Pimozide | STAT5 inhibitor/Dopamine D2 antagonist

CAS:
 2062-78-4
Catalog Number:
 10-2780

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Pimozide (2062-78-4) is a potent antagonist of dopamine receptors D2, D3, and D4 receptors (Ki = 2.4, 0.3, and 1.8 nM, respectively), as well as the 5-HT7 receptor (Ki = 0.5 nM).1,2 At higher concentrations it blocks additional receptors (Ki = 18 – >10,000 nM) and ion channels (IC50 = 42 nM and higher).1-3 Pimozide has also been shown to be a novel tool for inhibiting STAT5, reducing the expression of STAT5 target genes and inhibiting STAT5 tyrosine phosphorylation (however it does not inhibit tyrosine kinases).4 It has become a useful and reliable tool for studying STAT5 signaling.5

References/Citations:

  1. Burstein et al. (2005) Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist; J.  Pharmacol. Exp. Ther. 315 1278
  2. Fukuyama et al. (2023) Therapeutic Potential and Limitation of Serotonin Type 7 Receptor Modulation; Int. J. Mol. Sci. 24 2070
  3. Roufos et al. (1996) A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers; J. Med. Chem. 39 1514
  4. Nelson et al. (2011) The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors; Blood 117 3421
  5. Liu et al. (2022) Targeting STAT5 Signaling Overcomes Resistance to IDH Inhibitors in Acute Myeloid Leukemia through Suppression of Stemness; Cancer Res. 82 4325
2062-78-4, Dopamine D2 antagonist, Pimozide, Pimozide supplier, R6238, STAT5 inhibitor
CAS:
2062-78-4
Catalog Number:
10-2780
Activity:
STAT5 inhibitor/Dopamine D2 antagonist
Chemical Names:
1-[1-[4,4-bis(4-Fluorophenyl)butyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one
Alternate Name:
R6238
Molecular Weight:
461.56
Molecular Formula:

C28H29F2N3O

Solubility:
Soluble in DMSO (30 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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Pimozide (2062-78-4) is a potent antagonist of dopamine receptors D2, D3, and D4 receptors (Ki = 2.4, 0.3, and 1.8 nM, respectively), as well as the 5-HT7 receptor (Ki = 0.5 nM).1,2 At higher concentrations it blocks additional receptors (Ki = 18 – >10,000 nM) and ion channels (IC50 = 42 nM and higher).1-3 Pimozide has also been shown to be a novel tool for inhibiting STAT5, reducing the expression of STAT5 target genes and inhibiting STAT5 tyrosine phosphorylation (however it does not inhibit tyrosine kinases).4 It has become a useful and reliable tool for studying STAT5 signaling.5

References/Citations:

  1. Burstein et al. (2005) Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: Identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist; J.  Pharmacol. Exp. Ther. 315 1278
  2. Fukuyama et al. (2023) Therapeutic Potential and Limitation of Serotonin Type 7 Receptor Modulation; Int. J. Mol. Sci. 24 2070
  3. Roufos et al. (1996) A structure-activity relationship study of novel phenylacetamides which are sodium channel blockers; J. Med. Chem. 39 1514
  4. Nelson et al. (2011) The STAT5 inhibitor pimozide decreases survival of chronic myelogenous leukemia cells resistant to kinase inhibitors; Blood 117 3421
  5. Liu et al. (2022) Targeting STAT5 Signaling Overcomes Resistance to IDH Inhibitors in Acute Myeloid Leukemia through Suppression of Stemness; Cancer Res. 82 4325

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