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K-80003(TX-803)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
K-80003(TX-803)图片
CAS NO:1292821-90-9
规格:98%
分子量:336.4
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
K-80003有效抑制tRXRα依赖性的Akt激活和肿瘤细胞生长。
CAS:1292821-90-9
分子式:C22H21FO2
分子量:336.4
纯度:98%
存储:Store at -20°C

Background:

K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.


When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions[2].


K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity[1].


[1]. Zhou H, et al. NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling. Cancer Cell. 2010 Jun 15;17(6):560-73. [2]. Chen L, et al. Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα. Nat Commun. 2017 Jul 17;8:16066.