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292168-79-7

中文名稱 292168-79-7
英文名稱 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 結(jié)構(gòu)式 292168-79-7 結(jié)構(gòu)式

基本信息

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

物理化學性質(zhì)

密度1.54±0.1 g/cm3(Predicted)
儲存條件Keep in dark place,Inert atmosphere,2-8°C
溶解度DMSO:56.5(Max Conc. mg/mL);179.75(Max Conc. mM)
酸度系數(shù)(pKa)6.59±0.20(Predicted)
形態(tài)Solid
顏色Light yellow to yellow
292168-79-7價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-102028292168-79-7
KY1220
292168-79-72mg800元
2024/11/08HY-102028292168-79-7
KY1220
292168-79-710mM * 1mLin DMSO1380元
2024/11/08HY-102028292168-79-7
KY1220
292168-79-75mg1500元

常見問題列表

生物活性
KY1220 通過靶向 Wnt/β-catenin 通路,使得 β-catenin 和 Ras 的穩(wěn)定性被破壞,其在HEK293 reporter細胞中的IC50值為2.1 μM。
靶點
TargetValue
Ras
()
Wnt/β-catenin
(HEK293 reporter cells-based assay)
2.1 μM
體外研究

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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