中文名 | KY1220 |
英文名 | KY1220 |
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 |
英文别名 | KY1220 KY-1220 KY 1220 292168-79-7 4-Imidazolidinone, 5-[[1-(4-nitrophenyl)-1H-pyrrol-2-yl]methylene]-2-thioxo- |
CAS | 292168-79-7 |
化学式 | C14H10N4O3S |
分子量 | 314.32 |
溶解度 | DMSO: ≥ 100 mg/mL |
存储条件 | under inert gas (nitrogen or Argon) at 2–8 °C |
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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.181 ml | 15.907 ml | 31.815 ml |
5 mM | 0.636 ml | 3.181 ml | 6.363 ml |
10 mM | 0.318 ml | 1.591 ml | 3.181 ml |
5 mM | 0.064 ml | 0.318 ml | 0.636 ml |
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