Tag: 300-400

Inhibition of retinoblastoma cell growth by CEP1347 through activation of the P53 pathway was written by Togashi, Keita;Okada, Masashi;Suzuki, Shuhei;Sanomachi, Tomomi;Seino, Shizuka;Yamamoto, Masahiro;Yamashita, Hidetoshi;Kitanaka, Chifumi. And the article was included in Anticancer Research in 2020.Product Details of 63208-82-2 The following contents are mentioned in the article:

Background/Aim: Despite advances in treatment modalities, the visual prognosis of retinoblastoma still remains unsatisfactory, underscoring the need to develop novel therapeutic approaches. Materials and Methods: The effect on the growth of six human retinoblastoma cell lines and a normal human fibroblast cell line of CEP1347, a small-mol. kinase inhibitor originally developed for the treatment of Parkinson’s disease and therefore with a known safety profile in humans, was examined The role of the P53 pathway in CEP1347-induced growth inhibition was also investigated. Results: CEP1347 selectively inhibited the growth of retinoblastoma cell lines expressing murine double minute 4 (MDM4), a P53 inhibitor. Furthermore, CEP1347 reduced the expression of MDM4 and activated the P53 pathway in MDM4-expressing retinoblastoma cells, which was required for the inhibition of their growth by CEP1347. Conclusion: We propose CEP1347 as a promising candidate for the treatment of retinoblastomas, where functional inactivation of P53 as a result of MDM4 activation is reportedly common. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Product Details of 63208-82-2).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Product Details of 63208-82-2

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Apoptosis and autophagy induction of Seleno-β-lactoglobulin (Se-β-Lg) on hepatocellular carcinoma cells lines was written by Zhao, Yana;Liu, Yaowei;Wang, Wenhang;Wu, Di;Shi, Jianhui;Liu, Anjun. And the article was included in Journal of Functional Foods in 2018.Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide The following contents are mentioned in the article:

β-Lactoglobulin is important fraction in bovine milk. Selenium is an essential nutrient element. The apoptosis and autophagy induction of Se-β-Lg combined selenic acid in β-lactoglobulin on Hep G2 and Hep 3B cells were investigated in this study. MTT assay showed Se-β-Lg inhibited cells viability. Annexin V-FITC/PI and PI staining indicated Se-β-Lg triggered cells apoptosis and cell cycle arrest. Western blot of caspase-cascade suggested Hep-G2 and Hep-3B cells occurred irreversible extrinsic apoptosis. TEM and protein expression of LC3 indicated Se-β-Lg induced cells autophagy. Further explore found Se-β-Lg induced up-regulation of p53 and Fas/FasL in Hep G2 cells. Simultaneously, N-acetyl-L-cysteine, pifithrin-α, Z-VAD-FMK and 3-MA were used. These results further demonstrated Se-β-Lg triggered autophagy and receptor-related apoptosis via p53-mediated Fas/FasL pathway in Hep G2 cells and induced autophagy and p53/Fas-independent caspase activation in Hep 3B cells. Our research revealed that Se-β-Lg had potential to act as chemopreventive compounds in HCC therapy. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Lupeol-loaded nanoparticles enhance the radiosensitivity of hepatocellular carcinoma by inhibiting the hyperactivation in raf/mitogen-activated protein kinase and phospatidylinositol-3 kinase/mTOR pathways was written by Xie, Yinghai;Liu, Changwei;Zhou, Shuping;Wang, Qi;Tang, Xiaolong. And the article was included in Journal of Biomedical Nanotechnology in 2021.Application of 38215-36-0 The following contents are mentioned in the article:

Radioresistance limits the effectiveness of radiotherapy for hepatocellular carcinoma. Raf and PI3K signaling cascades promote the formation of radioresistance in hepatocellular carcinoma (HCC). Lupeol has anticancer activity despite its poor solubility in water and is toxic effect on normal tissue. In this study, nanoparticles (lupeol-NPs) were constructed using PEG-PLGA diblock copolymer vector, and results revealed that Lupeol-NPs reversed the radioresistance of hepatocellular carcinoma by inhibiting cellular proliferation and cell-cycle progression and promoting cellular apoptosis through blocking Raf/MAPK and PI3K/Akt signal transduction in radioresistant Huh-7R cells. In vivo, Lupeol-NPs combined with radiotherapy inhibited the growth of radioresistant hepatocellular carcinoma in a xenogenic nude mouse model. Ki-67 proliferation index decreased significantly (p < 0.05). We conclude that Lupeol-NPs can increase the sensitivity of radioresistant hepatocellular carcinoma to radiotherapy through inhibiting the Raf and PI3K signal cascades. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Application of 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Application of 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Hypoxia-responsive immunostimulatory nanomedicines synergize with checkpoint blockade immunotherapy for potentiating cancer immunotherapy was written by Chen, Weiguo;Sheng, Ping;Chen, Yujiang;Liang, Yi;Wu, Sixin;Jia, Liying;He, Xin;Zhang, Chunfeng;Wang, Chongzhi;Yuan, Chunsu. And the article was included in Chemical Engineering Journal (Amsterdam, Netherlands) in 2023.Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one The following contents are mentioned in the article:

