Category: 51644-96-3

Liu, Jing; Yu, Xufen; Chen, He; Kaniskan, H. Umit; Xie, Ling; Chen, Xian; Jin, Jian; Wei, Wenyi published an article in 2022. The article was titled 《TF-DUBTACs Stabilize Tumor Suppressor Transcription Factors》, and you may find the article in Journal of the American Chemical Society.Product Details of 51644-96-3 The information in the text is summarized as follows:

Targeted protein degradation approaches have been widely used for degrading oncogenic proteins, providing a potentially promising therapeutic strategy for cancer treatment. However, approaches to targeting tumor suppressor proteins are very limited, and only a few agonists have been developed to date. Here, we report the development of a platform termed TF-DUBTAC, which links a DNA oligonucleotide to a covalent ligand of the deubiquitinase OTUB1 via a click reaction, to selectively stabilize tumor suppressor transcription factors. We developed three series of TF-DUBTACs, namely, FOXO-DUBTAC, p53-DUBTAC, and IRF-DUBTAC, which stabilize FOXO3A, p53, and IRF3 in cells, resp., in an OTUB1-dependent manner. These results suggest that TF-DUBTAC is a generalizable platform to achieve selective stabilization of tumor suppressor transcription factors as a therapeutic means to suppress tumorigenesis. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Product Details of 51644-96-3) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Product Details of 51644-96-3

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Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics

In 2022,Li, Qinlan; Guo, Qian; Wang, Shuyi; Wan, Shanhe; Li, Zhonghuang; Zhang, Jiajie; Wu, Xiaoyun published an article in European Journal of Medicinal Chemistry. The title of the article was 《Design and synthesis of proteolysis targeting chimeras (PROTACs) as an EGFR degrader based on CO-1686》.Formula: C10H22N2O2 The author mentioned the following in the article:

Epidermal growth factor receptor (EGFR) inhibitors represent the first-line treatment of non-small-cell lung cancer (NSCLC). However, the emergence of acquired drug resistance and side effects largely encumbered their application in clinic. The emerging technol. proteolysis targeting chimera (PROTAC) could be an alternative strategy to overcome these problems. Herein, we reported the discovery of EGFRL858R/T790M degraders based on CO-1686. Promising PROTAC 1q could effectively and selectively inhibit the growth of PC-9 (EGFRDel 19) and H1975 (EGFRL858R/T790M) cells, but not that of A549 (EGFRWT) cells. In addition, 1q could time- and dose-dependently induce degradation of EGFRL858R/T790M in H1975 cells with a DC50 value of 355.9 nM, while did not show obvious effect on the EGFRDel 19 and EGFRWT protein. Preliminary mechanism study demonstrated that the protein degradation was mediated through ubiquitin-proteasome system (UPS). Furthermore, 1q could significantly induce the apoptosis of H1975 cells and arrest the cells in G0/G1 phase. These findings demonstrated that compound 1q could be used as initial lead compound for the development of new EGFRL858R/T790M degraders based therapy. The experimental process involved the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Formula: C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Formula: C10H22N2O2

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

Min, Jaeki; Mayasundari, Anand; Keramatnia, Fatemeh; Jonchere, Barbara; Yang, Seung Wook; Jarusiewicz, Jamie; Actis, Marisa; Das, Sourav; Young, Brandon; Slavish, Jake; Yang, Lei; Li, Yong; Fu, Xiang; Garrett, Shalandus H.; Yun, Mi-Kyung; Li, Zhenmei; Nithianantham, Stanley; Chai, Sergio; Chen, Taosheng; Shelat, Anang; Lee, Richard E.; Nishiguchi, Gisele; White, Stephen W.; Roussel, Martine F.; Potts, Patrick Ryan; Fischer, Marcus; Rankovic, Zoran published an article in 2021. The article was titled 《Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs》, and you may find the article in Angewandte Chemie, International Edition.Related Products of 51644-96-3 The information in the text is summarized as follows:

