PNU 74654,2-PHENOXYBENZOICACID-[(5-METHYL-2-FURANYL)METHYLEN

中文名称:

PNU 74654,2-PHENOXYBENZOICACID-[(5-METHYL-2-FURANYL)METHYLENE]HYDRAZIDE

中文同义词:

WNT/Β-CATENIN通路抑制剂(PNU-74654)

英文名称:

2-Phenoxybenzoicacid-[(5-methyl-2-furanyl)methylene]hydrazide

英文同义词:

2-Phenoxybenzoicacid-[(5-methyl-2-furanyl)methylene]hydrazide;PNU 74654;Benzoic acid, 2-phenoxy-, 2-[(5-methyl-2-furanyl)methylene]hydrazide;PNU 74654,2-Phenoxybenzoicacid-[(5-methyl-2-furanyl)methylene]hydrazide;PNU74654; PNU 74654;CS-2563

CAS号:

113906-27-7

分子式:

C19H16N2O3

分子量:

320.34

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

113906-27-7.mol

密度 

1.17±0.1 g/cm3(Predicted)

储存条件 

2-8°C

溶解度 

DMSO: >10mg/mL

形态

solid

酸度系数(pKa)

12.12±0.46(Predicted)

颜色

white to off-white

生物活性

PNU-74654是Wnt/β-catenin通路的的抑制剂，在NCI-H295 细胞中的IC50值为129.8 μM。

靶点

129.8 μM (Wnt/β-catenin, NCI-H295 cell)

体外研究

PNU-74654 binds to β-catenin with a K D of 450 nM. The Tcf3/Tcf4-binding surface on β-catenin contains a well-defined hot spot around residues K435 and R469. The binding mode of PNU-74654 involves the two narrow pockets on either side of this hot spot. In NCI-H295 cells,PNU-74654 significantly decreases cell proliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-catenin accumulation, impairs CTNNB1/beta-catenin expression and increases beta-catenin target genes 48 h after treatment. No effects are observed on HeLa cells. In NCI-H295 cells, PNU-74654 decreases cortisol, testosterone and androstenedione secretion 24 and 48 h after treatment. The SF1 and CYP21A2 mRNA expression as well as the protein levels of STAR and aldosterone synthase are decreased in NCI-H295 cells after 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h after treatment but does not decrease cell viability.

危险品标志 

Xn

危险类别码 

22

WGK Germany 

3