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NSC 319726

Catalog No.
A4208
Reactivator of mutant p53
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$77.00
In stock
5mg
$70.00
In stock
25mg
$290.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

NSC 319726 is a reactivator of mutant p53 with IC50 value of 8nM [1].

NSC 319726 belongs to the thiosemicarbazone family. In a mouse fibroblast cell line Balb/c 3T3, NSC 319726 shows greater inhibition of cell growth in cells expressing mutant p53 than in WT p53 control. NSC 319726 is also nontoxic to WI38 human fibroblasts (p53 WT). In three different ovarian carcinoma cell lines (TOV112D (p53R175H), OVCAR3 (p53R248W) and SKOV3 (p53-/-)), treatment of NSC 319726 results in an induction of apoptosis in the p53R175 mutant. NSC 319726 restores p53 function through inducing a conformation change of mutant p53 to a “WT-like” structure which can be recognized by the WT specific antibody. The inhibition of cell growth caused by NSC 319726 is also found in the TOV112D (p53R175H) xenografts when the dose of NSC 319726 is 1mg/kg. Furthermore, it is shown that zinc ion chelation and ROS changes are important for the apoptosis induced by NSC319726 [1].

References:
[1] Yu X, Vazquez A, Levine AJ, Carpizo DR. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-25.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt234.32
Cas No.71555-25-4
FormulaC11H14N4S
Solubility≥8.1 mg/mL in DMSO, ≥3.43 mg/mL in EtOH with ultrasonic and warming,insoluble in H2O
Chemical NameN-[(Z)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide
SDFDownload SDF
Canonical SMILESCC(=NNC(=S)N1CCC1)C2=CC=CC=N2
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description NSC 319726 is a reactivator of mutant p53 with IC50 value of 8 nM for fibroblasts expressing the p53R175 mutation.
Targets mutant p53          
IC50 8 nM (in fibroblasts expressing the p53R175 mutation)          

Quality Control

Chemical structure

NSC 319726