Targeting cereblon (CRBN) is currently one of the most frequently reported proteolysis-targeting chimera (PROTAC) approaches, owing to favorable drug-like properties of CRBN ligands, immunomodulatory imide drugs (IMiDs). However, IMiDs are known to be inherently unstable, readily undergoing hydrolysis in body fluids. Here we show that IMiDs and IMiD-based PROTACs rapidly hydrolyze in commonly utilized cell media, which significantly affects their cell efficacy. We designed novel CRBN binders, Ph glutarimide (PG) analogs, and showed that they retained affinity for CRBN with high ligand efficiency (LE >0.48) and displayed improved chem. stability. Our efforts led to the discovery of PG PROTAC 4 c (SJ995973), a uniquely potent degrader of bromodomain and extra-terminal (BET) proteins that inhibited the viability of human acute myeloid leukemia MV4-11 cells at low picomolar concentrations (IC50=3 pM; BRD4 DC50=0.87 nM). These findings strongly support the utility of PG derivatives in the design of CRBN-directed PROTACs. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Related Products of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Related Products of 51644-96-3

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

Computed Properties of C10H22N2O2In 2018 ,《Two-step activity-based protein profiling of diacylglycerol lipase》 appeared in Organic & Biomolecular Chemistry. The author of the article were van Rooden, Eva J.; Kreekel, Roy; Hansen, Thomas; Janssen, Antonius P. A.; van Esbroeck, Annelot C. M.; den Dulk, Hans; van den Berg, Richard J. B. H. N.; Codee, Jeroen D. C.; van der Stelt, Mario. The article conveys some information:

Diacylglycerol lipases (DAGL) produce the endocannabinoid 2-arachidonoylglycerol, a key modulator of neurotransmitter release. Chem. tools that visualize endogenous DAGL activity are desired. Here, we report the design, synthesis and application of a triazole urea probe for DAGL equipped with a norbornene as a biorthogonal handle. The activity and selectivity of the probe was assessed with activity-based protein profiling. This probe was potent against endogenous DAGLα (IC50 = 5 nM) and it was successfully applied as a two-step activity-based probe for labeling of DAGLα using an inverse electron-demand Diels-Alder ligation in living cells. The results came from multiple reactions, including the reaction of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Computed Properties of C10H22N2O2)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Computed Properties of C10H22N2O2

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

《Discovery of selective CDK9 degraders with enhancing antiproliferative activity through PROTAC conversion》 was written by Qiu, Xiaqiu; Li, Yuanqing; Yu, Bin; Ren, Jie; Huang, Huidan; Wang, Min; Ding, Hong; Li, Zhiyu; Wang, Jubo; Bian, Jinlei. Application of 51644-96-3This research focused ontriazine pomalidomide cyclin dependent kinase apoptosis pharmacokinetic antiapoptotic antiproliferative; AML; Antitumor; CDK9; Degrader; PROTAC. The article conveys some information:

Cyclin-dependent kinase 9 (CDK9) is an increasingly important potential cancer treatment target. Nowadays, developing selective CDK9 inhibitors has been extremely challenging as its ATP-binding sites are similar with other CDKs. Here, we report that the CDK9 inhibitor BAY-1143572 is converted into a series of proteolysis targeting chimeras (PROTACs) which leads to several compounds inducing the degradation of CDK9 in acute myeloid leukemia cells at a low nanomolar concentration In addition, the most potent PROTAC mol. could inhibit cell growth more effectively than warhead alone, with little inhibition of other kinases. This enhanced antiproliferative activity is mediated by a slight increase in kinase inhibitory activity and an increase in the level of apoptosis induction. Moreover, the most potent PROTAC mol. could induce the degradation of CDK9 in vivo. Our work provides evidence that the most potent PROTAC mol. represents a lead for further development and that CDK9 degradation is a potential valuable therapeutic strategy in acute myeloid leukemia. In addition to this study using tert-Butyl (5-aminopentyl)carbamate, there are many other studies that have used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application of 51644-96-3) was used in this study.

