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PNU 74654是一种Wnt/β-catenin 通路抑制剂,在NCI-H295 细胞中的IC50值为129.8 μM。
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PNU 74654是一种Wnt/β-catenin 通路抑制剂,在NCI-H295 细胞中的IC50值为129.8 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 172 | 现货 | |
5 mg | ¥ 438 | 现货 | |
10 mg | ¥ 638 | 现货 | |
25 mg | ¥ 1,390 | 现货 | |
50 mg | ¥ 2,490 | 现货 | |
100 mg | ¥ 3,770 | 现货 | |
200 mg | ¥ 5,390 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 483 | 现货 |
产品描述 | PNU 74654 binds to β-catenin (Kd = 450 nM), inhibiting its interaction with the transcription factor T cell factor 4 (Tcf4) resulting in disruption of the Wnt signaling pathway. |
靶点活性 | Wnt/β-catenin (NCI-H295 cells):129.8 μM |
体外活性 | 在NCI-H295细胞中,PNU 74654在治疗后96小时显著降低了细胞增殖,增加了早期和晚期凋亡,降低了核内beta-catenin积累,损害了CTNNB1/beta-catenin表达,并在治疗后48小时提高了beta-catenin目标基因的表达。HeLa细胞未观察到效应。在NCI-H295细胞中,PNU 74654在治疗后24小时和48小时降低了cortisol、testosterone和androstenedione的分泌。此外,在NCI-H295细胞中,PNU 74654在治疗后48小时降低了SF1和CYP21A2 mRNA的表达,以及STAR和aldosterone synthase的蛋白水平。在Y1细胞中,PNU 74654在治疗后24小时损害了corticosterone分泌,但未减少细胞活力[1]。 |
细胞实验 | Adrenal (NCI-H295 and Y1) and non-adrenal (HeLa) cell lines were treated with PNU 74654 (5-200 μM) for 24-96 h to assess cell viability (MTS-based assay), apoptosis (Annexin V), expression/localization of beta-catenin (qPCR, immunofluorescence, immunocytochemistry and western blot), expression of beta-catenin target genes (qPCR and western blot), and adrenal steroidogenesis (radioimmunoassay, qPCR and western blot)[1]. |
分子量 | 320.34 |
分子式 | C19H16N2O3 |
CAS No. | 113906-27-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 30 mg/mL (93.65 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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