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506168
Sigma-Aldrichp53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem
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.
More>>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. Less<<
p53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
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Description
Overview
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.
Catalogue Number
506168
Brand Family
Calbiochem®
Synonyms
2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
p53 Activator VII, STIMA-1 - CAS 91634-12-7 - Calbiochem Certificates of Analysis
Title
Lot Number
506168
References
Reference overview
Zache, N., et al. 2008. Mol. Oncol.2, 70.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
Revision
03-December-2010 RFH
Synonyms
2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
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.
Form
Off-white solid
Intert gas (Yes/No)
Packaged under inert gas
CAS number
91634-12-7
Chemical formula
C₁₀H₈N₂O
Structure formula
Purity
≥95% by HPLC
Solubility
DMSO (50 mg/ml)
Storage
Protect from light
+2°C to +8°C
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 week at -20°C. Prepare fresh as required.
