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PNU-74654 纯度: 99.42%
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。
PNU-74654 Chemical Structure
CAS No. : 113906-27-7
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥583 | In-stock | |
5 mg | ¥530 | In-stock | |
10 mg | ¥770 | In-stock | |
25 mg | ¥1700 | In-stock | |
50 mg | ¥3000 | In-stock | |
100 mg | ¥5500 | In-stock | |
200 mg | ¥8100 | In-stock | |
500 mg | 询价 | ||
1 g | 询价 |
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PNU-74654 相关产品
•相关化合物库:
- Bioactive Compound Library Plus
- Apoptosis Compound Library
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- Wnt/Hedgehog/Notch Compound Library
- Anti-Cancer Compound Library
- Anti-Aging Compound Library
- Differentiation Inducing Compound Library
- Cytoskeleton Compound Library
- Neuroprotective Compound Library
- Anti-Breast Cancer Compound Library
- Transcription Factor Targeted Library
- Anti-Liver Cancer Compound Library
- Anti-Colorectal Cancer Compound Library
生物活性 |
PNU-74654 is an inhibitor of Wnt/β-catenin pathway with an IC50 of 129.8 μM in NCI-H295 cell. |
IC50 & Target |
129.8 μM (Wnt/β-catenin, NCI-H295 cell)[1] |
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体外研究 (In Vitro) |
PNU-74654 binds to β-catenin with a KD 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[2]. 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[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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分子量 |
320.34 |
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Formula |
C19H16N2O3 |
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CAS 号 |
113906-27-7 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : ≥ 30 mg/mL (93.65 mM) * “≥” means soluble, but saturation unknown. 配制储备液
*
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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
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参考文献 |
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Cell Assay [1] |
The PNU-74654 compound is dissolved in DMSO at stock concentrations of 31.2 mM. For working solutions, PNU-74654 is diluted 100X in growth medium with no serum deprivation. NCI-H295 cells are plated at 200,000 cells per well in 24-well plates for gene expression, protein analysis and adrenal steroid measurements. After 48 h, cells are treated with vehicle (0.1%-0.4% DMSO) or 10, 50, 100 and 200 μM PNU-74654. After 24 and 48 h, medium supernatants are collected for adrenal steroid measurements[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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参考文献 |
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