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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
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
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
Nature, 533(7601), 86-89 (2016-04-26)
The evolution of novel cell types led to the emergence of new tissues and organs during the diversification of animals. The origin of the chondrocyte, the cell type that synthesizes cartilage matrix, was central to the evolution of the vertebrate
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)
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
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