292168-79-7
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- CAS号:
- 292168-79-7
- 英文名:
- KY1220
- 英文别名:
- KY1220;KY 1220;KY-1220;KY1220;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;4-Imidazolidinone, 5-[[1-(4-nitrophenyl)-1H-pyrrol-2-yl]methylene]-2-thioxo-
- 中文名:
- 292168-79-7
- 中文别名:
- 化合物KY1220;5-((1-(4-硝基苯基)-1H-吡咯-2-基)亚甲基)-2-硫代咪唑烷-4-酮
- CBNumber:
- CB63356162
- 分子式:
- C14H10N4O3S
- 分子量:
- 314.32
- MOL File:
- 292168-79-7.mol
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292168-79-7化学性质
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密度:
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1.54±0.1 g/cm3(Predicted)
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储存条件:
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under inert gas (nitrogen or Argon) at 2–8 °C
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溶解度:
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DMSO:56.5(Max Conc. mg/mL);179.75(Max Conc. mM)
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酸度系数(pKa):
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6.59±0.20(Predicted)
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292168-79-7性质、用途与生产工艺
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。
| Target | Value |
Ras
()
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Wnt/β-catenin
(HEK293 reporter cells-based assay)
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2.1 μM
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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.
292168-79-7
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-102028 | 292168-79-7
KY1220 | 292168-79-7 | 2mg | 800元 |
| 2024/01/25 | HY-102028 | 292168-79-7
KY1220 | 292168-79-7 | 10mM * 1mLin DMSO | 1380元 |
292168-79-7, 292168-79-7 相关搜索:
- 药靶配体
- 化合物KY1220
- 5-((1-(4-硝基苯基)-1H-吡咯-2-基)亚甲基)-2-硫代咪唑烷-4-酮
- 292168-79-7
- 5-((1-(4-Nitrophenyl)-1H-pyrrol-2-yl)methylene)-2-thioxoimidazolidin-4-one
- KY1220,Beta catenin,KY 1220,KY-1220,inhibit,Wnt,Inhibitor,β-catenin
- 4-Imidazolidinone, 5-[[1-(4-nitrophenyl)-1H-pyrrol-2-yl]methylene]-2-thioxo-
- KY 1220;KY-1220;KY1220
- KY1220