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324387

Sigma-Aldrich

Dopamine Receptor Antagonist II, Thioridazine, HCl

The Dopamine Receptor Antagonist II, Thioridazine, HCl, also referenced under CAS 130-61-0, controls the biological activity of Dopamine Receptor. This small molecule/inhibitor is primarily used for Biochemicals applications.

Synonym(s):

Dopamine Receptor Antagonist II, Thioridazine, HCl, 10-(2-(1-Methyl-2-piperidyl)ethyl)-2-(methylthio)-10H-phenothiazine, HCl, 10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylthio)-10H-phenothiazine, HCl

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About This Item

Empirical Formula (Hill Notation):
C21H26N2S2 · xHCl
CAS Number:
Molecular Weight:
370.57 (free base basis)
MDL number:
UNSPSC Code:
12352200

Quality Level

Assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

water: 25 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C21H26N2S2.ClH/c1-22-13-6-5-7-16(22)12-14-23-18-8-3-4-9-20(18)25-21-11-10-17(24-2)15-19(21)23;/h3-4,8-11,15-16H,5-7,12-14H2,1-2H3;1H

InChI key

NZFNXWQNBYZDAQ-UHFFFAOYSA-N

General description

A phenothiazine class antipsychotic and dopamine receptor (DR) antagonist that is reported to exhibit CSCs- (cancer stem cells) differentiating (EC50 ≤9.4 µM for v1H9) and anti-leukemic activity, without affecting non-neoplastic H9 hESC, adult fibroblast-derived iPSC, or HSPCs (hematopoietic stem-progenitor cells). However, Thioridazine′s high effective concentration (10 µM) against cancer cells suggests that other unidentified cellular targets/mechanisms in addition to DR antagonism may be also involved in its overall anti-CSC impact. Effectively augments AraC (Cat. No. 251010) in inhibiting primary AML in vitro colony formation (by 79%, 55%, and 100%, respectively, with 10 µM Thioridazine, 0.1 µM AraC, or a combination of both).
A phenothiazine class dopamine receptor (DR) antagonist that, in addition to its well known clinical use as an antipsychotic for schizophrenia treatment, is also reported to selectively induce the differentiation of neoplastic v1H9 (EC50 ≤9.4 µM in Oct4-GFP reporter assay) and v2H9, but not their parent non-neoplastic H9 hESC or adult fibroblast-derived iPSC. Both Thioridazine′s CSCs- (cancer stem cells) selective differentiation effect and anti-leukemic activity correlate well with the selective DR expression on CSCs and AML cells, but not H9, iPSC, normal HSCs (hematopoietic stem cells) or HSPCs (hematopoietic stem-progenitor cells). However, Thioridazine′s high effective concentration (10 µM) against cancer cells suggests that other unidentified cellular targets/mechanisms in addition to DR antagonism are involved in its overall anti-CSC impact. Effectively augments AraC (Cat. No. 251010) in inhibiting primary AML in vitro colony formation (by 79%, 55%, and 100%, respectively, with 10 µM Thioridazine, 0.1 µM AraC, or a combination of both) without exerting cytotoxic effect on normal HSPCs.

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

Sachlos, E., et al. 2012. Cell149, 1284.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Precautionary Statements

Hazard Classifications

Acute Tox. 4 Oral

Storage Class Code

11 - Combustible Solids

WGK

WGK 3


Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

JAN Code

324387-GM:
324387-2GM:


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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