids, and immunochem. for proteins. Our results revealed an age-specific lipid and cytokine profile, and glial activation in the App KI mice. Despite an early onset of Aβ pathol., pro-inflammatory and pro-resolving LMs were prominently increased only in the oldest age group. Furthermore, the LM biosynthetic enzymes increased, and their receptor expression decreased in the aged App KI mice. Arachidonic acid (AA)-containing phospholipid mol. species were elevated, correlating with decreased cPLA2 activity. MALDI mol. imaging depicted differential distribution of phospholipids according to genotype in hippocampal layers. Brain histol. disclosed increased microglia proliferation starting from young age in the App KI mice, while astrocyte numbers were enhanced in older ages. Our results demonstrate that the brain lipidome is modified preferentially during aging as compared to amyloid pathol. in the model studied here. However, alterations in phospholipids signal early pathol. changes in membrane composition

Acta Neuropathologica Communications published new progress about 321673-30-7. 321673-30-7 belongs to amides-buliding-blocks, auxiliary class Immunology/Inflammation,Scavenger receptor, name is [(2-Hexylcyclopentylidene)amino]thiourea, and the molecular formula is C12H23N3S, Application In Synthesis of 321673-30-7.

Referemce:
https://en.wikipedia.org/wiki/Amide,
Amide – an overview | ScienceDirect Topics