D1315
DT Diaphorase (NQO1) human
lyophilized powder, recombinant, expressed in E. coli, ≥90% (SDS-PAGE)
Synonyme(s) :
DTD, NQO1, Quinone reductase
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About This Item
Numéro MDL:
Code UNSPSC :
12352204
Nomenclature NACRES :
NA.54
Produits recommandés
Produit recombinant
expressed in E. coli
Niveau de qualité
Essai
≥90% (SDS-PAGE)
Forme
lyophilized powder
Activité spécifique
≥100 units/mg protein
Poids mol.
monomer 31000
Numéro d'accès UniProt
Température de stockage
2-8°C
Informations sur le gène
human ... NQO1(1728)
Application
Human DT diaphorase has been used in a study to assess the development of novel quinone phosphorodiamidate prodrugs. Human DT diaphorase has also been used to investigate its crystal structure for the development of a model for its interaction with the cytotoxic prodrug 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954).
Actions biochimiques/physiologiques
DT-diaphorase, also referred to as NAD(P)H:(quinone-acceptor) oxidoreductase, is involved in the reductive activation process of several cytotoxic antitumor quinones and nitrobenzenes. It catalyzes the two-electron reduction of quinones and quinonoid compounds to hydroquinones, using either NADH or NADPH as the electron donor. The flavoenzyme contains one mole of FAD per mole of enzyme.
NQO1 is a cytosolic homodimeric FAD-dependent enzyme that catalyses the reduction of a broad range of cytotoxic quinones resulting in protection from cellular oxidative stress. Oxidative stress may also enhance NQO1-mediated protection of p53 and p73 against proteasomal degredation. The highly Inducible expression of NQO1 is controlled by the Nrf2-Keap1/ARE pathway and appears to be affected by changes in susceptibility to oxidative stress. During Oxygen/glucose deprivation, NQO1 appears to be involved in AMPK-induced cancer cell death. NQO1 has been observed to be overexpressed in several types of solid tumors, including breast, pancreas, lung and colon cancer.
Shown to activate quinone based anti-tumor agents in vivo. Suitable for conjugation to carrier molecules.
Définition de l'unité
One unit will reduce 1.0 μmole cytochrome C per min/mg in the presence of menadione substrate at 37 °C.
Inhibiteur
Réf. du produit
Description
Tarif
Produit(s) apparenté(s)
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Équipement de protection individuelle
Eyeshields, Gloves, type N95 (US)
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Les clients ont également consulté
S Chen et al.
The Journal of biological chemistry, 272(3), 1437-1439 (1997-01-17)
DT-diaphorase (EC 1.6.99.2), also referred to as NAD(P)H:(quinone-acceptor) oxidoreductase, is involved in the reductive activation process of several cytotoxic antitumor quinones and nitrobenzenes. It has been observed in our and other laboratories that the rat enzyme is significantly more effective
C Flader et al.
Journal of medicinal chemistry, 43(16), 3157-3167 (2000-08-24)
A series of naphthoquinone and benzimidazolequinone phosphorodiamidates has been synthesized and studied as potential cytotoxic prodrugs activated by DT-diaphorase. Reduction of the quinone moiety in the target compounds was expected to provide a pathway for expulsion of the phosphoramide mustard
Yang Yang et al.
Journal of experimental & clinical cancer research : CR, 33, 14-14 (2014-02-07)
NAD (P) H: quinone oxidoreductase 1 (NQO1) is a xenobiotic metabolizing enzyme that detoxifies chemical stressors and antioxidants, providing cytoprotection in normal tissues. However, high-level expression of NQO1 has been correlated with numerous human malignancies, suggesting a role in carcinogenesis
Molecular of Modelling of Human DT-Diaphorase for Enzyme-Directed Bioreductive Drug Design.
Doughtyl, S.W. and Phillips, R.M.
Molecular Simulations, 24, 209-209 (2000)
Yue Ma et al.
BMC cancer, 14, 414-414 (2014-06-11)
NQO1 (NAD(P)H: quinone oxidoreductase-1), located on chromosome 16q22, functions primarily to protect normal cells from oxidant stress and electrophilic attack. Recent studies have revealed that NQO1 is expressed at a high level in most human solid tumors including those of
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