DBeQ - CAS 177355-84-9
Catalog number: 177355-84-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C22H20N4
Molecular Weight:
340.42
COA:
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Targets:
p97
Description:
DBeQ inhibits p97 competitively with respect to ATP, with Ki of 3.2 μM, suggesting that it binds to the active site of the D2 domain.
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Purity:
>98%
Synonyms:
JRF 12
MSDS:
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1.Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways.
Chou TF1, Brown SJ, Minond D, Nordin BE, Li K, Jones AC, Chase P, Porubsky PR, Stoltz BM, Schoenen FJ, Patricelli MP, Hodder P, Rosen H, Deshaies RJ. Proc Natl Acad Sci U S A. 2011 Mar 22;108(12):4834-9. doi: 10.1073/pnas.1015312108. Epub 2011 Mar 7.
A specific small-molecule inhibitor of p97 would provide an important tool to investigate diverse functions of this essential ATPase associated with diverse cellular activities (AAA) ATPase and to evaluate its potential to be a therapeutic target in human disease. We carried out a high-throughput screen to identify inhibitors of p97 ATPase activity. Dual-reporter cell lines that simultaneously express p97-dependent and p97-independent proteasome substrates were used to stratify inhibitors that emerged from the screen. N2,N4-dibenzylquinazoline-2,4-diamine (DBeQ) was identified as a selective, potent, reversible, and ATP-competitive p97 inhibitor. DBeQ blocks multiple processes that have been shown by RNAi to depend on p97, including degradation of ubiquitin fusion degradation and endoplasmic reticulum-associated degradation pathway reporters, as well as autophagosome maturation. DBeQ also potently inhibits cancer cell growth and is more rapid than a proteasome inhibitor at mobilizing the executioner caspases-3 and -7.
2.The AAA ATPase Vps4 Plays Important Roles in Candida albicans Hyphal Formation and is Inhibited by DBeQ.
Zhang Y1, Li W2, Chu M1, Chen H1, Yu H1, Fang C1, Sun N1, Wang Q1, Luo T1, Luo K1, She X1, Zhang M1, Yang D3. Mycopathologia. 2015 Dec 23. [Epub ahead of print]
Candida albicans is an opportunistic human pathogen, and its pathogenicity is associated with hyphal formation. Previous studies have shown that at neutral-to-alkaline pH, hyphal growth is dependent on the Rim101 pathway whose activation requires Snf7, a member of the ESCRT system. In this work, we described the purification and characterization of the C. albicans Vps4, an AAA ATPase required for recycling of the ESCRTs. Its role on hyphal growth has been investigated. Our data suggest deletion of Vps4 decreases overall hyphal growth at pH 7 and increases the growth of multiple hyphae induced by serum, which indicates that the ESCRTs may make a Rim101-independent contribution to hyphal growth. Furthermore, DBeQ, an inhibitor of the AAA ATPase p97, was shown to inhibit the ATPase activity of Vps4 with an IC50 of about 11.5 μM. To a less degree, it also inhibits hyphal growth. Our work may provide a new strategy to control C. albicans infection.
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CAS 177355-84-9 DBeQ

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