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Endothall

CAS No. : 145-73-3

MCE 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 M。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 g/mL), whereas newborn rat hepatocytes growing exponentially in primary culture (IC₅₀=6.2 g/mL), rat DHD/K12 colon carcinoma cells (IC₅₀=3.6 g/mL), or human HT-29 colon carcinoma cells (IC₅₀=4.9 g/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 g/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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