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  3. 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).

For research use only. We do not sell to patients.

Thioridazine Chemical Structure

Thioridazine Chemical Structure

CAS No. : 50-52-2

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Thioridazine:

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  • Biological Activity

  • Purity & Documentation

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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].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
3.5 μM
Compound: thioridazine
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
HBL1 GI50
6.6 μM
Compound: Thioridazine
Antiproliferative activity against human HBL1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
Antiproliferative activity against human HBL1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
[PMID: 34181850]
HEK293 IC50
1.32 μM
Compound: Thioridazine
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit
[PMID: 22761000]
HEK293 IC50
1830 nM
Compound: Thioridazine
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA
[PMID: 21300721]
J774 IC50
4.1 μg/mL
Compound: 1; TZ
Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
[PMID: 28039773]
KG-1a IC50
6.01 μM
Compound: THD
Antiproliferative activity against human KG1a cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Antiproliferative activity against human KG1a cells assessed as reduction in cell viability incubated for 2 days by MTT assay
[PMID: 31541872]
L5178Y IC50
12.72 nM
Compound: TZ
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against mouse L5178Y cells assessed as reduction in cell viability by MTT assay
[PMID: 32871268]
L5178Y IC50
12.72 μM
Compound: TZ
Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 27156771]
L5178Y IC50
7.43 nM
Compound: TZ
Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
Cytotoxicity against multidrug resistance mouse L5178Y cells expressing human MDR1 assessed as reduction in cell viability by MTT assay
[PMID: 32871268]
L5178Y IC50
7.43 μM
Compound: TZ
Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against multi-drug resistant mouse L5178Y cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 27156771]
Macrophage cell line CC50
13.8 μM
Compound: TZ
Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
[PMID: 28964936]
MCF7 IC50
12.95 μM
Compound: THD
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
[PMID: 31541872]
MDA-MB-231 IC50
14.19 μM
Compound: THD
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
[PMID: 31541872]
MRC5 IC50
8.2 μg/mL
Compound: 1; TZ
Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
Cytotoxicity against human MRC5 cells assessed as decrease in cell viability after 24 hrs by resazurin reduction assay
[PMID: 28039773]
OCI-Ly1 GI50
13.4 μM
Compound: Thioridazine
Antiproliferative activity against human OCI-Ly1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
Antiproliferative activity against human OCI-Ly1 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
[PMID: 34181850]
PBMC IC50
13.78 μM
Compound: TZ
Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay
Cytotoxicity against human PBMC assessed as cell viability after 3 days by AlamarBlue assay
[PMID: 26197353]
SK-BR-3 IC50
18.23 μM
Compound: THD
Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Antiproliferative activity against human SKBR3 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
[PMID: 31541872]
SUM-159-PT IC50
14.51 μM
Compound: THD
Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Antiproliferative activity against human SUM159 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
[PMID: 31541872]
TMD8 GI50
5.9 μM
Compound: Thioridazine
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
Antiproliferative activity against human TMD8 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo luminescent assay
[PMID: 34181850]
Ventricular myocyte IC50
1.3 μM
Compound: Thioridazine
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
[PMID: 22761000]
Ventricular myocyte IC50
1300 nM
Compound: Thioridazine
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes
[PMID: 21300721]
Vero CC50
15.96 μM
Compound: Thioridazine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero IC50
17.79 μg/mL
Compound: Tz
Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
[PMID: 32526553]
Vero IC50
5.3 μg/mL
Compound: thioridazine
Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability by MTT assay
[PMID: 25238443]
Vero IC50
6.69 μM
Compound: Thioridazine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
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.
Appearance

Oil

Color

Colorless to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (269.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6985 mL 13.4927 mL 26.9855 mL
5 mM 0.5397 mL 2.6985 mL 5.3971 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6985 mL 13.4927 mL 26.9855 mL 67.4636 mL
5 mM 0.5397 mL 2.6985 mL 5.3971 mL 13.4927 mL
10 mM 0.2699 mL 1.3493 mL 2.6985 mL 6.7464 mL
15 mM 0.1799 mL 0.8995 mL 1.7990 mL 4.4976 mL
20 mM 0.1349 mL 0.6746 mL 1.3493 mL 3.3732 mL
25 mM 0.1079 mL 0.5397 mL 1.0794 mL 2.6985 mL
30 mM 0.0900 mL 0.4498 mL 0.8995 mL 2.2488 mL
40 mM 0.0675 mL 0.3373 mL 0.6746 mL 1.6866 mL
50 mM 0.0540 mL 0.2699 mL 0.5397 mL 1.3493 mL
60 mM 0.0450 mL 0.2249 mL 0.4498 mL 1.1244 mL
80 mM 0.0337 mL 0.1687 mL 0.3373 mL 0.8433 mL
100 mM 0.0270 mL 0.1349 mL 0.2699 mL 0.6746 mL
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    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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Product Name:
Thioridazine
Cat. No.:
HY-B0965A
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