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Literature summary for 1.8.1.9 extracted from

  • Powis, G.; Wipf, P.; Lynch, S.M.; Birmingham, A.; Kirkpatrick, D.L.
    Molecular pharmacology and antitumor activity of palmarumycin-based inhibitors of thioredoxin reductase (2006), Mol. Cancer Ther., 5, 630-636.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 1.8.1.9

Application

Application Comment Organism
medicine development of novel anticancer agents Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
palmarumycin CP1 0.001 mM, the naphthoquinone spiroketal fungal metabolite palmarumycin CP1 is a potent inhibitor of thioredoxin reductase-1, IC50: 0.00035 mM Homo sapiens
PX-911 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.0032 mM Homo sapiens
PX-916 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, potent inhibitor of purified human thioredoxin reductase-1, IC50: 0.00028 mM Homo sapiens
PX-960 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.00027 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
 Homo sapiens 5829
-

Metals/Ions

Metals/Ions Comment Organism Structure
selenium 0.001 mM, 5fold increase of activity after 7 days Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast cancer cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-
rhabdomyosarcoma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5,5'-dithiobis(2-nitrobenzoic acid) + NADPH
-
 Homo sapiens 2-nitro-5-thiobenzoate + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
NADPH-dependent thioredoxin reductase-1
-
 Homo sapiens
thioredoxin reductase
-
 Homo sapiens
TrxR
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00027
-
 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.00027 mM Homo sapiens PX-960
0.00028
-
 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, potent inhibitor of purified human thioredoxin reductase-1, IC50: 0.00028 mM Homo sapiens PX-916
0.00035
-
 0.001 mM, the naphthoquinone spiroketal fungal metabolite palmarumycin CP1 is a potent inhibitor of thioredoxin reductase-1, IC50: 0.00035 mM Homo sapiens palmarumycin CP1
0.0032
-
 0.001 mM, a water-soluble prodrug of a palmarumycin CP1 analogue, IC50: 0.0032 mM Homo sapiens PX-911