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.
Synonym(s):
p53 Activator VII, STIMA-1, 2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
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About This Item
Empirical Formula (Hill Notation):
C10H8N2O
CAS Number:
Molecular Weight:
172.18
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
SMILES string
n1c2c(c(nc1C=C)O)cccc2
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.
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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