292168-79-7
中文名称 | 292168-79-7 |
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中文同义词 | 5-((1-(4-硝基苯基)-1H-吡咯-2-基)亚甲基)-2-硫代咪唑烷-4-酮;化合物KY1220 |
英文名称 | KY1220 |
英文同义词 | KY1220;KY 1220;KY-1220;KY1220;4-Imidazolidinone, 5-[[1-(4-nitrophenyl)-1H-pyrrol-2-yl]methylene]-2-thioxo-;KY1220,Beta catenin,KY 1220,KY-1220,inhibit,Wnt,Inhibitor,β-catenin;5-((1-(4-Nitrophenyl)-1H-pyrrol-2-yl)methylene)-2-thioxoimidazolidin-4-one |
CAS号 | 292168-79-7 |
分子式 | C14H10N4O3S |
分子量 | 314.32 |
EINECS号 | |
相关类别 | |
Mol文件 | 292168-79-7.mol |
结构式 |
292168-79-7 性质
密度 | 1.54±0.1 g/cm3(Predicted) |
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储存条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
溶解度 | DMSO:56.5(最大浓度 mg/mL);179.75(最大浓度 mM) |
酸度系数(pKa) | 6.59±0.20(Predicted) |
形态 | 固体 |
颜色 | 浅黄至黄色 |
Target | Value |
Ras
() | |
Wnt/β-catenin
(HEK293 reporter cells-based assay) | 2.1 μM |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/08/19 | HY-102028 | 292168-79-7 KY1220 | 292168-79-7 | 2mg | 800元 |
2024/08/19 | HY-102028 | 292168-79-7 KY1220 | 292168-79-7 | 10mM * 1mLin DMSO | 1380元 |