Tag: M.W=200-250

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Arsenic is an environmental chem. of toxicol. concern today since it is a human genotoxin and chronic exposure is associated with development of cancers, including skin. Inorganic arsenate is metabolically reduced to arsenite by glutathione (GSH) prior to methylation. The aim of this study was to determine the relative toxic effects of arsenate and arsenite in HaCat cells (immortalized human keratinocytes) in vitro by measuring cytotoxicity, DNA damage, depletion of glutathione and apoptotic and necrotic events. HaCat cells were treated with arsenate and arsenite (10¦ÌM) for DNA damage detection using Comet assay and cytotoxicity (10, 60 and 100¦ÌM) all measured at 24 h. In some experiment arsenate or arsenite (10¦ÌM) was added at the same time as BSO 10¦ÌM for 24 h, and GSH levels were measured by HPLC with fluorescence detection. Flow cytometry was used to investigate apoptotic and necrotic events following arsenate and arsenite (10¦ÌM) treatment for 24 h. Arsenate and arsenite at 60 and 100¦ÌM, but not 10¦ÌM, reduced the number of adherent viable cells with time. Therefore, DNA damage could only be measured at 10¦ÌM as at higher concentrations the cells did not produce classical Comets but showed fragmentation. DNA damage was significantly (p < 0.001) increased in cells treated for 24 h with 10¦ÌM arsenate and arsenite compared to control. GSH levels were significantly increased in HaCat cells treated with10¦ÌM arsenate and arsenite (p <0.05, p < 0.001, resp.) compared to control. Cells treated with buthionine sulfoximine (BSO) at the same time as arsenate had increased GSH levels (p < 0.001), but arsenite and BSO did not increase cellular GSH. Arsenate and arsenite increased apoptosis, and arsenate increased necrosis, although none of the values reached statistical significance. Arsenite was more cytotoxic than arsenate. Arsenate and arsenite are known to produce oxidative stress involving ROS formation and depletion of glutathione. The increase in GSH levels at low doses of arsenate and arsenite, and by arsenate even in the presence of BSO. Genotoxic effect of arsenate and arsenite in human hacat cells in culture using comet assay. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

A general method for the N-alkylation of NH-sulfoximines and NH-sulfondiimines has been developed, employing alkyl bromides with KOH in DMSO at room temperature A variety of previously inaccessible N-alkylated sulfoximines and sulfondiimines was prepared in good to excellent yields (up to 97%). As an application, the conditions were used to access the biol. active Suloxifen.

N-Alkylations of NH-sulfoximines and NH-sulfondiimines with alkyl halides mediated by potassium hydroxide in dimethyl sulfoxide. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Approx. 20-30% of human lung adenocarcinomas (LUADs) harbor mutations in Kelch-like ECH-associated protein 1 (KEAP1) that hyperactivate the nuclear factor, erythroid 2-like 2 (NFE2L2) antioxidant program. We previously showed that Kras-driven Keap1-mutant LUAD is highly aggressive and dependent on glutaminolysis. Here we performed a druggable genome CRISPR screen and uncovered a Keap1-mutant-specific dependency on solute carrier family 33 member 1 (Slc33a1), as well as several functionally related genes associated with the unfolded protein response. Genetic and biochem. experiments using mouse and human Keap1-mutant tumor lines, as well as preclin. genetically engineered mouse models, validate Slc33a1 as a robust Keap1-mutant-specific dependency. Furthermore, unbiased genome-wide CRISPR screening identified addnl. genes related to Slc33a1 dependency. Overall, our study provides a rationale for stratification of patients harboring KEAP1-mutant or NRF2-hyperactivated tumors as likely responders to targeted SLC33A1 inhibition and underscores the value of integrating functional genetic approaches with genetically engineered mouse models to identify and validate genotype-specific therapeutic targets.

Keap1 mutation renders lung adenocarcinomas dependent on Slc33a1. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(2S)-2-Amino-4-(butylsulfonimidoyl)butanoic acid (BD136012) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 1621962-30-8.

Thioredoxin reductase (TrxR) is a pivotal regulator of redox homeostasis, while dysregulation of redox homeostasis is a hallmark for cancer cells. Thus, there is considerable potential to inhibit the aberrantly upregulated TrxR in cancer cells to discover selective cancer therapeutic agents. Nevertheless, the structural types of TrxR inhibitors presented currently are still relatively limited. We herein report that PACMA 31, previously reported to inhibit protein disulfide isomerase (PDI), is a potent TrxR inhibitor. PACMA 31 possesses a pharmacophore scaffold that is structurally different from the announced TrxR inhibitors and exhibits effective cytotoxicity against cervical cancer cells. Our results reveal that PACMA 31 selectively inhibits TrxR over the related glutathione reductase (GR) and in the presence of reduced glutathione (GSH). Further studies with mutant enzyme and mol. docking suggest that the propynamide fragment of PACMA 31 interacts covalently with the selenocysteine residue of TrxR. Moreover, PACMA 31 effectively and selectively curbs TrxR activity in cells and further stimulates the production of reactive oxygen species (ROS) at low micromolar concentrations, which in turn triggers the accumulation of oxidized thioredoxin (Trx) and GSSG in cells. Follow-up studies demonstrate that PACMA 31 targets TrxR in cells to induce oxidative stress-mediated cancer cell apoptosis. Our results provide a new structural type of TrxR inhibitor that may serve as a useful probe for investigating the biol. of TrxR-implicated pathways, and uncover a new target of PACMA 31 that contributes to it becoming a candidate for cancer treatment.

Revealing PACMA 31 as a new chemical type TrxR inhibitor to promote cancer cell apoptosis. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Cinnamomum camphora leaf essential oil was extracted using enzymic-ultrasound pretreatment followed by microwave assisted extraction method and simultaneously studied as a mycelial growth inhibitor against five important pathogens which cause potato dry rot. The optimum EUP-MAE conditions with a real CEO yield of 19.23 ¡À 0.12 mg/g were obtained through Plackett-Burman design and Box-Behnken design as follows: 3% of enzyme dosage, 2 h of pretreatment time, 5 of pH, 210 W of ultrasound power, 50¡ãC pretreatment temperature, 16 mL/g of water to solid ratio, 30 min of microwave time and 500 W of microwave power. Compared to the reference methods, EUP-MAE possessed a highest CEO yield than these of ultrasound-microwave assisted extraction (U-MAE) and traditional hydrodistillation (HD). Gas chromatog.-mass spectrometry (GC-MS) anal. demonstrated that eucalyptol, camphor, and ¦Á-terpineol were the three main constituents of CEO. Results from in vitro antifungal activity assay revealed that the mycelial growths of all the five tested Fusarium solani, Fusarium culmorum, Fusarium trichothecioides, Fusarium sporotrioides, and Fusarium avenaceum were apparently affected by CEO. These findings not only provide a potential paradigm for the separation of plant essential oil, but also guarantee a promising utilization of the CEO for potato protection to control the Fusarium spp.

Efficient separation of Cinnamomum camphora leaf essential oil and in vitro evaluation of its antifungal activity. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

This article discusses about chem. composition and antimicrobial activity of the leaf essential oil of Vernonia solanifolia. The leaves of Vernonia solanifolia were collected from Hanh Dich Commune and essential oil was obtained by hydrodistillation The instrumental anal. of the essential oil was achieved using gas chromatog. The antimicrobial activity was measured by the determination of MIC and median inhibitory concentration . The major constituents of the essential oil of Vernonia solanifolia have shown antimicrobial activity against E. faecalis, S. aureus, B. cereus, and C. albicans

Chemical Composition and Antimicrobial Activity of the Leaf Essential Oil of Vernonia solanifolia. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1-Bromo-4-(S-methylsulfonimidoyl)benzene (BD336512) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 4381-25-3 and 83730-53-4.

Addtional text regarding the HRMS should be added to the Section 1 of the Exptl. on page S2; the corrected text is given.

Synthesis of N-Imidoyl and N-Oxoimidoyl Sulfoximines from 1-Alkynes, N-Sulfonyl Azides, and Sulfoximines [Erratum to document cited in CA163:145350]. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/1621962-30-8.html, 50578-18-2

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

The effect of seasonings on the quality retention of dried mackerel (Scomber scombrus Linnaeus) was investigated by analyzing the components of the seasonings and prepared dried mackerel. The pH, water content, salt concentration, and inosinic acid content of dried mackerel were influenced by the water content of seasoning liquid The free amino acid content of dried mackerel depended on the seasoning liquid The DPPH radical-scavenging activity of mirin seasoning liquid was significantly higher than that of salt and chorizo, and that of black seven spices (shichimi) and chorizo seasoning powders was extremely high. The content of some aldehydes, alkenes, and alkane of dried mackerel flavored with mirin, shichimi, and chorizo was significantly lower than that flavored with salt. Hexanal concentration further decreased in dried mackerel flavored with shichimi and chorizo. Therefore, the use of shichimi and chorizo as seasoning powders was effective for maintaining the quality of dried mackerel. The production and consumption of dried fish have decreased yearly in Japan. Recently, two types of seasonings flavored with shichimi and chorizo have been, therefore, developed for preparing dried mackerel. These seasonings consisted of liquid and powder. This is the first attempt to use seasoning powders in the production of dried mackerel. This study demonstrated that the generation of fishy volatile components from dried mackerel was inhibited by the shichimi and chorizo seasoning powders.

Effect of various seasonings on the quality retention of dried mackerel (Scomber scombrus Linnaeus). Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Chamaecyparis formosensis Matsumura and C. obtusa var. formosana (Hayata) Rehder are important, precious, and well-known species grown in Asia. Renowned for excellent natural durability, their wood logs are regularly used as quality building materials or furniture. However, these two species have similar appearances, e.g., leaf, twig, wood, hardly distinguishable by the naked eye. The purpose of the present study is to phytochem. differentiate these two species using volatile compounds from the woods. Wood essential oils were obtained by 6-h hydrodistillation The chem. composition was identified by GC-MS, and semi-quantification was carried out to determine the content of each compound Furthermore, compounds with a significantly higher content than those of the other species were screened by t-test and principal component anal. (PCA). Results from semi-quantification and t-test showed that C. formosensis contained higher content of cis-myrtanol (ratio 37.1 ¡À 19.8), chamaecynone (11.0 ¡À 6.7), and ¦Á-eudesmol (8.5 ¡À 7.9), while C. obtusa var. formosana comprised mainly of ¦Á-terpineol (30.2 ¡À 10.1) and borneol (24.0 ¡À 16.1). Moreover, PCA results showed that the representative compounds of C. formosensis were cis-myrtanol and chamaecynone, while those of C. obtusa var. formosana were ¦Á-terpineol, borneol, and ¦Á-cadinol. Taken together, the above-mentioned results suggested significant compositional differences between these two species. For distinguishing the two kinds of wood, C. formosensis should be easily identified by its two characteristic compounds: cis-myrtanol and chamaecynone; while C. obtusa var. formosana could also be distinguished by its characteristic compounds: ¦Á-terpineol and borneol.

Chemotaxonomic identification of Chamaecyparis formosensis Matsumura and Chamaecyparis obtusa var. formosana (Hayata) Rehder using characteristic compounds of wood essential oils. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. Trivial name: delta-Cadinene.
2. It’s mainly derived from flue-cured tobacco, burley tobacco and flavoured tobacco, it has a strong aroma and a good fixing effect, suitable for perfume, cosmetics, can also be used in wine, cigarettes, and toothpaste.
. Recommended Products is: 29350-73-0 and 51905-84-1.

Essential oil compositions and antimicrobial activity of leaves and rhizomes of Alpinia calcicola rom vietnam. The min. inhibitory concentration (MIC) and median inhibitory concentration (IC50) values were measured by the microdilution broth susceptibility assay. The essential oils from the leaves and rhizomes of A. calcicola displayed antimicrobial activity against five of the seven tested microorganisms

Essential Oil Compositions and Antimicrobial Activity of the Leaves and Rhizomes of Alpinia calcicola from Vietnam. Recommended basis is Cadinene. Products is: https://www.ambeed.com/products/189165-77-3.html, 51905-84-1

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem