PNU-74654 _Wnt 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPNU-74654Cat. No.: HY-101130CAS No.: 113906-27-7分式: CHNO分量: 320.34作靶点: Wnt; -catenin作通路: Stem Cell/Wnt储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 30 mg/mL (93.65 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.1217 mL 15.6084 mL 31.2168 mL5 mM 0.6243 mL 3.1217 mL 6.2434 mL10 mM 0.3122 mL 1.5608 mL 3.1217 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储

3、备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.80 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (7.80 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性

4、PNU-74654是Wnt/-catenin通路的的抑制剂，在NCI-H295 细胞中的IC50值为129.8 M。IC50 & Target 129.8 M (Wnt/-catenin, NCI-H295 cell) 1体外研究 PNU-74654 binds to -catenin with a KD of 450 nM. The Tcf3/Tcf4-binding surface on -catenin contains awell-defined hot spot around residues K435 and R469. The binding mode of PNU-74654

5、involves the twonarrow pockets on either side of this hot spot 2. In NCI-H295 cells,PNU-74654 significantly decreases cellproliferation 96 h after treatment, increases early and late apoptosis, decreases nuclear beta-cateninaccumulation, impairs CTNNB1/beta-catenin expression and increases beta-cate

6、nin target genes 48 h aftertreatment. 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 mRNAexpression as well as the protein levels of STAR and aldosterone synthase are d

7、ecreased in NCI-H295 cellsafter 48 h PNU-74654 treatment. In Y1 cells, PNU-74654 impairs corticosterone secretion 24 h aftertreatment but does not decrease cell viability 1.PROTOCOLCell Assay 1 The PNU-74654 compound is dissolved in DMSO at stock concentrations of 31.2 mM. For working solutions,PNU-

8、74654 is diluted 100X in growth medium with no serum deprivation. NCI-H295 cells are plated at200,000 cells per well in 24-well plates for gene expression, protein analysis and adrenal steroidmeasurements. After 48 h, cells are treated with vehicle (0.1%-0.4% DMSO) or 10, 50, 100 and 200 MPNU-74654.

9、 After 24 and 48 h, medium supernatants are collected for adrenal steroid measurements 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 J Cell Physiol. 2019 Jan 26.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Leal L

10、F, et al. Inhibition of the Tcf/beta-catenin complex increases apoptosis and impairs adrenocortical tumor cell proliferation andadrenal steroidogenesis. Oncotarget. 2015 Dec 15;6(40):43016-32.2. Trosset JY, et al. Inhibition of protein-protein interactions: the discovery of druglike beta-catenin inhibitors by combining virtual andbiophysical screening. Proteins. 2006 Jul 1;64(1):60-7.McePdfHeightCaution: Product has not been fully