2093387-36-9 Usage
Description
3-(4-bromo-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione is a lenalidomide analog, which is a type of chemical compound that has potential applications in various fields due to its unique structure and properties. It is particularly useful in the field of protein degradation, specifically in the research of Proteolysis Targeting Chimeras (PROTACs), as it can be utilized to recruit the CRBN protein.
Uses
Used in Pharmaceutical Industry:
3-(4-bromo-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione is used as a research compound for the development of novel therapeutics. Its ability to recruit the CRBN protein makes it a valuable tool in the design and synthesis of new drugs targeting specific proteins for degradation, which can be beneficial in the treatment of various diseases.
Used in PROTAC Research:
In the field of protein degradation, 3-(4-bromo-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione is used as a key component in the development of PROTACs. These are bifunctional molecules that facilitate the targeted degradation of specific proteins by recruiting the cellular machinery responsible for protein degradation. The compound's ability to recruit the CRBN protein makes it a promising candidate for the development of new PROTACs with potential applications in the treatment of various diseases, including cancer and neurodegenerative disorders.
Used in Drug Design and Synthesis:
3-(4-bromo-1-oxo-2,3-dihydro-1H-isoindol-2-yl)piperidine-2,6-dione is also used as a building block in the design and synthesis of new drugs. Its unique structure allows for the creation of novel compounds with potential therapeutic applications. Researchers can use this compound to develop new drugs that target specific proteins, leading to more effective treatments for a wide range of diseases.
Check Digit Verification of cas no
The CAS Registry Mumber 2093387-36-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 2,0,9,3,3,8 and 7 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 2093387-36:
(9*2)+(8*0)+(7*9)+(6*3)+(5*3)+(4*8)+(3*7)+(2*3)+(1*6)=179
179 % 10 = 9
So 2093387-36-9 is a valid CAS Registry Number.
2093387-36-9Relevant articles and documents
A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3-Ligase PROTACs**
Borrows, Rachel E. A.,Diène, Coura R.,Fairley, Gary,Fallan, Charlene,Fillery, Shaun M.,Hayhow, Thomas G.,Scott, James S.,Watson, David W.
, p. 16818 - 16823 (2020)
A palladium-catalysed Buchwald–Hartwig amination for lenalidomide-derived aryl bromides was optimised using high throughput experimentation (HTE). The substrate scope of the optimised conditions was evaluated for a range of alkyl- and aryl- amines and functionalised aryl bromides. The methodology allows access to new cereblon-based bifunctional proteolysis targeting chimeras with a reduced step count and improved yields.
PROTACs suppression of GSK-3β, a crucial kinase in neurodegenerative diseases
Jiang, Xueyang,Zhou, Junting,Wang, Yang,Liu, Xin,Xu, Kaiying,Xu, Jian,Feng, Feng,Sun, Haopeng
supporting information, (2020/10/26)
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 molecule 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 can effectively degrade GSK-3β in a dose-dependent manner, which can induce 44.2% protein degradation at 2.8 μM. Further pharmacological 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 biological function of GSK-3β protein and its association with diseases.
MDM2 DEGRADERS AND USES THEREOF
-
, (2021/09/26)
The present invention relates to compounds and methods useful for the modulation of mouse double minute 2 homolog ("MDM2") protein via ubiquitination and/or degradation by compounds according to the present invention.
