Thioridazine 是一种具有口服活性的多巴胺受体D2家族蛋白的拮抗剂，具有有效的抗焦虑活性。Thioridazine 也是一种有效的PI3K-Akt-mTOR信号通路的抑制剂，具有抗血管生成作用。Thioridazine 在多种类型的癌细胞中显示出抗增殖和凋亡诱导作用，对靶向癌症干细胞 (CSCs) 具有特异性。
| 生物活性 | Thioridazine, an antagonist of thedopamine receptorD2family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor ofPI3K-Akt-mTORsignaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative andapoptosisinduction effects in various types ofcancercells, with specificity on targetingcancer stem cells(CSCs)[1][2][3][4]. |
体外研究
(In Vitro) | Thioridazine (0.01-100 μM; 48 h) reduces the cell viability of NCI-N87 and AGS cells in a concentration-dependent manner[2].
Thioridazine (15 μM; 24 h) reduces cell viability of the cervical (HeLa, Caski and C33A) and endometrial (HEC-1-A and KLE) cancer cells[4].
Thioridazine (1-15 μM; 24-48 h) induces gastric cancer cell death via the mitochondrial apoptosis pathway and mitochondrial pathway[2].
Thioridazine (15 μM; 24 h) modulates the regulation of cell cycle progression by interfering with the PI3K/Akt pathway and induces G1cell cycle arrest in cervical and endometrial cancer cells[4].
Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains ofA. baumannii[3].
Cell Viability Assay[1] | Cell Line: | NCI-N87 and AGS cells. | | Concentration: | 0.01, 0.1, 0.5, 1, 5, 10, 20, 50, 100 μM. | | Incubation Time: | 48 hours. | | Result: | Exhibited cytotoxicity in gastric cancer cells. |
Western Blot Analysis[1] | Cell Line: | NCI-N87 and AGS cells | | Concentration: | 1, 5, 10, 15 μM. | | Incubation Time: | 24, 48 hours. | | Result: | Downregulated the precursors of caspase-9, caspase-8 and caspase-3. |
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体内研究
(In Vivo) | Thioridazine (25 mg/kg; i.p. every 3 days for 3 weeks) extends the survival of tumor-bearing mice and reduces the number of pluripotent embryonal carcinoma (EC) cells within tumors[5].
Thioridazine (1.0-5.0 mg/kg; s.c.) reduces oral behavior and selectively blocks repetitive head bobbing[1].
| Animal Model: | Nude and Rag2KO mice were injected with iPS cells or NT2D1 cells[5] | | Dosage: | 25 mg/kg. | | Administration: | I.p. every 3 days for 3 weeks. | | Result: | Reduced the number of OCT4-expressing cells within malignant teratocarcinomas and extended the survival of tumor-bearing mice.
With no effect on fertility. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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