Category: 63208-82-2

Pifithrin-μ modulates microglial activation and promotes histological recovery following spinal cord injury was written by Caponegro, Michael D.;Torres, Luisa F.;Rastegar, Cyrus;Rath, Nisha;Anderson, Maria E.;Robinson, John K.;Tsirka, Stella E.. And the article was included in CNS Neuroscience & Therapeutics in 2019.Computed Properties of C16H19BrN2OS The following contents are mentioned in the article:

Treatments immediately after spinal cord injury (SCI) are anticipated to decrease neuronal death, disruption of neuronal connections, demyelination, and inflammation, and to improve repair and functional recovery. Currently, little can be done to modify the acute phase, which extends to the first 48 h post-injury. Efforts to intervene have focused on the subsequent phases – secondary (days to weeks) and chronic (months to years) – to both promote healing, prevent further damage, and support patients suffering from SCI. We used a contusion model of SCI in female mice, and delivered a small mol. reagent during the early phase of injury. Histol. and behavioral outcomes were assessed and compared. We find that the reagent Pifithrin-μ (PFT-μ) acts early and directly on microglia in vitro, attenuating their activation. When administered during the acute phase of SCI, PFT-μ resulted in reduced lesion size during the initial inflammatory phase, and reduced the numbers of pro-inflammatory microglia and macrophages. Treatment with PFT-μ during the early stage of injury maintained a stable anti-inflammatory environment. Our results indicate that a small mol. reagent PFT-μ has sustained immunomodulatory effects following a single dose after injury. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Computed Properties of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) 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. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Computed Properties of C16H19BrN2OS

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

Bilayer pifithrin-α loaded extracellular matrix/PLGA scaffolds for enhanced vascularized bone formation was written by Xie, Xiaobo;Wang, Wanshun;Cheng, Jing;Liang, Haifeng;Lin, Zefeng;Zhang, Tao;Lu, Yao;Li, Qi. And the article was included in Colloids and Surfaces, B: Biointerfaces in 2020.Synthetic Route of C16H19BrN2OS The following contents are mentioned in the article:

Small intestinal submucosa extracellular matrix (SIS-ECM) composite materials are catching eyes in tissue engineering but have been rarely studied in bone repair. In this study, we developed the unique bilayer bone scaffolds by assembling decellularized SIS-ECM and poly(lactic-co-glycolic acid) (PLGA) nanofibers through the electrospinning technique. To strengthen the bioactivity of the scaffolds, pifithrin-α (PFTα), a p53 inhibitor that can reduce the repressive function of p53 in osteogenesis, was preloaded in the PLGA electrospinning solution We found that the resultant SIS-ECM/PLGA/PFTα scaffolds exhibited porous morphol., good biocompatibility, and enhanced osteoinductivity. Specifically, the SIS-ECM/PLGA/PFTα scaffolds could promote the osteogenic differentiation and mineralization of the preosteoblasts MC3T3-E1 in a PFTα does dependent manner in vitro. Furthermore, the SIS-ECM/PLGA/PFTα scaffolds were better than the pure SIS-ECM and SIS-ECM/PLGA scaffolds in terms of vessel and new bone tissue formation after 4 wk post-implantation in vivo. These overall findings indicated that the bilayer PFTα loaded SIS-ECM/PLGA scaffolds facilitated vascularized bone regeneration, showing promising potential for bone tissue engineering. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Synthetic Route of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. 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.Synthetic Route of C16H19BrN2OS

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

8-Acetonyldihydronitidine inhibits the proliferation of human colorectal cancer cells via activation of p53 was written by Zhou, Jiawang;Li, Ziqian;Zhang, Junjie;Wang, Hongsheng;Yin, Sheng;Du, Jun. And the article was included in European Journal of Pharmacology in 2019.Recommanded Product: 63208-82-2 The following contents are mentioned in the article:

