2. GPCR/G Protein Neuronal Signaling Apoptosis Autophagy Anti-infection
  3. Dopamine Receptor Apoptosis 5-HT Receptor Autophagy Bacterial
  4. 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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Based on 4 publication(s) in Google Scholar

Other Forms of Thioridazine:

Thioridazine Related Antibodies

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  • Biological Activity

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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.

Thioridazine Related Antibodies

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Thioridazine Related Classifications

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Help & FAQs
  • 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.

Keywords:

Thioridazine50-52-2Dopamine ReceptorApoptosis5-HT ReceptorAutophagyBacterialSerotonin Receptor5-hydroxytryptamine ReceptorD2antipsychoticantianxietyPI3KAktmTORapoptosiscancerCSCInhibitorinhibitorinhibit

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