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品質等級
化驗
≥98% (HPLC)
形狀
solid
顏色
white to off-white
溶解度
DMSO: >10 mg/mL
儲存溫度
2-8°C
SMILES 字串
Cc1ccc(\C=N\NC(=O)c2ccccc2Oc3ccccc3)o1
InChI
1S/C19H16N2O3/c1-14-11-12-16(23-14)13-20-21-19(22)17-9-5-6-10-18(17)24-15-7-3-2-4-8-15/h2-13H,1H3,(H,21,22)/b20-13+
InChI 密鑰
JJEDWBQZCRESJL-DEDYPNTBSA-N
應用
PNU-74654已被:
- 作为β-连环蛋白信号转导抑制剂,研究对乌贼胚漏斗软骨分化的影响
- 作为Wnt信号抑制剂,研究其对前列腺癌细胞系糖原合成酶激酶3 (GSK-3)的抑制作用
- 作为Wnt信号通路抑制剂,研究其对瘦素诱导的乳腺癌细胞增殖的影响
生化/生理作用
PNU-74654 通过阻断 β-连环蛋白和 TCF(T 细胞因子)抑制 Wnt-β。PNU-74654 也是一种抗肿瘤药物。Wnt /β-catenin通路(经典通路)的异常激活通过β-catenin和T细胞因子(TCF)之间的相互作用参与驱动不同肿瘤(如结肠癌)的发生/发展,T细胞因子分解细胞增殖和分化中靶基因的表达。在癌细胞系中抑制该通路活性可有效阻断其生长。PNU-74654通过抑制β-catenin和TCF之间的相互作用抑制该通路。
訊號詞
Warning
危險聲明
危險分類
Acute Tox. 4 Oral
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
Oncotarget, 6(40), 43016-43032 (2015-10-31)
To date, there is no effective therapy for patients with advanced/metastatic adrenocortical cancer (ACC). The activation of the Wnt/beta-catenin signaling is frequent in ACC and this pathway is a promising therapeutic target. To investigate the effects of the inhibition of
Biochemical and biophysical research communications, 525(3), 563-569 (2020-03-03)
Supercentenarians (≥110-year-old, SC) are a uniquely informative population not only because they surpass centenarians in age, but because they appear to age more slowly with fewer incidences of chronic age-related disease than centenarians. We reprogramed donor B-lymphoblastoid cell lines (LCL)
International immunopharmacology, 32, 118-124 (2016-01-30)
Many tumors are characterized by mutation-induced constitutive activation of β-catenin which promotes tumor growth and survival. Consequently, the development of specific β-catenin inhibitors for tumor therapy has come into the focus of drug development. β-Catenin was also shown to contribute
Cancer research, 78(16), 4533-4548 (2018-06-20)
MAPK signaling pathways are constitutively active in colon cancer and also promote acquired resistance to MEK1 inhibition. Here, we demonstrate that BRAFV600E -mutated colorectal cancers acquire resistance to MEK1 inhibition by inducing expression of the scaffold protein CEMIP through a
Journal of thrombosis and haemostasis : JTH, 14(11), 2261-2273 (2016-08-23)
Essentials Polyphosphate (polyP) activates mTOR but its role in Wnt/β-catenin signaling is not known. PolyP-mediated cyclin D1 expression (β-catenin target gene) was monitored in endothelial cells. PolyP and boiled platelet-releasates induced the expression of cyclin D1 by similar mechanisms. PolyP
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