Here, we showed that 8-AHN significantly inhibited the proliferation of human colorectal cell lines via induction of G2/M cell cycle arrest and apoptosis. We found that the p53 played a central role in 8-AHN-induced cell proliferation inhibition. Mechanistically, 8-AHN induced p53 expression and enhanced transcriptional activity, subsequently elevating the expression of p53 target genes, including p21, FAS, and BAX, and then increased the level of activated caspase-3 and decreased the level of cyclin B and cyclin A. Moreover, pifithrin-a, the p53 inhibitor, markedly reversed the above responses induced by 8-AHN, and small interfering RNA-mediated knockdown of TP53 also significantly decreased 8-AHN-induced cell apoptosis. The experiments in vivo showed that 8-AHN significantly suppressed the growth of HCT116 xenograft tumors, associated with proliferation suppression and apoptosis induction in tumor tissues, without inducing any notable major organ-related toxicity. In summary, 8-AHN displays an antitumor effect through cell cycle arrest and apoptosis in colorectal cells via activating p53, which suggests that 8-AHN, exerted a therapeutic potential against colorectal cancer cells, and may be regarded as an effective lead compound 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: 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. 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.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Recommanded Product: 63208-82-2

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

TRPV1 induced apoptosis of colorectal cancer cells by activating calcineurin-NFAT2-p53 signaling pathway was written by Hou, Nengyi;He, Xuelai;Yang, Yuhui;Fu, Junwen;Zhang, Wei;Guo, Zhiyi;Hu, Yang;Liang, Liqin;Xie, Wei;Xiong, Haibo;Wang, Kang;Pang, Minghui. And the article was included in BioMed Research International in 2019.Related Products of 63208-82-2 The following contents are mentioned in the article:

Background/Aims. TRPV1 is a nonselective Ca2+ channel which has recently been observed in many cancers, while its effect on cell proliferation, apoptosis, metabolism, and cancer development in colorectal cancer (CRC) is still unclear. In this study, we hypothesized that TRPV1 is a tumor suppressor in CRC development as well as the underlying mechanism. Methods. Immunohistochem. assay was applied to detect the expression of TRPV1 protein in CRC tissues. HCT116 cell proliferation and apoptosis were measured by CCK-8 and fow cytometry, resp. Cellular Ca2+ concentration was measured by Fluo-4/AMbased fow cytometer. Apoptosis-related proteins were measured by Western blotting. Results. In this study, we found that TRPV1 expression was signifcantly decreased in CRC tissues, compared with CRC-adjacent tissues and normal tissues, resp. Ten, we found that the TRVP1 agonist capsaicin treatment inhibited CRC growth and induced apoptosis by activating P53. Subsequent mechanistic study revealed that the TRPV1 induced cytosolic Ca2+ infux to regulate cell apoptosis and p53 activation through calcineurin. Conclusions. Tis study suggests that TRPV1 served as a tumor suppressor in CRC and contributed to the development of novel therapy of CRC. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Related Products 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 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.Related Products of 63208-82-2

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

Novel roles of ER stress in repressing neural activity and seizures through Mdm2- and p53-dependent protein translation was written by Liu, Dai-Chi;Eagleman, Daphne E.;Tsai, Nien-Pei. And the article was included in PLoS Genetics in 2019.Synthetic Route of C16H19BrN2OS The following contents are mentioned in the article:

In this study, we discovered that the acute ER stress response functions to repress neural activity through a protein translation-dependent mechanism. We found that inducing ER stress promotes the expression and distribution of murine double minute-2 (Mdm2) in the nucleus, leading to ubiquitination and down-regulation of the tumor suppressor p53. Reduction of p53 subsequently maintains protein translation, before the onset of translational repression seen during the latter phase of the ER stress response. Disruption of Mdm2 in an Mdm2 conditional knockdown (cKD) mouse model impairs ER stress-induced p53 down-regulation, protein translation, and reduction of neural activity and seizure severity. Importantly, these defects in Mdm2 cKD mice were restored by both pharmacol. and genetic inhibition of p53 to mimic the inactivation of p53 seen during ER stress. Altogether, our study uncovered a novel mechanism by which neurons respond to acute ER stress. Further, this mechanism plays a beneficial role in reducing neural activity and seizure severity. These findings caution against inhibition of ER stress as a neuroprotective strategy for seizures, epilepsies, and other pathol. conditions associated with excessive neural activity. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Synthetic Route of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Synthetic Route of C16H19BrN2OS

