Pimozide

Catalog No.S4358 Batch:S435803

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Technical Data

Formula

C28H29F2N3O
Molecular Weight 461.55 CAS No. 2062-78-4
Solubility (25°C)* In vitro DMSO 31 mg/mL (67.16 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Targets
STAT3 [1] STAT5 [2] Dopamine D3 receptor [3]
(Cell-free assay)		 Dopamine D2 receptor [3]
(Cell-free assay)		 α1-adrenoceptor [3]
(Cell-free assay)		 View More
0.83 nM(Ki) 3.0 nM(Ki) 39 nM(Ki)
In vitro

Pimozide, a STAT5 inhibitor, has no effect on prolactin-induced ERα phosphorylation.[4]

Protocol (from reference)

Cell Assay:

[4]
  • Cell lines

    MMQ rat prolactinoma cell line

  • Concentrations

    5 µM

  • Incubation Time

    --

  • Method

    MMQ cells were treated with PRL (20 ng/ml) in the absence and presence of the JAK2 inhibitor AG-490 (50 μM), the PI3K inhibitor wortmannin (0.5 µM), the MEK inhibitor U0126 (10 µM) or the STAT5 inhibitor pimozide (5 µM).

    (Data sourced from selleck products)

Selleck's Pimozide has been cited by 2 publications

A combinatorial therapeutic approach to enhance FLT3-ITD AML treatment [ Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286] PubMed: 37951217
RSK inhibition induces apoptosis by downregulating protein synthesis in a variety of acute myeloid leukemia cell lines [ Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531] PubMed: 34602526

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.