292168-79-7
基本信息
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)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-102028 | 292168-79-7 KY1220 | 292168-79-7 | 2mg | 800元 |
2024/11/08 | HY-102028 | 292168-79-7 KY1220 | 292168-79-7 | 10mM * 1mLin DMSO | 1380元 |
2024/11/08 | HY-102028 | 292168-79-7 KY1220 | 292168-79-7 | 5mg | 1500元 |
常見問題列表
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.