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

Application of P53 mRNA in signal transduction mechanisms of skeletal muscle cells. was written by Xia, Shu. And the article was included in Pakistan journal of pharmaceutical sciences in 2021.Computed Properties of C16H19BrN2OS The following contents are mentioned in the article:

By analyzing the effects of P53 inhibitors and ladder climbing exercise on P53 mRNA transcription in skeletal muscle of mice, the application of P53 mRNA in signal transduction mechanism of skeletal muscle cells was studied. Several clean ICR mice were fed for experiment. The experimental mice were divided into groups to analyze the effect of P53 inhibitor on P53 mRNA transcription in gastrocnemius muscle of mice. The mice were randomly divided into The application of P53 mRNA in signal transduction mechanism of skeletal muscle cells was studied, and the corresponding endurance exercise program and ladder climbing training program were designed. According to the research, exercise is to some extent a stimulating factor affecting P53 inhibitor. Endurance training and injection of P53 inhibitor affect P53 mRNA content. Exercise has a benign effect on ICR mice injected with P53 inhibitor. The expression of P53 mRNA in skeletal muscle was significantly affected by climbing training in youth, and decreased by climbing training in old age. However, there was no difference between long-term climbing training and short-term climbing training in the expression of P53 mRNA in skeletal muscle. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Computed Properties of C16H19BrN2OS).

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. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Computed Properties of C16H19BrN2OS

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

Establishment of an oligoasthenospermia mouse model based on TAp73 gene suppression was written by Liu, Hong-Juan;Deng, Meng-Yun;Zhu, Yan-Yan;Wu, De-Ling;Tong, Xiao-Hui;Li, Li;Wang, Lei;Xu, Fei;Wang, Tong-Sheng. And the article was included in Animal Models and Experimental Medicine in 2021.Category: thiazole The following contents are mentioned in the article:

Oligoasthenospermia is one of the main causes of male infertility. Researchers usually use chem. drugs to directly damage germ cells to prep oligoasthenospermia models, which disregards the adhesion and migration between spermatogenic cells and Sertoli cells. TAp73 is a critical regulator of the adhesin of germ cell; thus, we sought to explore a novel oligoasthenospermia model based on TAp73 gene suppression. Mice in the Pifithrin-α group were injected i.p. with 2.5 mg/kg Pifithrin-α (TAp73 inhibitor) daily for 30 consecutive days. Reproductive hormone levels and epididymal sperm quality, as well as the network morphologyof Sertoli cells were tested. Sperm d, motility, and the relative protein and mRNA expression of TAp73 and Nectin 2 were obviously decreased in the Pifithrin-α group compared with the normal control group. No significant distinction was observed in the relative mRNA and protein expression of ZO-1. Furthermore, the tight junctions (TJs) and apical ectoplasmic specialization (ES) were destroyed in the Pifithrin-α group. The above indicate that we successfully established a new oligoasthenospermia mouse model. This study provides a foundation for further exploration of the roles of TAp73 genes during spermatogenesis and provides new research objects for further oligospermia research and future drug discovery. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Category: thiazole).

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 is notable as a component of the vitamin thiamine (B1). Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole

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

TP53 upregulates α-smooth muscle actin expression in tamoxifen-resistant breast cancer cells was written by Kim, Sangmin;You, Daeun;Jeong, Yisun;Yu, Jonghan;Kim, Seok Won;Nam, Seok Jin;Lee, Jeong Eon. And the article was included in Oncology Reports in 2019.Category: thiazole The following contents are mentioned in the article:

In a previous study, we reported that α-smooth muscle actin (α-SMA), one of the mesenchymal marker proteins, is highly expressed in tamoxifen-resistant breast cancer (TamR) cells. However, the exact mechanism of α-SMA expression in TamR cells is not fully understood. Here, we investigated the effect of TP53 on α-SMA expression in breast cancer cells. The levels of α-SMA mRNA and protein expression were analyzed by real-time PCR and western blotting, resp. In estrogen receptor-pos. [ER(+)] breast cancer patients, aberrant α-SMA expression was found to be associated with a poor prognosis. The level of α-SMA expression was significantly increased in established TamR cells compared to tamoxifen-sensitive (TamS) cells. To verify the regulatory mechanism of α-SMA expression, we analyzed diverse kinase activities between TamS and TamR cells. The activity of TP53 was markedly increased in the TamR cells. When TamS cells were treated with TP53 activator, Nutlin3 (Nut3), α-SMA expression was increased in the TamS cells. In addition, α-SMA expression was significantly increased by TP53 overexpression in breast cancer cells. On the contrary, the basal level of α-SMA expression was decreased by the TP53 inhibitor, pifithrin-α (PFT-α). Taken together, we demonstrated that α-SMA expression is regulated by TP53 activity in TamR cells. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Category: thiazole).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Category: thiazole

