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292168-79-7

中文名称 292168-79-7
英文名称 KY1220
CAS 292168-79-7
分子式 C14H10N4O3S
分子量 314.32
MOL 文件 292168-79-7.mol
更新日期 2024/03/01 14:56:22
292168-79-7 结构式 292168-79-7 结构式

基本信息

中文别名
5-((1-(4-硝基苯基)-1H-吡咯-2-基)亚甲基)-2-硫代咪唑烷-4-酮
英文别名
KY1220
KY 1220
KY-1220
KY1220
4-Imidazolidinone, 5-[[1-(4-nitrophenyl)-1H-pyrrol-2-yl]methylene]-2-thioxo-

物理化学性质

密度1.54±0.1 g/cm3(Predicted)
储存条件Keep in dark place,Inert atmosphere,2-8°C
溶解度DMSO:56.5(Max Conc. mg/mL);179.75(Max Conc. mM)
酸度系数(pKa)6.59±0.20(Predicted)
形态Solid
颜色Light yellow to yellow
292168-79-7价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-102028292168-79-7
KY1220
292168-79-71 mg321元
2025/05/22HY-102028292168-79-7
KY1220
292168-79-75mg866元
2025/05/22HY-102028292168-79-7
KY1220
292168-79-710mg1185元

常见问题列表

生物活性
KY1220 通过靶向 Wnt/β-catenin 通路,使得 β-catenin 和 Ras 的稳定性被破坏,其在HEK293 reporter细胞中的IC50值为2.1 μM。
靶点
TargetValue
Ras
()
Wnt/β-catenin
(HEK293 reporter cells-based assay)
2.1 μM
体外研究

KY1220 shows an IC 50 of 2.1 μM in HEK293 reporter cells. KY1220 dose dependently decreases Wnt3a-CM-induced TOPflash reporter activation and mRNA expression of Wnt target genes CCND1 and MYC in HEK293 cells. In HEK293 cells, both β-catenin and panRas protein levels are similarly reduced in a dose-dependent manner after treatment with KY1220, whereas the mRNA levels of CTNNB1 (which encodes β-catenin), NRAS, KRAS and HRAS remain unchanged. K-Ras, which has a critical role in progression of CRCs, is also destabilized by KY1220 via polyubiquitin-dependent proteasomal degradation. KY1220 accelerates the degradation rates of both β-catenin and Ras in SW480 cell lines. Ras destabilization by KY1220 consequently inhibits the activities of both ERK and Akt, which are downstream effectors of Ras in SW480 cells harboring a KRAS mutation. The proliferation and transformation of the HCT15, SW480, D-WT and D-MT CRC cells are efficiently inhibited after treatment with KY1220.

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