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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.
产品信息
Form Off-white solid
Molar mass 172.2
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO or EtOH
Chemical formula C10H8N2O
CAS number 91634-12-7
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |