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Merck

A4111

2-AAPA hydrate

≥95% (HPLC), Irreversible glutathione reductase inhibitor, powder

Synonyma:

R,R′-2-Acetylamino-3-[4-(2-acetylamino-2-carboxyethylsulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid hydrate, S, S′-[1,4-Phenylenebis(iminocarbonothioyl)]bis[N-acetyl-L-Cysteine] hydrate

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O této položce

Empirický vzorec (Hillův zápis):
C18H22N4O6S4
Molekulová hmotnost:
518.65
UNSPSC Code:
12352200
NACRES:
NA.25
Assay:
≥95% (HPLC)
Form:
powder
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Název produktu

2-AAPA hydrate, ≥95% (HPLC)

Quality Segment

assay

≥95% (HPLC)

form

powder

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

General description

2-Acetylamino-3-[4-(2-acetylamino-2-carboxy-ethylsulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid (2-AAPA) can block reductase systems, thereby modulating peroxiredoxin oxidation and mitochondrial function in A172 glioblastoma cells.

Biochem/physiol Actions

Abnormal thiol redox state (TRS) is involved in the pathogenesis of a variety of diseases, such as chronic heart disease and atherosclerosis, rheumatoid arthritis , AIDS , Parkinson disease, Alzheimer disease, etc. Thus there is a need for tools capable of regulating TRS. Glutathione reductase (GR) is a critical enzyme in the homeostasis of TRS. Thus selective GR inhibitor would be a valuable research tool in studying TRS-related processes. Carmustine (#C0400) an anticancer drug is commonly used as GR inhibitor (IC50~470 microM). 2-AAPA is novel, potent cell-penetrable GR inhibitor. The compound is quite selective. But small reduction of activity for GP and GST was observed at 0.1mM concentration of 2-AAPT.
Glutathione reductase (GR) is a critical enzyme in the homeostasis of cellular thiol redox state. 2-AAPA is potent, selective, cell-permeable GR inhibitor, a valuable research tool in studying processes related to thiol redox state. For example, it was used in a study of the relationship between thiol redox state and overall redox state. In addition to the expected decrease in GSH and increase in GSSG, 2-AAPA increased the ratios of NAD(P)H/NAD(P)+. Significant protein glutathionylation was also observed.
Potent cell-permeable irreversible glutathione reductase (GR) inhibitor


Skladovací třída

11 - Combustible Solids

wgk

nwg

flash_point_f

Not applicable

flash_point_c

Not applicable



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