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Application of 51644-96-3

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

Fu, Dingqiang; Yuan, Yi; Qin, Fengming; Xu, Yan; Cui, Xin; Li, Guangxun; Yao, Shaohua; Deng, Yun; Tang, Zhuo published their research in European Journal of Medicinal Chemistry in 2021. The article was titled 《Design, synthesis and biological evaluation of tyrosinase-targeting PROTACs》.Application of 51644-96-3 The article contains the following contents:

The human tyrosinase is the most prominent therapeutic target for pigmentary skin disorders. However, the overwhelming majority efforts have been devoted to search mushroom tyrosinase inhibitors, which show poor inhibitory activity on human tyrosinase and certain side effects that cause skin damage in practical application. Herein, a series of degraders that directly targeted human tyrosinase was firstly designed and synthesized based on newly developed PROTAC technol. The best PROTAC I induced human tyrosinase degradation obviously in dose and time-dependent manner, and its mechanism of inducing tyrosinase degradation has also been clearly demonstrated. Besides, encouraging results that low-toxicity PROTAC I was applied to reduce zebrafish melanin synthesis have been obtained, highlighting the potential to treatment of tyrosinase-related disorders. Moreover, this work has innovatively expanded the application scope of PROTAC technol. and laid a solid foundation for further development of novel drugs treating pigmentary skin disorders. In the experiment, the researchers used many compounds, for example, tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Application of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Application of 51644-96-3

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

Recommanded Product: tert-Butyl (5-aminopentyl)carbamateIn 2021 ,《First orally bioavailable prodrug of proteolysis targeting chimera (PROTAC) degrades cyclin-dependent kinases 2/4/6 in vivo》 was published in European Journal of Medicinal Chemistry. The article was written by Wei, Mingming; Zhao, Rui; Cao, Yuting; Wei, Yujiao; Li, Ming; Dong, Zhiqiang; Liu, Yulin; Ruan, Hao; Li, Ying; Cao, Sheng; Tang, Zhiwen; Zhou, Yuanyuan; Song, Wei; Wang, Yubo; Wang, Jiefu; Yang, Guang; Yang, Cheng. The article contains the following contents:

A growing number of reports suggested that the inhibitor targeting cyclin-dependent kinases (CDK) 2/4/6 can act as a more feasible chemotherapy strategy. In the present paper, a novel PROTAC mol. was developed based on the structure of Ribociclib′s derivative In malignant melanoma cells, the degrader can not only degrade CDK 2/4/6 simultaneously and effectively, but also remarkably induce cell cycle arrest and apoptosis of melanoma cells. Moreover, PROTAC mols. with CRBN ligands always have poor oral bioavailability. We developed the orally bioavailable prodrug for the first time. It would provide general solution for oral administration of the PROTAC mols., derived from CRBN ligands, for animal test conveniently. In the experiment, the researchers used many compounds, for example, tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Recommanded Product: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Recommanded Product: tert-Butyl (5-aminopentyl)carbamate

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

Name: tert-Butyl (5-aminopentyl)carbamateIn 2020 ,《Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1》 appeared in European Journal of Medicinal Chemistry. The author of the article were Cheng, Binbin; Ren, Yichang; Cao, Hao; Chen, Jianjun. The article conveys some information:

Novel resorcinol di-Ph ether-based PROTACs (PROteolysis TArgeting Chimeras) were designed and evaluated for their inhibitory activity against the programmed cell death-1/programmed cell death-ligand 1 (PD-1/PD-L1) pathway and their ability to degrade PD-L1 protein. Most of the compounds displayed excellent inhibitory activities against PD-1/PD-L1, as assessed by the homogeneous time-resolved fluorescence (HTRF) binding assay, with IC50 values ranging from 25 nM to 200 nM. Among them, compound P22 (I) is one of the best with an IC50 value of 39.2 nM. In addition to inhibiting PD-1/PD-L1 interaction, P22 also significantly restored the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. Furthermore, flow cytometry (FCM) and western-blot data demonstrated that P22 could moderately reduce the protein levels of PD-L1 in a lysosome-dependent manner, which may contribute to its immune effects. Preliminary FCM and western-blot data suggest that it is possible to build PD-L1-targeting PROTAC-like mols. based on PD-1/PD-L1 small mol. inhibitors, though these compounds showed only modest degradation efficiencies. Collectively, this work suggests that P22 may serve as a starting point for exploring the degradation of PD-L1 by PROTAC-like strategy. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Name: tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Name: tert-Butyl (5-aminopentyl)carbamate

