487020-03-1
487020-03-1 结构式
基本信息
HI-TOPK-032
HI-TOPK-032 (HI TOPK 032
N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide
2-Thiophenecarboxamide, N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-
物理化学性质
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/04/30 | HY-101550 | TOPK抑制剂(HI-TOPK-032) HI-TOPK-032 | 487020-03-1 | 5mg | 750元 |
| 2024/04/30 | HY-101550 | TOPK抑制剂(HI-TOPK-032) HI-TOPK-032 | 487020-03-1 | 10mg | 1200元 |
| 2024/04/30 | S6882 | TOPK抑制剂(HI-TOPK-032) HI-TOPK-032 | 487020-03-1 | 5mg | 1270.23元 |
常见问题列表
| Target | Value |
|
TOPK
() | |
|
ERK-RSK
() | |
|
p53
() | |
|
Caspase-7
() | |
|
PARP
() |
HI-TOPK-032 strongly suppresses TOPK kinase activity but has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 also inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP.
Treatment of mice with 1 or 10 mg/kg of HI-TOPK-032 significantly inhibits HCT-116 tumor growth by more than 60% relative to the vehicle-treated group. Mice are well tolerated with HI-TOPK-032 treatment. The expression of p53 is strongly induced, and phosphorylation of ERK and RSK, a direct downstream protein of ERK, is markedly inhibited in the HI-TOPK-032-treated group.