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

Farnesoid X receptor functions in cervical cancer via the p14^ARF-mouse double minute 2-p53 pathway was written by Huang, Xiaohua;Wang, Bin;Shen, Huimin;Huang, Danmei;Shi, Ganggang. And the article was included in Molecular Biology Reports in 2022.Computed Properties of C16H19BrN2OS The following contents are mentioned in the article:

Cervical cancer is the second most common cancer among women living in developing countries. Farnesoid X receptor (FXR) is a member of the nuclear receptor family, which regulates the development and proliferation of cancer. However, the role of and mol. mechanism by which FXR acts in cervical cancer are still unknown. The relationship between FXR and the proliferation of cervical cancer cell lines was detected by MTT and colony formation assays. Immunohistochem. was used to detect the expression of FXR in cervical cancer tissue slides. Western blotting was used to detect the expression of p14ARF, mouse double minute 2 (MDM2) and p53 when FXR was overexpressed or siRNA was applied. Western blotting was used to detect the expression of MDM2 and p53 when pifithrin-α (PFT-α) was applied. FXR activation inhibited the proliferation of cervical cancer cell lines. FXR was significantly decreased in cervical squamous cell carcinoma, which was correlated with TNM stage, but not with metastasis. Overexpression of FXR activated the p14ARF-MDM2-p53 pathway. As a p53 inhibitor, PFT-α increased MDM2 in Lenti-vector cells, but had no effect on MDM2 in Lenti-FXR cells. FXR inhibits cervical cancer by upregulating the p14ARF-MDM2-p53 pathway. Activation of FXR may be a potential strategy for the treatment of cervical cancer. This study involved multiple reactions and reactants, such as 2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2Computed Properties of C16H19BrN2OS).

2-(2-Imino-4,5,6,7-tetrahydrobenzothiazol-3-yl)-1-p-tolylethanone Hydrobromide (cas: 63208-82-2) 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.Computed Properties of C16H19BrN2OS

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

PFT-α inhibits gallid alpha herpesvirus 1 replication by repressing host nucleotide metabolism and ATP synthesis was written by Xu, Li;Wang, Zhitao;Chen, Zhijie;Cui, Lu;Liu, Zheyi;Liang, Yumeng;Li, Xuefeng;Zhang, Yanhui;Liu, Shengwang;Li, Hai. And the article was included in Veterinary Microbiology in 2022.Recommanded Product: 63208-82-2 The following contents are mentioned in the article:

Therapeutics targeting virus-host interactions have been considered promising strategies for treating herpesvirus infection. Our previous study on avian infectious laryngotracheitis virus (ILTV), an avian herpesvirus economically important to the poultry industry worldwide, identified the small mol. Pifithrin-α (PFT-α) as a potential therapeutic agent. However, the underlying mechanisms of its antiviral function remain largely unknown. Using the ILTV-permissive chicken cell line LMH as the model, we found that PFT-α effectively suppressed the transcription and genome replication of ILTV and greatly reduced the level of infectious virions. Genome-wide transcriptome anal. revealed extensive repression of the metabolic processes of infected cells by PFT-α administration. Further metabolome assays of ILTV-infected cells using liquid chromatog. coupled with mass spectrometry suggest host nucleotide metabolism and ATP synthesis as the key targets of PFT-α treatment during its repression of ILTV replication, which was exptl. supported by the reduced transcription of many key enzymes essential to nucleotide metabolism and ATP synthesis. The present study provides insights into the mechanisms by which PFT-α inhibits ILTV infection, which may increase the probability of successful clin. application of this mol. 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: 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. 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: 63208-82-2

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