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

《Characterization of the promiscuous N-acyl CoA transferase, LgoC, in legonoxamine biosynthesis》 was written by Maglangit, Fleurdeliz; Alrashdi, Saad; Renault, Justine; Trembleau, Laurent; Victoria, Catherine; Tong, Ming Him; Wang, Shan; Kyeremeh, Kwaku; Deng, Hai. Product Details of 51644-96-3 And the article was included in Organic & Biomolecular Chemistry in 2020. The article conveys some information:

More than 500 siderophores are known to date, but only three were identified to be aryl-containing hydroxamate siderophores, legonoxamines A and B from Streptomyces sp. MA37, and aryl ferrioxamine 2 from Micrococcus luteus KLE1011. Siderophores are produced by microorganisms to scavenge iron from the environment, thereby making this essential metal nutrient available to the microbe. We demonstrate here that LgoC from MA37 is responsible for the key aryl-hydroxamate forming step in legonoxamine biosynthesis. Biochem. characterization established that LgoC displays considerable promiscuity for the acylation between N-hydroxy-cadaverine and SNAC (N-acetylcysteamines) thioester derivatives The experimental part of the paper was very detailed, including the reaction process of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Product Details of 51644-96-3)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Product Details of 51644-96-3

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

In 2016,Healy, Alan R.; Nikolayevskiy, Herman; Patel, Jaymin R.; Crawford, Jason M.; Herzon, Seth B. published 《A Mechanistic Model for Colibactin-Induced Genotoxicity》.Journal of the American Chemical Society published the findings.Safety of tert-Butyl (5-aminopentyl)carbamate The information in the text is summarized as follows:

Precolibactins and colibactins represent a family of natural products that are encoded by the clb gene cluster and are produced by certain commensal, extraintestinal, and probiotic E. coli. Clb+ E. coli induce megalocytosis and DNA double-strand breaks in eukaryotic cells, but paradoxically, this gene cluster is found in the probiotic Nissle 1917. Evidence suggests precolibactins are converted to genotoxic colibactins by colibactin peptidase (ClbP)-mediated cleavage of an N-acyl-D-Asn side chain, and all isolation efforts have employed ΔclbP strains to facilitate accumulation of precolibactins. It was hypothesized that colibactins form unsaturated imines that alkylate DNA by cyclopropane ring opening (2→3, Scheme 1). However, as no colibactins have been isolated, this hypothesis has not been tested exptl. Addnl., precolibactins A-C (7-9, Figure 1) contain a pyridone that cannot generate the unsaturated imines that form the basis of this hypothesis. To resolve this, we prepared 13 synthetic colibactin derivatives and evaluated their DNA binding and alkylation activity. We show that unsaturated imines, but not the corresponding pyridone derivatives, potently alkylate DNA. The imine, unsaturated lactam, and cyclopropane are essential for efficient DNA alkylation. A cationic residue enhances activity. These studies suggest that precolibactins containing a pyridone are not responsible for the genotoxicity of the clb cluster. Instead, we propose that these are off-pathway fermentation products produced by a facile double cyclodehydration route that manifests in the absence of viable ClbP. The results presented herein provide a foundation to begin to connect metabolite structure with the disparate phenotypes associated with clb+ E. coli. After reading the article, we found that the author used tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3Safety of tert-Butyl (5-aminopentyl)carbamate)

Some of the reported applications of tert-Butyl (5-aminopentyl)carbamate(cas: 51644-96-3) include: synthesis of of a supermacrocycle that self-assemble to form organic nanotubes., preparation of water-soluble unsymmetrical sulforhodamine fluorophores from monobrominated sulfoxanthene dye, synthesis of functionalized porphyrins as biocompatible carrier system for photodynamic therapy (PDT).Safety of tert-Butyl (5-aminopentyl)carbamate

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