157654-67-6 Usage
Description
NSC-632839 (157654-67-6) is a pan-specific ubiquitin isopeptidase inhibitor. (IC50= 45, 37 and 9.8 μM for USP2, USP7 and SENP2 respectively) Does not effect proteasome proteolytic activity. NSC-632839 induces apoptosis via a Bcl-2-dependent but apoptosome-independent mitochondrial pathway.1,2?Cell permeable.
Uses
Protein ubiquitination is a dynamic process that can be reversed by deubiquitinating enzymes (DUBs) that remove ubiquitin from proteins, sparing them from degradation by the proteasome. The DUBs have been divided into various groups, the largest being the ubiquitin-specific proteases (USPs). NSC 632839 inhibits USP2 and USP7 as well as the ubiquitin-like SUMO peptidase SENP2 with EC50 values of 45, 37, and 9.8 μM, respectively. It is reported to inhibit apoptosis through a Bcl-2-dependent and apoptosome-independent pathway of caspase activation (IC50 = 15.7 μM in cells sensitized by E1A, an adenoviral oncogene).
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
