An activator of p53
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NSC 146109 (hydrochloride)

Item No. 16430

Technical Information
Formal Name
carbamimidothioic acid, (10-methyl-9-anthracenyl)methyl ester, monohydrochloride
CAS Number
59474-01-0
Synonyms
  • XI-011
Molecular Formula
C17H16N2S • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: 30 mg/mlEthanol: 3 mg/ml
λmax
260 nm
SMILES
NC(SCC1=C2C(C=CC=C2)=C(C)C3=CC=CC=C31)=N.Cl
InChi Code
InChI=1S/C17H16N2S.ClH/c1-11-12-6-2-4-8-14(12)16(10-20-17(18)19)15-9-5-3-7-13(11)15;/h2-9H,10H2,1H3,(H3,18,19);1H
InChi Key
VIBMUYOXJUCEMA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    NSC 146109 is an activator of the tumor suppressor p53 that increases expression of p53 and the p53 target DR5 in wild-type and p53-knockout HCT116 colon adenocarcinoma cells.1 It is selective for p53, having no effect on p73 expression in HCT116 cells at a concentration of 2 μM. NSC 146109 activates p53, which induces cell accumulation in the sub-G0/G1 phase and apoptosis in MCF-7 breast cancer cells.2 It increases p53 expression, decreases expression of the p53 suppressor MDMX, and reduces viability in a panel of breast cancer cell lines when used at a concentration of 0.5 μM. NSC 146109 also reduces growth of AMC-HN9 head and neck carcinoma (HNC) cells in vitro and in vivo when administered alone or in combination with cisplatin (Item No. 13119) in a mouse xenograft model at a dose of 70 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, W., Kim, S.H., and El-Deiry, W.S. Small-molecule modulators of p53 family signaling and antitumor effects in p53-deficient human colon tumor xenografts. Proc. Natl. Acad. Sci. USA 103(29), 11003-11008 (2006).

    2. Wang, H., and Yan, C. A small-molecule p53 activator induces apoptosis through inhibiting MDMX expression in breast cancer cells. Neoplasia 13(7), 611-619 (2011).

    3. Roh, J.L., Park, J.Y., and Kim, E.H. XI-011 enhances cisplatin-induced apoptosis by functional restoration of p53 in head and neck cancer. Apoptosis 19(11), 1594-1602 (2014).