1. Thioridazine

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).

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Thioridazine Chemical Structure

Thioridazine Chemical Structure

CAS No. : 50-52-2

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Description

Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].

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 G1 cell cycle arrest in cervical and endometrial cancer cells [4].
Thioridazine inhibits the growth of antibiotic-sensitive and multidrug-resistant strains of A. baumannii[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Clinical Trial
Molecular Weight

370.57

Formula

C21H26N2S2

CAS No.
SMILES

CSC(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Thioridazine
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HY-B0965A
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