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.

• Sinónimos: p53 Activator VII, STIMA-1, 2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
• Fórmula empírica (notación de Hill): C₁₀H₈N₂O
• Número de CAS: 91634-12-7
• Peso molecular: 172.18
• UNSPSC Code: 12352200
• NACRES: NA.77

Propiedades

• Quality Level: 100
• 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

Descripción

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable