506168-M
p53 Activator VII, STIMA-1
The p53 Activator VII, STIMA-1, also referenced under CAS 91634-12-7, modulates the biological activity of p53. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
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Synonym(s):
p53 Activator VII, STIMA-1, 2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
Empirical Formula (Hill Notation):
C10H8N2O
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
InChI
1S/C10H8N2O/c1-2-9-11-8-6-4-3-5-7(8)10(13)12-9/h2-6H,1H2,(H,11,12,13)
InChI key
VCHFWHQHIKFOIC-UHFFFAOYSA-N
General description
A cell-permeable styrylquinazoline compound that preferentially induces apoptotic death of mutant p53-harboring H1299-His175 and Saos-2-His273 tumor cells (IC50 = 3.4 and 4.9 µM, respectively), while exhibiting much reduced potency towards p53-null (IC50 = 9.6, 11.4, and 14.7 µM against H1299, Saos-2, and HCT116, respectively) or wild-type p53-expressing (IC50 = 13.2 and 20.3 µM against HCT116 and HDF, respectively) cells. STIMA-1 is demonstrated to covalently modify free thiols on mutant p53 in H1299-His175 cells and fully restore its DNA binding activity to the level seen with wild-type p53, resulting in upregulation of p53-dependent gene expression, including p21, PUMA, and Bax.
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 week at -20°C. Prepare fresh as required.
Other Notes
Zache, N., et al. 2008. Mol. Oncol.2, 70.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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