506164

mutant p53 Reactivator, RETRA

The mutant p53 Reactivator, RETRA, also referenced under CAS 1036069-26-7, controls the biological activity of mutant p53. This small molecule/inhibitor is primarily used for Activators/Inducers applications.

• 别名: mutant p53 Reactivator, RETRA, p53 Activator VI, p73 Activator, 2-(4,5-Dihydro-1,3-thiazol-2-ylthio)-1-(3,4-dihydroxyphenyl)ethanone, HCl, Reactivation of Transcriptional Reporter Activity
• 经验公式（希尔记法）: C₁₁H₁₁NO₃S₂ · xHCl
• CAS号: 1036069-26-7
• 分子量: 269.34 (free base basis)
• UNSPSC代码: 12352200

属性

• 质量水平: 100
• 方案: ≥98% (HPLC)
• 表单: solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; desiccated (hygroscopic); protect from light
• 颜色: off-white
• 溶解性: DMSO: 100 mg/mL
• 运输: ambient
• 储存温度: 2-8°C
• InChI: 1S/C11H11NO3S2.ClH/c13-8-2-1-7(5-9(8)14)10(15)6-17-11-12-3-4-16-11;/h1-2,5,13-14H,3-4,6H2;1H
• InChI key: ZZAVDVMJZKDBIB-UHFFFAOYSA-N

说明

一般描述

A cell-permeable thioethanone compound that upregulates p53 family-responsive element-dependent reporter plasmid transcription activity in cells bearing Glu266, His273, Lys280, or Trp278 mutant p53 by increasing the cellular protein, but not mRNA, level of the p53 homologue p73 (by ~3.7-fold in A431 cells in 20 h with 2 µg/ml RETRA) as well as by disrupting p73 interaction with mutant p53, while exhibiting no similar effects in wild-type p53-bearing or p53-null cells. RETRA is shown to increase transcription of proapoptotic genes (5- and >10-fold increase, respectively, of PUMA/BBC3 and p21/CDKN1A, with 1.5 µg/ml RETRA for 14 h), induce apoptosis, and inhibit the growth of A431, but not wild-type p53-bearing or p53-null cells, in a p53- and p73-dependent manner in vitro, as well as delay (by ~4 days) and reduce (by ~50% on day 25) A431-derived tumor formation in mice (0.4 mg/animal via 6 daily i.p.) in vivo.

包装

Packaged under inert gas

警告

Toxicity: Toxic (F)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

其他说明

Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Kravchenko, J.E., et al. 2008. Proc. Natl. Acad. Sci. USA105, 6302.

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 1
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable