Category: 51857-17-1

Product Details of 51857-17-1In 2020 ,《Development of selective mono or dual PROTAC degrader probe of CDK isoforms》 appeared in European Journal of Medicinal Chemistry. The author of the article were Zhou, Fei; Chen, Luyu; Cao, Chaoguo; Yu, Jiang; Luo, Xiaojiao; Zhou, Peiting; Zhao, Lifeng; Du, Wu; Cheng, Jijun; Xie, Yongmei; Chen, Yuanwei. The article conveys some information:

Cyclin-dependent kinase (CDK) family members are promising mol. targets in discovering potent inhibitors in disease settings, they function differentially. CDK2, CDK4 and CDK6, directly regulate the cell cycle, while CDK9 primarily modulates the transcription regulation. In discovering inhibitors of these CDKs, toxicity associated with off-target effect on other CDK homologs often posts as a clin. issue and hinders their further therapeutic development. To improve efficacy and reduce toxicity, here, using the Proteolysis Targeted Chimeras (PROTACs) approach, we design and further optimize small mol. degraders targeting multiple CDKs. We showed that heterobifunctional compound A9 selectively degraded CDK2. We also identified a dual-degrader, compound F3, which potently induced degradation of both CDK2 (DC50: 62 nM) and CDK9 (DC50: 33 nM). In human prostate cancer PC-3 cells, compound F3 potently inhibits cell proliferation by effectively blocking the cell cycle in S and G2/M phases. Our preliminary data suggests that PROTAC-oriented CDK2/9 degradation is potentially an effective therapeutic approach. In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1

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Recommanded Product: N-Boc-1,6-DiaminohexaneIn 2021 ,《Mechanical bonding activation in rotaxane-based organocatalysts》 was published in Organic Chemistry Frontiers. The article was written by Perez, Jesus de Maria; Puigcerver, Julio; Orlando, Tainara; Pastor, Aurelia; Martins, Marcos A. P.; Alajarin, Mateo; Martinez-Cuezva, Alberto; Berna, Jose. The article contains the following contents:

Herein the enhanced efficiency as organocatalysts of a series of succinamide-based hydrogen-bonded [2]rotaxanes functionalized with an acyclic secondary amine as the catalytically active site was reported. Their catalytic activity was also evaluated by, comparing with that of their non-interlocked threads, in an iminium-type process between crotonaldehyde and acetylacetone. The presence of an interlocked polyamide macrocycle notably increased the catalytic activity of the entwined organocatalysts. The mechanized catalysts rapidly form a reactive iminium intermediate with the aldehyde, increasing its population. The hydrogen-bonding interaction established between the macrocycle and the electrophile was proposed as one of the reasons for the rapid formation and stabilization of this key intermediate. The experimental part of the paper was very detailed, including the reaction process of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Recommanded Product: N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Recommanded Product: N-Boc-1,6-Diaminohexane

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Recommanded Product: N-Boc-1,6-DiaminohexaneIn 2021 ,《Discovery of sertraline and its derivatives able to combat drug-resistant gastric cancer cell via inducing apoptosis》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Mu, Chao; Peng, Rui-Kun; Guo, Chun-Ling; Li, Ao; Yang, Xiu-Ming; Zeng, Rong; Li, Yu-Long; Gu, Jing; Ouyang, Qin. The article contains the following contents:

Resistance phenomena during chemotherapy of tumor has been severely hampering the applications of chemotherapeutics. Due to advantage of drug repurposing, discovery of new chemosensitizers based on approved drugs is an effect strategy to find new candidates. Herein, we found antidepressant drug – sertraline, could sensitize drug-resistant gastric cancer cell (SGC-7901/DDP) with the IC50 value of 18.73μM. To understand the structure-activity relationship and improve the activity, 30 derivatives were synthesized and evaluated. The IC50 value of the best compound was improved to 5.2μM. Moreover, we found apoptosis induction and cell cycle arrest was the reason for the cell death of the drug-resistant cells after treatment of sertraline and derivatives, and PI3K/Akt/mTOR pathway was involved. The experimental process involved the reaction of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Recommanded Product: N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Recommanded Product: N-Boc-1,6-Diaminohexane

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

Name: N-Boc-1,6-DiaminohexaneIn 2021 ,《Discovery of a PROTAC targeting ALK with in vivo activity》 appeared in European Journal of Medicinal Chemistry. The author of the article were Yan, Guoyi; Zhong, Xinxin; Yue, Lin; Pu, Chunlan; Shan, Huifang; Lan, Suke; Zhou, Meng; Hou, Xueyan; Yang, Jie; Li, Rui. The article conveys some information:

Anaplastic lymphoma kinase (ALK) was involved in the development of various cancer types. Although several ALK inhibitors have been advanced to clin. trials, the emergence of drug resistance has limited the clin. application of them. To overcome the drug resistance, proteolysis targeting chimeras (PROTACs) could be an alternative strategy. In this study, a series of ALK degraders were designed and synthesized. The degraders were developed through the conjugation of LDK378 and CRBN E3 ubiquitin ligase ligands. Among all the mols., compound I showed potent selective inhibitory activity to ALK and can decrease the cellular levels of ALK fusion proteins in a concentration- and time-dependent manner in H3122 cell line. Meanwhile, I showed improved anticancer activity in vitro comparing with LDK378 and the antiproliferative activity to xenograft tumor model was acceptable. All the results demonstrated that ALK degrader I with in vitro and in vivo anti-cancer activities was valuable for further investigation. In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Name: N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Name: N-Boc-1,6-Diaminohexane

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

Duan, Zhenyu; Luo, Qiang; Dai, Xinghang; Li, Xiaoling; Gu, Lei; Zhu, Hongyan; Tian, Xiaohe; Zhang, Hu; Gong, Qiyong; Gu, Zhongwei; Luo, Kui published an article in 2021. The article was titled 《Synergistic Therapy of a Naturally Inspired Glycopolymer-Based Biomimetic Nanomedicine Harnessing Tumor Genomic Instability》, and you may find the article in Advanced Materials (Weinheim, Germany).Safety of N-Boc-1,6-Diaminohexane The information in the text is summarized as follows:

Inspired by natural saccharide-protein complexes, a stimuli-responsive biodegradable and branched glycopolymer-pyropheophorbide-a (Ppa) conjugate (BSP) with saccharide units for cancer therapy is constructed. A linear glycopolymeric conjugate (LSP), a branched glycopolymeric conjugate (BShP) from Ppa with long carbon chains, and a branched conjugate (BHSP) based on poly[N-(2-hydroxypropyl) methacrylamide] (polyHPMA) without saccharide units are prepared as controls. Through structure-activity relationship studies, BSP with a 3D network structure forms stable nanostructures via weak intermol. interactions, regulating the stacking state of Ppa to improve the singlet oxygen quantum yield and the corresponding photodynamic therapy (PDT) effect. BSP shows high loading of olaparib, and are further coated with tumor cell membranes, resulting in a biomimetic nanomedicine (CM-BSPO). CM-BSPO shows highly efficient tumor targeting and cellular internalization properties. The engulfment of CM-BSPO accompanied with laser irradiation results in a prominent antitumor effect, evidenced by disruption of cell cycles in tumor cells, increased apoptosis and DNA damage, and subsequent inhibition of repair for damaged DNA. The mechanism for the synergistic effect from PDT and olaparib is unveiled at the genetic and protein level through transcriptome anal. Overall, this biodegradable and branched glycopolymer-drug conjugate could be effectively optimized as a biomimetic nanomedicine for cancer therapy. In the part of experimental materials, we found many familiar compounds, such as N-Boc-1,6-Diaminohexane(cas: 51857-17-1Safety of N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Safety of N-Boc-1,6-Diaminohexane

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

《Fluorescent Probes for Ecto-5′-nucleotidase (CD73)》 was published in ACS Medicinal Chemistry Letters in 2020. These research results belong to Schmies, Constanze C.; Rolshoven, Georg; Idris, Riham M.; Losenkova, Karolina; Renn, Christian; Schaekel, Laura; Al-Hroub, Haneen; Wang, Yulu; Garofano, Francesca; Schmidt-Wolf, Ingo G. H.; Zimmermann, Herbert; Yegutkin, Gennady G.; Mueller, Christa E.. Safety of N-Boc-1,6-Diaminohexane The article mentions the following:

Ecto-5′-nucleotidase (CD73) catalyzes the hydrolysis of AMP to anti-inflammatory, immunosuppressive adenosine. It is expressed on vascular endothelial, epithelial, and also numerous cancer cells where it strongly contributes to an immunosuppressive microenvironment. In the present study we designed and synthesized fluorescent-labeled CD73 inhibitors with low nanomolar affinity and high selectivity based on N6-benzyl-α,β-methylene-ADP (PSB-12379) as a lead structure. Fluorescein was attached to the benzyl residue via different linkers resulting in PSB-19416 (14b, Ki 12.6 nM) and PSB-18332 (14a, Ki 2.98 nM) as fluorescent high-affinity probes for CD73. These compounds are anticipated to become useful tools for biol. studies, drug screening, and diagnostic applications. In the experimental materials used by the author, we found N-Boc-1,6-Diaminohexane(cas: 51857-17-1Safety of N-Boc-1,6-Diaminohexane)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) can be used as a linear hexyl spacer (C6-spacer) to synthesize biodegradable poly(disulfide amine)s for gene delivery, a multifunctional dendrimer for theranostics and so on.Safety of N-Boc-1,6-Diaminohexane

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

Shan, Huifang; Ma, Xinyu; Yan, Guoyi; Luo, Meng; Zhong, Xinxin; Lan, Suke; Yang, Jie; Liu, Yuanyuan; Pu, Chunlan; Tong, Yu; Li, Rui published an article in 2021. The article was titled 《Discovery of a novel covalent CDK4/6 inhibitor based on palbociclib scaffold》, and you may find the article in European Journal of Medicinal Chemistry.Electric Literature of C11H24N2O2 The information in the text is summarized as follows:

Cyclin-dependent kinases 4 and 6 (CDK4/6), which are involved in dynamic regulation of cell cycle, play an indispensable role in controlling the tumor growth. Here, based on the scaffold of palbociclib, we designed and synthesized a series of covalent CDK4/6 inhibitors that targeted amino acid Thr107. The optimized compound C-13(I) exhibited potent in vitro anticancer activity against CDK4/6 with high selectivity over CDK4/6. Moreover, C-13 showed significant tumor growth inhibition in MDA-MB-231 tumor xenograft model (TGI of 93.49% at dose of 40 mg/kg) without causing significant weight loss and toxicity during the treatment period. The experimental part of the paper was very detailed, including the reaction process of N-Boc-1,6-Diaminohexane(cas: 51857-17-1Electric Literature of C11H24N2O2)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsElectric Literature of C11H24N2O2

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

Jiang, Xueyang; Zhou, Junting; Wang, Yang; Liu, Xin; Xu, Kaiying; Xu, Jian; Feng, Feng; Sun, Haopeng published an article in 2021. The article was titled 《PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases》, and you may find the article in European Journal of Medicinal Chemistry.HPLC of Formula: 51857-17-1 The information in the text is summarized as follows:

Glycogen synthase kinase 3β (GSK-3β) is involved in a variety of diseases such as neurodegenerative diseases, bipolar disorder, and diabetes. In this study, a series of heterobifunctional small mol. proteolysis targeting chimera (PROTAC) were designed and synthesized based on E3 ubiquitin ligase cereblon (CRBN). Most of PROTACs displayed good inhibitory activity, with the IC50 values at the double-digits nanomolar levels and moderate protein degradation ability against GSK-3β. Western-blot data showed compound PG21(I) can effectively degrade GSK-3β in a dose-dependent manner, which can induce 44.2% protein degradation at 2.8μM. Further pharmacol. experiments revealed that the ability of PG21 to degrade GSK-3β is mediated by the ubiquitin-proteasome system (UPS). In addition, PG21 protects against glutamate-induced cell death in HT-22 cells. As the first PROTAC example to degrade GSK-3β protein, the present study has provided potential candidates for further investigation in the biol. function of GSK-3β protein and its association with diseases. In the part of experimental materials, we found many familiar compounds, such as N-Boc-1,6-Diaminohexane(cas: 51857-17-1HPLC of Formula: 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is a compound useful in organic synthesis used in the preparation of mixed self-assembled monolayers (SAMs) that resist adsorption of proteins using the reaction of amines with a SAM that presents interchain carboxylic anhydride groupsHPLC of Formula: 51857-17-1

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

HPLC of Formula: 51857-17-1In 2022 ,《Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold》 appeared in European Journal of Medicinal Chemistry. The author of the article were Chen, Jingjing; He, Huixin; Wei, Aihuan; Li, Yalei; Cheng, Gang; Qin, Hui; Zhong, Hanyue; Liu, Hongchun; Geng, Meiyu; Shen, Aijun; Hu, Youhong. The article conveys some information:

Novel pyrrolopyridone BET degraders were designed and synthesized based on the binding mode between the pyrrolopyridone BET inhibitor with the BRD4 protein. The potent degraders on MV-4-11 cells were discovered through structure-activity relationship study. Modification of warhead on pyrrolopyridone BET degraded significantly regulates BRD4 isoform (long and short) protein degradation, which induced differential cell cycle arrest and apoptosis on MV-4-11 cells. Docking study revealed that the fine structural modification of BET degraders might bind with the BD domain of BRD4 protein to engaged various surface areas that bind with CRBN. In the part of experimental materials, we found many familiar compounds, such as N-Boc-1,6-Diaminohexane(cas: 51857-17-1HPLC of Formula: 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.HPLC of Formula: 51857-17-1

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

《Synthesis and in vitro evaluation of vanillin derivatives as multi-target therapeutics for the treatment of Alzheimer’s disease》 was written by Blaikie, Laura; Kay, Graeme; Kong Thoo Lin, Paul. Product Details of 51857-17-1This research focused onvanillin naphthalimido phthalimido preparation Alzheimer agent mol modeling; cholinesterase inhibitor naphthalimido phthalimido vanillin; Alzheimer’s disease; Antioxidant; Binding conformation; Cholinesterase inhibitor; Multi-target strategy; Vanillin derivatives. The article conveys some information:

A number of novel naphthalimido and phthalimido vanillin derivatives were synthesized, and evaluated as antioxidants and cholinesterase inhibitors in vitro. Antioxidant activity was assessed using DPPH, FRAP, and ORAC assays. All compounds demonstrated enhanced activity compared to the parent compound, vanillin. They also exhibited BuChE selectivity in Ellman’s assay. A lead compound, naphthalimido derivative I, was identified and displayed strong antioxidant activity (IC50 of 16.67μM in the DPPH assay, a 25-fold increase in activity compared to vanillin in the FRAP assay, and 9.43 TE in the ORAC assay). Furthermore, I exhibited potent BuChE selectivity, with an IC50 of 0.27μM which was around 53-fold greater than the corresponding AChE inhibitory activity. Mol. modeling studies showed that mols. with bulkier groups, as in I, exhibited better BuChE selectivity. This work provides a promising basis for the development of multi-target hybrid compounds based on vanillin as potential AD therapeutics. After reading the article, we found that the author used N-Boc-1,6-Diaminohexane(cas: 51857-17-1Product Details of 51857-17-1)

N-Boc-1,6-Diaminohexane(cas: 51857-17-1) is used to prepare 1,3-Bis[6-(Boc-amino)hexyl]urea by reacting with carbonyl dichloride in the presence of triethylamine. Further, it is used as a reagent for the introduction of a C6-spacer.Product Details of 51857-17-1

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