Cat. No.: HY-A0077

Perphenazine

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.

For research use only. We do not sell to patients.

Purity: 99.81%
CAS No.: 58-39-9
Formula: C₂₁H₂₆ClN₃OS
Molecular Weight:403.97

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Perphenazine Chemical Structure

CAS No.: 58-39-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

5-HT_2A Receptor

D₂ Receptor

0.56 nM (Ki)

D₃ Receptor

0.43 nM (Ki)

D₄ Receptor

28.5 nM (Ki)

5-HT_2A Receptor

5.6 nM (Ki)

5-HT₆ Receptor

17 nM (Ki)

5-HT₇ Receptor

23 nM (Ki)

H₂ Receptor

132 nM (Ki)

5-HT_1A Receptor

421 nM (Ki)

All Dopamine Receptor Isoforms :

All Histamine Receptor Isoforms :

All 5-HT Receptor Isoforms :

All Adrenergic Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
AN3-CA	IC₅₀	25.4 μM Compound: PPZ	Antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human AN3CA cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
CHO-K1	IC₅₀	0.3 nM Compound: Perphenazine	Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay Antagonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 assessed as inhibition of agonist-induced response incubated for 60 mins in incubator followed by 15 mins at room temperature by FLIPR assay	[PMID: 23675993]
FL5.12	IC₅₀	4.8 μM Compound: 4	Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis Inhibition of protein phosphatase 2A in mouse FL5.12 cells assessed as reduction in cell viability incubated for 48 hrs by propidium iodide staining based flow cytometric analysis	[PMID: 31383588]
HEC-1-A	IC₅₀	23.3 μM Compound: PPZ	Antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human Hec1A cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
HEC-1B cell line	IC₅₀	29.8 μM Compound: PPZ	Antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human HEC1B cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
HUVEC	IC₅₀	97.76 μM Compound: Perphenazine	Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human HUVEC cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]
Ishikawa	IC₅₀	19.4 μM Compound: PPZ	Antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human Ishikawa cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
KLE	IC₅₀	30.8 μM Compound: PPZ	Antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay Antiproliferative activity against human KLE cells assessed as inhibition of cell viability by CCK8 assay	[PMID: 32527541]
L02	IC₅₀	>160 μM Compound: SYSU-20611S	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay	10.1039/C3MD00397C
MCF7	IC₅₀	35.81 μM Compound: Perphenazine	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	30.37 μM Compound: Perphenazine	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34435487]
MDA-MB-231	IC₅₀	31.77 μM Compound: Perphenazine	Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay Antiproliferative activity against human drug tolerant MDA-MB-231/lapatinib cells assessed as inhibition of cell growth in measured after 72 hrs by MTT assay	[PMID: 34435487]

In Vitro

Perphenazine (40 μM, 48 h) inhibits cell viability, and induces cell apoptosis mediated by CTSD (Cathepsin D) in L02 cells^[2].
Perphenazine (30 μM, 24 h) induces intense lysosome vacuolation, impaired lysosomal membrane, and induces lysosomal membrane permeabilization (LMP), ultimately triggering lysosomal cell death in L02 cells^[2].
Perphenazine (10-40 μM, 24 h) inhibits autophagic flux in L02 cells^[2].
Perphenazine (1 μM, 24 h) decreases glioblastoma U-87 MG cell migration and invasion^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:

L02 cells
Concentration:

10-100 μM
Incubation Time:

12, 24, 48 h
Result:

Inhibited cell viability in a concentration and time-dependent manner.

Western Blot Analysis^[2]

Cell Line:

L02 cells
Concentration:

10, 20, 30, and 40 μM
Incubation Time:

24 h
Result:

Increased LC3 I/II and P62/SQSTM1 levels

Cell Migration Assay ^[4]

Cell Line:

U-87 MG cells
Concentration:

1 µM
Incubation Time:

0, 3, 6, 9, 12, and 24 h
Result:

Increased the wound closure in human glioblastoma cell cultures from 24.6 to 62.7%.

