TOPK抑制剂(HI-TOPK-032)
| 中文名称 | TOPK抑制剂(HI-TOPK-032) |
|---|---|
| 中文同义词 | TOPK抑制剂(HI-TOPK-032);化合物HI-TOPK-032;HI TOPK 032,T-LAK细胞起源的蛋白激酶(TOPK)抑制剂;化合物HI-TOPK-032,10 MM DMSO 溶液;N-(12-氰基吲哚嗪[2,3-b]喹喔啉-2-基)-2-噻吩甲酰胺 |
| 英文名称 | N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide |
| 英文同义词 | N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide;HI-TOPK-032;HI-TOPK-32;N-(12-Cyanoindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxamide;HI-TOPK-032 (HI TOPK 032;2-Thiophenecarboxamide, N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)-;HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor;HI-TOPK-032, 10 mM in DMSO |
| CAS号 | 487020-03-1 |
| 分子式 | C20H11N5OS |
| 分子量 | 369.4 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds |
| Mol文件 | 487020-03-1.mol |
| 结构式 |  |
TOPK抑制剂(HI-TOPK-032) 性质
| 沸点 | 415.3±45.0 °C(Predicted) |
|---|---|
| 密度 | 1.50±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | DMSO：可溶，3mg/mL，澄清（加热） |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.32±0.46(Predicted) |
| 颜色 | 橙褐色 |
| InChI | 1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26) |
| InChIKey | BCSBXWKRZUPFHW-UHFFFAOYSA-N |
| SMILES | [s]1c(ccc1)C(=O)Nc2cc3[n](c4nc5c(nc4c3C#N)cccc5)cc2 |
| 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.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-101550 | TOPK抑制剂(HI-TOPK-032) HI-TOPK-032 | 487020-03-1 | 5mg | 750元 |
| 2025/12/22 | HY-101550 | TOPK抑制剂(HI-TOPK-032) HI-TOPK-032 | 487020-03-1 | 10mg | 1200元 |