TOPK抑制剂(HI-TOPK-032)
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- CAS号:
- 487020-03-1
- 英文名:
- N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide
- 英文别名:
- HI-TOPK-32;HI-TOPK-032;HI-TOPK-032
(HI TOPK 032;HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor;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)-
- 中文名:
- TOPK抑制剂(HI-TOPK-032)
- 中文别名:
- 化合物HI-TOPK-032;TOPK抑制剂(HI-TOPK-032);HI TOPK 032,T-LAK细胞起源的蛋白激酶(TOPK)抑制剂
- CBNumber:
- CB42695998
- 分子式:
- C20H11N5OS
- 分子量:
- 369.4
- MOL File:
- 487020-03-1.mol
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TOPK抑制剂(HI-TOPK-032)化学性质
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沸点:
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415.3±45.0 °C(Predicted)
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密度:
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1.50±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble3mg/mL, clear (warmed)
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酸度系数(pKa):
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9.32±0.46(Predicted)
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形态:
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powder
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颜色:
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orange-brown
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TOPK抑制剂(HI-TOPK-032)性质、用途与生产工艺
HI-TOPK-032 是一种有效的、特异性的 TOPK 的抑制剂。HI-TOPK-032 还可以降低 ERK-RSK 磷酸化，调节 p53、裂化的 caspase-7 和裂化的 PARP 的丰度，并在癌细胞中诱导凋亡。
| Target | Value |
TOPK
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ERK-RSK
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p53
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Caspase-7
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PARP
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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.
TOPK抑制剂(HI-TOPK-032)
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 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 |
TOPK抑制剂(HI-TOPK-032)
生产厂家
487020-03-1, TOPK抑制剂(HI-TOPK-032) 相关搜索:
- Aromatics, Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds
- 药靶配体
- 细胞生物学试剂
- C20H11N5OS
- HI TOPK 032,T-LAK细胞起源的蛋白激酶(TOPK)抑制剂
- 化合物HI-TOPK-032
- TOPK抑制剂(HI-TOPK-032)
- 487020-03-1
- HITOPK032,inhibit,HI TOPK 032,TOPK,Inhibitor
- 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)-
- HI-TOPK-32
- HI-TOPK-032
- N-(12-Cyanindolizino[2,3-b]quinoxalin-2-yl)-2-thiophenecarboxaMide