Inducing cell death while simultaneously enhancing antitumor immune responses is a promising therapeutic approach for multiple cancers. Celastrol (Cel) and 7-ethyl-10-hydroxycamptothecin (SN38) have contrasting physicochem. properties, but strong synergy in immunogenic cell death induction and anticancer activity. Herein, a hypoxia-sensitive nanosystem (CS@TAP) was designed to demonstrate effective immunotherapy for colorectal cancer by systemic delivery of an immunostimulatory chemotherapeutic combination. Furthermore, the combination of CS@TAP with anti-PD-L1 mAb (αPD-L1) exhibited a significant therapeutic benefit of delaying tumor growth and increased local doses of immunogenic signaling and T-cell infiltration, ultimately extending survival. We conclude that CS@TAP is an effective inducer of immunogenic cell death (ICD) in cancer immunotherapy. Therefore, this study provides an encouraging strategy to synergistically induce immunogenic cell death to enhance tumor cytotoxic T lymphocytes (CTLs) infiltration for anticancer immunotherapy. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Application In Synthesis of 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Thermo/glutathione-sensitive release kinetics of heterogeneous magnetic micro-organogel prepared by sono-catalysis was written by Dong, Jun;Du, Xiaoyu;Zhang, Yongqiang;Zhuang, Tingting;Cui, Xuejun;Li, Zhanfeng. And the article was included in Colloids and Surfaces, B: Biointerfaces in 2021.Electric Literature of C20H18N2O2S The following contents are mentioned in the article:

To improve the loading and delivery for hydrophobic drugs and optimize the release efficiency in tumor microenvironment, a novel core-shell magnetic micro-organogel carrier was successfully prepared by a sono-catalysis process in the study. As-synthesized magnetic micro-organogel had an appropriate dispersibility in water owing to the hydrophilicity of protein shell and could be kept steadily with a well-defined spherical morphol. owing to the three-dimensional gel structure of oil core, and it promised an accessible targeted drug delivery owing to its good magnetism-mediated motion ability. Moreover, the magnetic micro-organogel showed a high loading efficiency up to 94.22% for coumarin 6 which was dissolved into the micro-organogel as a model hydrophobic drug. More importantly, the release kinetics revealed that the magnetic micro-organogel had a thermo-sensitive and glutathione (GSH)-sensitive ability to control the drug release, and proved that its release mechanisms referred to the combination of erosion, diffusion and degradation This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Electric Literature of C20H18N2O2S).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Electric Literature of C20H18N2O2S

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Preparation and evaluation of SN-38-loaded MMP-2-responsive polymer micelles was written by He, Xiuting;Cao, Zhongcheng;Li, Nuannuan;Chu, Liuxiang;Wang, Jiazhen;Zhang, Chunyan;He, Xiaoyan;Lu, Xiaoyan;Sun, Kaoxiang;Meng, Qingguo. And the article was included in Journal of Drug Delivery Science and Technology in 2021.Reference of 38215-36-0 The following contents are mentioned in the article:

7-Ethyl-10-hydroxycamptothecin (SN-38)-loaded polyethylene glycol-GPLGVRG-poly β-benzyl-L-aspartic acid (PEG-GPLGVRG-PBLA) self-assemblies were successfully prepared using a classical nanopptn. method to give an enzyme-responsive nano-drug delivery system. The PEG-GPLGVRG-PBLA/SN-38 self-assemblies were characterized by transmission electron microscopy, dynamic light scattering, and high-performance liquid chromatog. The encapsulation efficiency was 91.7 ± 1.21% and the drug loading was 16.6 ± 0.93%. The 12 h in vitro release of SN-38 from PEG-GPLGVRG-PBLA/SN-38 treated with MMP-2 was 73.2 ± 2.05%, which was significantly higher than that for the group without MMP-2, demonstrating the enzyme-responsiveness of the nano-drug delivery system. In addition, the cellular uptake and tumor accumulation of PEG-GPLGVRG-PBLA were better than those of PEG-PBLA, and the blank PEG-GPLGVRG-PBLA showed high biocompatibility. These findings indicate that the enzyme-responsive nano SN-38 delivery system could provide new opportunities in tumor therapy. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Reference of 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Reference of 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Anti-fibrotic effects of p53 activation induced by RNA polymerase I inhibitor in primary cardiac fibroblasts was written by Pang, Shu;Chen, Ye;Dai, Chaochao;Liu, Tengfei;Zhang, Wenjing;Wang, Jianli;Cui, Xiaopei;Guo, Xiaosun;Jiang, Fan. And the article was included in European Journal of Pharmacology in 2021.Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide The following contents are mentioned in the article:

Several lines of studies have indicated that the p53 pathway may have important anti-fibrotic functions. Previously we found that the novel selective RNA polymerase I inhibitor CX-5461 induced a robust response of p53 phosphorylation and activation in vascular smooth muscle cells. In the present study, we characterized the anti-fibrotic effects of CX-5461 in primary cardiac fibroblasts. We showed that CX-5461 suppressed spontaneous and mitogen-stimulated activation, proliferation, and myofibroblast differentiation, at a concentration (1μM) with no cytotoxicity. The inhibitory effects of CX-5461 were primarily mediated by activation of the p53 pathway rather than limiting the rate of ribosome biogenesis. It was also shown that CX-5461 triggered a non-canonical DNA damage response in cardiac fibroblasts, which acted as the upstream signal leading to p53 activation. Taking these together, we suggest that p53 activation by pharmacol. inhibition of Pol I may represent a viable approach to repress the development of cardiac fibrosis. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.Recommanded Product: 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Amide-Linked Dendron-based Amphiphiles: A class of pH sensitive and highly biocompatible drug carrier for sustained drug release was written by Kumar, Ashwani;Singh, Mamta;Panda, Amulya Kumar;Tyagi, Yogesh Kumar. And the article was included in Supramolecular Chemistry in 2021.HPLC of Formula: 38215-36-0 The following contents are mentioned in the article:

PG-dendritic amide-linked amphiphilic micelles were studied to increase the solubility of hydrophobic mols. The encapsulation study was done by utilizing hydrophobic pyrene dye using U.V. technique. The encapsulation efficiency of the non-ionic amphiphiles was obtained at neutral p.H. and at room temperature (p.H. 7.0 & 28 °C). The G.3 dendron-based non-ionic oleic (C₁₈-cis)-amphiphile was found to have the 78.2% encapsulation efficiency. Studies show that the amide-linked G.1 dendron-based non-ionic (C₁₈-cis) amphiphiles have sustained dye release percentage of 78.00% at p.H. 6.2 and 26.19% at p.H. 7.0 in 72 h at 37 °C. The in vitro cyto-toxicol. studies showed that after 24-48 h treatment, the G.1 amide amphiphiles exhibit more than 80% of cell viability for concentration as high as 31.25 μg/mL. The cellular uptake was demonstrated using Coumarin 6. The integrated amphiphiles are biocompatible and can be used in the biomedical field as medication encapsulation and target drug delivery. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0HPLC of Formula: 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.HPLC of Formula: 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Surface-modified polylactic acid nanospheres with chitosan for antibacterial activity of 1, 2-benzisothiazolin-3-one was written by Yao, Junwei;Liu, Jingxia;Zhi, Heng;Tao, Hongbing;Xie, Xiaobao;Shi, Qingshan. And the article was included in Carbohydrate Polymers in 2021.HPLC of Formula: 38215-36-0 The following contents are mentioned in the article:

The primary purpose of this study was to develop an innovative chitosan (CS) modified polylactic acid (PLA) nanospheres for enhancing the bioavailability of 1, 2-benzisothiazolin-3-one (BIT). The cellular uptake efficiency was corresponded pos. to the quantity of CS coated on BIT-PLA nanospheres against E. coli and S. aureus. The membrane potentials of E.coli and S. aureus treated with BIT-PLA, BIT-PLA-0.1%CS and BIT-PLA-0.5%CS were reduced with the extension of incubation time and the ratio of coated CS. The enhancement of CS modified on BIT-PLA nanospheres was reduced antioxidase activities and generated excessive reactive oxygen species. The lowest EC50 value of the modified BIT-PLA-0.5%CS suggested that its toxicity index was around 2.95-fold and 2.11-fold that of non-modified BIT-PLA against E. coli and S. aureus, resp. These results revealed that the CS modified BIT-PLA nanospheres had a bright prospect in antibacterial formulation delivery system and improving the bioavailability. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0HPLC of Formula: 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.HPLC of Formula: 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

Multifunctional nanocomposite eye drops of cyclodextrin complex@layered double hydroxides for relay drug delivery to the posterior segment of the eye was written by Xu, Chen;Lu, Jinhui;Zhou, Li;Liang, Jie;Fang, Lei;Cao, Feng. And the article was included in Carbohydrate Polymers in 2021.Reference of 38215-36-0 The following contents are mentioned in the article:

Topical drug delivery system to the posterior segment of the eye is facing many challenges, such as rapid drug elimination, low permeability, and low concentration at the targeted sites. To overcome these challenges, Multifunctional nanocomposite eye drops of dexamethasone-carboxymethyl-β-cyclodextrin@layered double hydroxides-glycylsarcosine (DEX-CM-β-CD@LDH-GS) were developed for relay drug delivery. Herein, our studies demonstrated that DEX-CM-β-CD@LDH-GS could penetrate through human conjunctival epithelial cells with an intact structure and exhibited integrity in the sclera of rabbits eyes with in vivo fluorescence resonance energy transfer imaging. Consequently, tissue distribution indicated that DEX-CM-β-CD@LDH-GS nanocomposite eye drops could maintain the effective therapeutic concentration of DEX in choroid-retina within 3 h. As a relay drug delivery system, drug-CD@LDH nanocomposites offer an efficient strategy for drug delivery from ocular surface to the posterior segment. This study involved multiple reactions and reactants, such as 3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0Reference of 38215-36-0).

3-(Benzo[d]thiazol-2-yl)-7-(diethylamino)-2H-chromen-2-one (cas: 38215-36-0) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Reference of 38215-36-0

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica