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- 2025年07月12日
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- 详细信息
- 技术资料
- 保存条件：
-20°C, sealed storage, away from moisture
- 英文名：
Endothal
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- 规格：
5 mg
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Endothall
CAS No. : 145-73-3
MCE 国际站：Endothall
产品活性：Endothall (Endothal) 是一种蛋白磷酸酶 2A (PP2A) 抑制剂，对 PP2A 和 PP1 的 IC50 分别为 90 nM 和 5 µM。Endothall 可用作除草剂。Endothall 在癌症化疗中也很有用。
研究领域：Metabolic Enzyme/Protease
作用靶点：Phosphatase
In Vitro: Endothall, an organic acid, is the least toxic structural analogue of Cantharidin that still inhibits PP2A.
Endothall inhibits preferentially hepatocellular carcinoma (HCC) growth and these new rat hepatocellular carcinoma lines may be useful for further biochemical and pharmacological studies on PP2A inhibitors, and for testing new forms of treatment of hepatic cell carcinomas. The HR-2, HR-3, HR-4, and Zajdela hepatocellular carcinomas are most sensitive to Endothall (IC50 of 1.7, 1.2, 0.9, and 1.7 µg/mL), whereas newborn rat hepatocytes growing exponentially in primary culture (IC50=6.2 µg/mL), rat DHD/K12 colon carcinoma cells (IC50=3.6 µg/mL), or human HT-29 colon carcinoma cells (IC50=4.9 µg/mL) were less sensitive.
Endothall inhibits the growth of HCC lines in culture more than that of normal hepatocytes or colon carcinomas, inducing mitotic arrest, followed by cell death. Endothall causes dose- and time-dependent cytostasis specifically in G2/M.
Endothall (3 µg/mL) inhibits the cell cycle at G2/M and subsequent apoptotic cell death.
In Vivo: Endothall exhibits acute LD50 of 14 mg/kg in mice.
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