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.

• 同義詞: p53 Activator VII, STIMA-1, 2-Vinyl-1H-quinazolin-4-one, SH group Targeting and Induction of Massive Apoptosis
• 經驗公式（希爾表示法）: C₁₀H₈N₂O
• CAS號碼: 91634-12-7
• 分子量：: 172.18
• MDL號碼: MFCD13195810
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 品質等級: 100
• 化驗: ≥95% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: 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 密鑰: VCHFWHQHIKFOIC-UHFFFAOYSA-N

描述

一般說明

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.

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 week at -20°C. Prepare fresh as required.

其他說明

Zache, N., et al. 2008. Mol. Oncol.2, 70.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 2
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable