157654-67-6 Usage
Description
NSC-632839hydrochloride, also known as NSC-632839, is a pan-specific ubiquitin isopeptidase inhibitor with the chemical formula 157654-67-6. It is a cell-permeable compound that does not affect proteasome proteolytic activity. NSC-632839hydrochloride is characterized by its ability to inhibit deubiquitinating enzymes (DUBs) such as USP2, USP7, and the ubiquitin-like SUMO peptidase SENP2, with EC50 values of 45, 37, and 9.8 μM, respectively. NSC632839hydrochloride also induces apoptosis through a Bcl-2-dependent but apoptosome-independent mitochondrial pathway.
Uses
Used in Pharmaceutical Applications:
NSC-632839hydrochloride is used as an inhibitor for deubiquitinating enzymes (DUBs) such as USP2, USP7, and SENP2 for the purpose of modulating protein ubiquitination and preventing protein degradation by the proteasome. This can be particularly useful in the development of therapeutic strategies for various diseases, including cancer.
Used in Cancer Research:
NSC-632839hydrochloride is used as a research tool to study the role of DUBs in cancer cell survival and apoptosis. By inhibiting USP2, USP7, and SENP2, it can help researchers understand the underlying mechanisms of cancer progression and identify potential targets for therapeutic intervention.
Used in Drug Development:
NSC-632839hydrochloride is used as a lead compound in the development of novel drugs targeting DUBs, which may have potential applications in the treatment of various diseases, including cancer. Its ability to induce apoptosis and inhibit protein ubiquitination makes it a promising candidate for further research and development.
Used in Cell Biology Research:
NSC-632839hydrochloride is used as a research tool in cell biology to study the role of protein ubiquitination and deubiquitination in cellular processes, such as cell signaling, protein turnover, and cellular stress responses. This can help researchers gain insights into the complex regulatory mechanisms governing cellular functions and identify potential therapeutic targets for various diseases.
Biological Activity
Inhibitor of ubiquitin isopeptidase activity that displays no effect on the proteolytic activity of the proteasome. Induces apoptosis via a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC 50 values are 15.65 and 16.23 μ M in E1A and E1A/C9CN cells respectively).
References
1) Aleo et al. (2006), Identification of new compounds that trigger apoptosome-independent caspase activation and apoptosis; Cancer Res., 66 9235
2) Nicholson et al. (2008), Characterization of ubiquitin and ubiquitin-like-protein isopeptidase activities; Protein Sci. 17 1035
Check Digit Verification of cas no
The CAS Registry Mumber 157654-67-6 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,7,6,5 and 4 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 157654-67:
(8*1)+(7*5)+(6*7)+(5*6)+(4*5)+(3*4)+(2*6)+(1*7)=166
166 % 10 = 6
So 157654-67-6 is a valid CAS Registry Number.
InChI:InChI=1/C21H21NO.ClH/c1-15-3-7-17(8-4-15)11-19-13-22-14-20(21(19)23)12-18-9-5-16(2)6-10-18;/h3-12,22H,13-14H2,1-2H3;1H/b19-11+,20-12+;
157654-67-6Relevant articles and documents
Cytotoxic evaluation of some 3,5-diarylidene-4-piperidones and various related quaternary ammonium compounds and analogs
Dimmock,Arora,Quail,Pugazhenthi,Allen,Kao,De Clercq
, p. 1124 - 1130 (2007/10/02)
A number of 3,5-diarylidene-4-piperidones (1) and some related quaternary ammonium salts (5) as well as closely related analogs were prepared principally as candidate cytotoxic agents in two screens. The first test system used an average of 54 human tumor
