基本信息

产品描述

FH535是一种Wnt/β-catenin信号传导抑制剂，同时也是PPARγ和PPARδ的双重拮抗剂。

靶点（IC50 & Targe）

PPARγ

PPARδ

Wnt/β-catenin

体外研究

FH535拮抗β-连环蛋白/Tcf介导的转录，并抑制共激活剂GRIP1和β-连环蛋白对PPARδ 和 PPAR的聚集作用。对某些表达较高的或活跃的Wnt/β-连环蛋白通路癌细胞，FH535表现出选择性抗增殖作用。[1] FH535增加香烟烟雾冷凝液的细胞毒性，并引起β-连环蛋白和EGR-1信号的改变。[2]以肝癌干细胞和肝细胞癌细胞系为靶点，FH535在肝癌治疗中具有潜在治疗价值。[3]

激酶实验

FH535拮抗β-连环蛋白/Tcf介导的转录，并抑制共激活剂GRIP1和β-连环蛋白对PPARδ 和 PPAR的聚集作用。对某些表达较高的或活跃的Wnt/β-连环蛋白通路癌细胞，FH535表现出选择性抗增殖作用。[1] FH535增加香烟烟雾冷凝液的细胞毒性，并引起β-连环蛋白和EGR-1信号的改变。[2]以肝癌干细胞和肝细胞癌细胞系为靶点，FH535在肝癌治疗中具有潜在治疗价值。[3]

细胞实验

Cell lines: HCT116，SW48，RKO，LoVo，COLO205，IEC6，A427，HCC15，NCI-H1703，A549，HepG2，Hep3b，Huh7，成纤维细胞

Concentrations: 30 μM

Incubation Time: 48小时

Method: 细胞活性通过改进的3H-胸腺嘧啶整合试验测定。简而言之，细胞接种在96孔微板上培养24小时，并用不同浓度的测试化合物以一式三份进行处理。化合物接触48小时后，细胞在不含化合物的培养基中再培养48小时。然后细胞在包含3H-胸腺嘧啶的培养基中培养24小时，在96孔板中用闪烁液洗涤并混合。各孔中细胞用96孔闪烁计数器计数，并计算LC5。

(Only for Reference)

参考文献

[1] Handeli S, et al. Mol Cancer Ther. 2008, 7(3), 521-529.

[2] Polk WW. Int J Toxicol. 2012, 31(4), 380-389.

[3] Gedaly R, et al. PLoS One. 2014, 9(6), e99272.

安全信息

图形或危害标志
提示语	Danger
危险说明	H302 H318
防范说明	P280 P305+P351+P338
WGK	3

产品说明

一般描述

A cell-permeable sulfonamide compound that acts as a dual pathway inhibitor against Wnt/β-catenin (≥80% inhibition at 15 µM in β-catenin/Tcf-dependent cellular reporter assays) and PPARγ/δ (≥30% inhibition at 0.5 µM in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARγ-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks β-catenin/PPARγ interaction and the antagonistic activity of FH535 does not involve the covalent modification of or non-covalent interaction with the PPAR ligand-binding site cystein residue that is crucial for GW9662 action.
A cell-permeable sulfonamide compound that acts as a dual pathway inhibitor against Wnt/β-catenin (≥80% inhibition at 15 µM in β-catenin/Tcf-dependent cellular reporter assays) and PPARγ/δ (≥30% inhibition at 0.5 µM in PPRE cellular reporter assays) signalings. Although both FH535 and the structurally similar PPARγ-selective inhibitor GW9662 (Cat. No. 370700) inhibit coactivator/PPAR binding, only FH535 blocks β-catenin/PPARγ interaction and the antagonistic activity of FH535 does not involve the covalent modification of or non-covalent interaction with the PPAR ligand-binding site cystein residue that is crucial for GW9662 action.

包装

10 mg in Plastic ampoule
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Handeli, S., and Simon, J.A. 2008. Mol. Cancer Ther.7, 521.

法律信息

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

基本信息

产品性质

安全信息