506149
p53 Activator III, RITA
The p53 Activator III, RITA, also referenced under CAS 213261-59-7, modulates the biological activity of p53. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
别名:
p53 Activator III, RITA, NSC 652287, 2,5- bis-(5-Hydroxymethyl-2-thienyl)-furan, Reactivation of p53 and Induction of Tumor cell Apoptosis, MDM2 Antagonist VII, MDM2 Inhibitor X
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About This Item
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质量水平
方案
≥97% (HPLC)
表单
crystalline solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
溶解性
ethanol: 1 mg/mL
DMSO: 3 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
[s]1c(ccc1c2[o]c(cc2)c3[s]c(cc3)CO)CO
InChI
1S/C14H12O3S2/c15-7-9-1-5-13(18-9)11-3-4-12(17-11)14-6-2-10(8-16)19-14/h1-6,15-16H,7-8H2
InChI key
KZENBFUSKMWCJF-UHFFFAOYSA-N
一般描述
A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53—MDM2 interaction and p53 ubiquitination and induces p53-dependent apoptosis in tumor cells expressing wild-type p53. Shown to restore the tumor suppressor function of p53 by inducing its accumulation in HCT116 colon carcinoma cells (~0.1 µM) and in p53-positive SCID mice xenografted with HCT116 cells (0.1, 1 or 10 mg/kg, ip) in vivo.
A cell-permeable, p53-targeting, tricyclic thiophene derivative that displays antitumor properties. Blocks p53—MDM2 interaction and p53 ubiquitination and induces p53-dependent apoptosis in tumor cells expressing wild-type p53. Shown to restore the tumor suppressor function of p53 by inducing its accumulation in HCT116 colon carcinoma cells (~0.1 µM) and in p53-positive SCID mice xenografted with HCT116 cells (0.1, 1 or 10 mg/kg, ip) in vivo.
生化/生理作用
Cell permeable: yes
Primary Target
p53
p53
Product does not compete with ATP.
Reversible: no
包装
Packaged under inert gas
警告
Toxicity: Irritant (B)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Grinkevich, V., et al. 2005. Nat. Med.11, 1136.
Krajewski, M., et al. 2005. Nat. Med.11, 1135.
Issaeva, N., et al. 2004. Nat. Med.10, 1321.
Nieves-Neira, W., et al. 1999. Mol. Pharmacol.56, 478.
Rivera, M.I., et al. 1999. Biochem. Pharmacol.57, 1283.
Krajewski, M., et al. 2005. Nat. Med.11, 1135.
Issaeva, N., et al. 2004. Nat. Med.10, 1321.
Nieves-Neira, W., et al. 1999. Mol. Pharmacol.56, 478.
Rivera, M.I., et al. 1999. Biochem. Pharmacol.57, 1283.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Shiwei Xie et al.
International journal of biological sciences, 17(9), 2367-2379 (2021-07-10)
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