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PNU-74654

CAS号

113906-27-7

分子式

C19H16N2O3

主要靶点

Wnt/beta-catenin|Apoptosis

仅限科研使用

Cat No : CM06899

Print datasheet

Synonyms

Apoptosis|betacatenin|beta-catenin|bcatenin|Beta catenin|inhibit|Inhibitor|PNU74654|PNU-74654|PNU 74654|βcatenin|β-catenin|Wnt|Wnt/β-catenin|Wnt/b-catenin|Wnt/betacatenin

验证数据展示

  • CAS No.: 113906-27-7

    PNU-74654
    CAS#: 113906-27-7

产品信息

CAS号 113906-27-7
分子式 C19H16N2O3
主要靶点 Wnt/beta-catenin|Apoptosis
主要通路 干细胞|细胞骨架|凋亡
分子量 320.34
纯度 ≥95%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Apoptosis|betacatenin|beta-catenin|bcatenin|Beta catenin|inhibit|Inhibitor|PNU74654|PNU-74654|PNU 74654|βcatenin|β-catenin|Wnt|Wnt/β-catenin|Wnt/b-catenin|Wnt/betacatenin

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]。

溶解度

DMSO:30 mg/mL (93.65 mM)

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].

参考文献

1.Leal, Letícia F, Bueno A C , Gomes, Débora C, et al. Inhibition of the Tcf/beta-catenin complex increases apoptosis and impairs adrenocortical tumor cell proliferation and adrenal steroidogenesis[J]. Oncotarget, 2015, 6(40).
2.Durand J , Lampron A , Mazzuco T L , et al. Characterization of Differential Gene Expression in Adrenocortical Tumors Harboring β-Catenin ( CTNNB1 ) Mutations[J]. The Journal of Clinical Endocrinology and Metabolism, 2011, 96(7):E1206-11.

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