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PRIMA-1(MET) | Reactivates mutant p53

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

References/Citations

1) Bykov et al. (2005), PRIMA-1MET synergizes with cisplatin to induce tumor cell apoptosis; Oncogene 24 3484
2) Shen et al. (2008), PRIMA-1MET induces mitochondrial apoptosis through activation of caspase-2; Oncogene 27 6571
3) Saha et al. (2013), PRIMA-1MET/APR-246 displays high antitumor in multiple myeloma by induction of p73 and Noxa; Mol. Cancer Ther. 12 2331
4) Rokaeus et al. (2010), PRIMA-1(MET)/APR-246 targets mutant forms of p53 family members p63 and p73; Oncogene 29 6442
5) Tessoulin et al. (2014), PRIMA-1Met induces myeloma cell death independent of p53 by impairing GSH/ROS balance; Blood 124 1626
6) Liu et al. (2017), Inhibiting the system xc-/glutathione axis selectively targets cancers with mutant-p53 accumulation; Nat. Commun. 28 14844
7) Synnott et al. (2018), The Mutant p53-Targeting Compound APR-246 Induces ROS-modulating Genes in Breast Cancer Cells; Transl. Oncol. 11 1343
8) Haffo et al. (2018), Inhibition of the glutaredoxin and thioredoxin systems and ribonucleotide reductase by mutant p53-targeting compound APR-246; Oncogene 24 3484

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Catalog#  10-4175-0005

$60.00
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CAS:
5291-32-7
Catalog Number:
10-4175
Activity:
Reactivates mutant p53
Chemical Name:
2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one
Alternate Names:
APR-246
Molecular Weight:
199.25
Molecular Formula:
C10H17NO3
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
White solid
Purity:
95%
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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