Chemical Name: 2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one. Alternate Names: APR-246
Reactivates mutant p53
Molekulargewicht:
199.25
Reinheit:
95%, NMR (Conforms)
Formulierung:
White solid
CAS Nummer:
[5291-32-7]
Formel:
C10H17NO3
Anwendungsbeschreibung:
PRIMA-1MET reactivates mutant p53, an important tumor suppressor gene, in cancer cells.1 It induces p53-dependent mitochondrial apoptosis via activation of caspase-2.2 PRIMA-1MET showed significant antitumor activity in multiple myeloma via activation of p733 and had previously been shown to target p53 family members p63 and p734. Tumor cell death by PRIMA-1MET has been also shown to be caused by glutathione depletion and induced ROS production in a p53 independent manner.5-7 PRIMA-1MET probably induces tumor cell death by both reactivating mutant p53 and inhibiting cellular thiol-dependent redox systems.8
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