Thioridazine
Based on 5 publication(s) in Google Scholar
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.
- Purity: 99.50%
- CAS No.: 50-52-2
- Formula: C21H26N2S2
- Molecular Weight:370.57
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Thioridazine
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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Microbiological Assay
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Microbiological Assay
All Dopamine Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.5 μM
Compound: thioridazine
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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
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[PMID: 23812503] |
| HBL1 | GI50 |
6.6 μM
Compound: Thioridazine
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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
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[PMID: 34181850] |
| HEK293 | IC50 |
1.32 μM
Compound: Thioridazine
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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
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[PMID: 22761000] |
| HEK293 | IC50 |
1830 nM
Compound: Thioridazine
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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
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[PMID: 21300721] |
| J774 | IC50 |
4.1 μg/mL
Compound: 1; TZ
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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
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[PMID: 28039773] |
| KG-1a | IC50 |
6.01 μM
Compound: THD
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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
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[PMID: 31541872] |
| L5178Y | IC50 |
12.72 nM
Compound: TZ
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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
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[PMID: 32871268] |
| L5178Y | IC50 |
12.72 μM
Compound: TZ
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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
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[PMID: 27156771] |
| L5178Y | IC50 |
7.43 nM
Compound: TZ
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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
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[PMID: 32871268] |
| L5178Y | IC50 |
7.43 μM
Compound: TZ
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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
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[PMID: 27156771] |
| Macrophage cell line | CC50 |
13.8 μM
Compound: TZ
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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
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[PMID: 28964936] |
| MCF7 | IC50 |
12.95 μM
Compound: THD
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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
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[PMID: 31541872] |
| MDA-MB-231 | IC50 |
14.19 μM
Compound: THD
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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
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[PMID: 31541872] |
| MRC5 | IC50 |
8.2 μg/mL
Compound: 1; TZ
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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
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[PMID: 28039773] |
| OCI-Ly1 | GI50 |
13.4 μM
Compound: Thioridazine
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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
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[PMID: 34181850] |
| PBMC | IC50 |
13.78 μM
Compound: TZ
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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
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[PMID: 26197353] |
| SK-BR-3 | IC50 |
18.23 μM
Compound: THD
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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
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[PMID: 31541872] |
| SUM-159-PT | IC50 |
14.51 μM
Compound: THD
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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
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[PMID: 31541872] |
| TMD8 | GI50 |
5.9 μM
Compound: Thioridazine
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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
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[PMID: 34181850] |
| Ventricular myocyte | IC50 |
1.3 μM
Compound: Thioridazine
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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
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[PMID: 22761000] |
| Ventricular myocyte | IC50 |
1300 nM
Compound: Thioridazine
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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
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[PMID: 21300721] |
| Vero | CC50 |
15.96 μM
Compound: Thioridazine
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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
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
17.79 μg/mL
Compound: Tz
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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
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[PMID: 32526553] |
| Vero | IC50 |
5.3 μg/mL
Compound: thioridazine
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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
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[PMID: 25238443] |
| Vero | IC50 |
6.69 μM
Compound: Thioridazine
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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
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10.1101/2020.03.20.999730 |
| Vero C1008 | IC50 |
6.24 μM
Compound: Thioridazine
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Antiviral activity against Ebolavirus expressing eGFP infected in African green monkey Vero E6 cells assessed as inhibition of viral replication after 48 hrs by spectrofluorometric method
Antiviral activity against Ebolavirus expressing eGFP infected in African green monkey Vero E6 cells assessed as inhibition of viral replication after 48 hrs by spectrofluorometric method
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[PMID: 29741894] |
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.
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Cell Line:NCI-N87 and AGS cells.
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Concentration:0.01, 0.1, 0.5, 1, 5, 10, 20, 50, 100 μM.
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Incubation Time:48 hours.
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Result:Exhibited cytotoxicity in gastric cancer cells.
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Cell Line:NCI-N87 and AGS cells
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Concentration:1, 5, 10, 15 μM.
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Incubation Time:24, 48 hours.
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Result:Downregulated the precursors of caspase-9, caspase-8 and caspase-3.
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.
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Animal Model:Nude and Rag2KO mice were injected with iPS cells or NT2D1 cells[5]
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Dosage:25 mg/kg.
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Administration:I.p. every 3 days for 3 weeks.
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Result:Reduced the number of OCT4-expressing cells within malignant teratocarcinomas and extended the survival of tumor-bearing mice.
With no effect on fertility.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 50-52-2
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Appearance Oil
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Molecular Weight 370.57
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Formula C21H26N2S2
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Color Colorless to off-white
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SMILES
CSC(C=C1N2CCC3N(C)CCCC3)=CC=C1SC4=C2C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
The combination of cloxacillin, thioridazine and tetracycline protects mice against Staphylococcus aureus peritonitis by inhibiting α-Hemolysin-induced MAPK/NF-κB/NLRP3 activation. [Abstract]2022 Feb 15:198:1-10. PMID: 34963621 -
Br J Cancer
DRD4 promotes chemo-resistance and cancer stem cell-like phenotypes by mediating the activation of the Akt/β-catenin signaling axis in liver cancer. [Abstract]2024 Oct;131(7):1212-1223. PMID: 39174739
Thioridazine purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2024 Oct;131(7):1212-1223. [Abstract]
HepG2-R cells were seeded at a density of 3 × 103 cells per well in 96-well plates and cultured overnight. The cells were exposed to 250 nM and 500 nM adriamycin (ADR) and 20 μM Thioridazine hydrochloride (TDZ) either individually or in combination for a duration of 48 h. The viability of these cells was assessed using an MTS assay, measuring the optical density at 490 nm (OD490 value).
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Int J Mol Sci
Miltefosine and Nifuratel Combination: A Promising Therapy for the Treatment of Leishmania donovani Visceral Leishmaniasis. [Abstract]2023 Jan 13;24(2):1635. PMID: 36675150 -
Pol J Microbiol
Inhibition of Drug Resistance of Staphylococcus aureus by Efflux Pump Inhibitor and Autolysis Inducer to Strengthen the Antibacterial Activity of β-lactam Drugs. [Abstract]2019 Dec;68(4):477-491. PMID: 31880892
Thioridazine purchased from MedChemExpress. Usage Cited in: Pol J Microbiol. 2019 Dec;68(4):477-491. [Abstract]
In the MRSA-infected groups, the mammary glands varied in color; those of the blank control group were milky white, those of the infection control group were purple, those of the MCZ or Thioridazine hydrochloride (TZ, 12 and 16 mg/kg) treated group were red, those of a portion of the CXN treated group were red but most were milky white, and most were also milky white in the group treated with the combination of the three drugs.
Thioridazine purchased from MedChemExpress. Usage Cited in: Pol J Microbiol. 2019 Dec;68(4):477-491. [Abstract]
Colony counts from mice of the clinical strain MRSA135-infected group showed that the bacterial concentration was 6.96 × 107 CFU/ml without therapy. Following treatment, the bacterial concentration in mice of the MCZ-treatment group was 2.23 × 107 CFU/ml; in the Thioridazine hydrochloride (TZ, 4 μg/mL)-treatment group it was 1.73 × 107 CFU/ml; after CXN treatment it was 3.20 × 106 CFU/ml (p = 0.0447 < 0.05), and after the combination therapy with CXN, TZ, and MCZ it was 1.10 × 106 CFU/ml (p = 0.0427 < 0.05).
Thioridazine purchased from MedChemExpress. Usage Cited in: Pol J Microbiol. 2019 Dec;68(4):477-491. [Abstract]
The MICs values of individual antimicrobial agents against Staphylococcus aureus isolates.
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bioRxiv
2025 Nov 21:2025.11.20.689520. PMID: 41332603
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (282 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Tschanz JT, et, al. Atypical antipsychotic drugs block selective components of amphetamine-induced stereotypy. Pharmacol Biochem Behav. 1988 Nov;31(3):519-22. [Content Brief]
[2]. Mu J, et, al. Thioridazine, an antipsychotic drug, elicits potent antitumor effects in gastric cancer. Oncol Rep. 2014 May;31(5):2107-14. [Content Brief]
[3]. Kang S, et, al. Thioridazine induces apoptosis by targeting the PI3K/Akt/mTOR pathway in cervical and endometrial cancer cells. Apoptosis. 2012 Sep;17(9):989-97. [Content Brief]
[4]. Loehr AR, et, al. Targeting Cancer Stem Cells with Differentiation Agents as an Alternative to Genotoxic Chemotherapy for the Treatment of Malignant Testicular Germ Cell Tumors. Cancers (Basel). 2021 Apr 23;13(9):2045. [Content Brief]
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 |