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.
Synonym(s):
p53 Activator VII, STIMA-1, 2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
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
Storage Class
11 - Combustible Solids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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