In Vivo

Perphenazine (oral gavage, 180 mg/kg, every other day for 21 days) induces liver injury and lysosomal membrane damage in ICR mice^[2].
Perphenazine (oral administration, 10 mg/kg, every other day for 6 days) attenuates morphological phenotype in mouse models of Th2-type allergic dermatitis^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

ICR mice^[2]
Dosage:

10, 30, 60, 120, 180 mg/kg
Administration:

Oral gavage, every other day for 21 days.
Result:

Increased histological injury and aminotransferases compared with control.

Animal Model:

Oxazolone-treated animal model of dermatitis^[3]
Dosage:

10 mg/kg
Administration:

Oral administration, every other day for 6 days
Result:

Decreased The levels of mice ear swelling.

Chemical Information

CAS No. 58-39-9
Appearance Solid
Molecular Weight 403.97
Formula C₂₁H₂₆ClN₃OS
Color White to off-white
SMILES

OCCN1CCN(CCCN2C3=C(C=CC=C3)SC4=CC=C(Cl)C=C24)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (3)

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Journal Impact Factor

Adv Sci (Weinh)

Detachment-Induced FAK-STAT3-NNMT Inhibits CTCs Anoikis to Promote Breast Cancer Metastasis by Enhancing Fatty Acid Oxidation. [Abstract]

2026 Mar 12:e22837. PMID: 41816955
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Toxicol Lett

Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. [Abstract]

2022 Aug 15:367:76-87. PMID: 35914675

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (247.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4754 mL

12.3772 mL

24.7543 mL

5 mM

0.4951 mL

2.4754 mL

4.9509 mL

10 mM

0.2475 mL

1.2377 mL

2.4754 mL

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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.19 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.19 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.19 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Richtand NM, et al. Dopamine and serotonin receptor binding and antipsychotic efficacy. Neuropsychopharmacology. 2007 Aug;32(8):1715-26. [Content Brief]

[2]. Lei Tao, et al. Lysosomal membrane permeabilization mediated apoptosis involve in perphenazine-induced hepatotoxicity in vitro and in vivo. Toxicol Lett. 2022 Jul 29;367:76-87. [Content Brief]

[3]. Min-Jeong Heo, et al. Perphenazine Attenuates the Pro-Inflammatory Responses in Mouse Models of Th2-Type Allergic Dermatitis. Int J Mol Sci. 2020 May 3;21(9):3241. [Content Brief]

[4]. Michał Otręba, et al. Perphenazine and prochlorperazine decrease glioblastoma U-87 MG cell migration and invasion: Analysis of the ABCB1 and ABCG2 transporters, E-cadherin, α-tubulin and integrins (α3, α5, and β1) levels. Oncol Lett. 2022 Jun;23(6):182. [Content Brief]

[5]. Michał Otręba, et al. n vitro anticancer activity of fluphenazine, perphenazine and prochlorperazine. A review. J Appl Toxicol. 2021 Jan;41(1):82-94. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4754 mL	12.3772 mL	24.7543 mL	61.8858 mL
	5 mM	0.4951 mL	2.4754 mL	4.9509 mL	12.3772 mL
	10 mM	0.2475 mL	1.2377 mL	2.4754 mL	6.1886 mL
	15 mM	0.1650 mL	0.8251 mL	1.6503 mL	4.1257 mL
	20 mM	0.1238 mL	0.6189 mL	1.2377 mL	3.0943 mL
	25 mM	0.0990 mL	0.4951 mL	0.9902 mL	2.4754 mL
	30 mM	0.0825 mL	0.4126 mL	0.8251 mL	2.0629 mL
	40 mM	0.0619 mL	0.3094 mL	0.6189 mL	1.5471 mL
	50 mM	0.0495 mL	0.2475 mL	0.4951 mL	1.2377 mL
	60 mM	0.0413 mL	0.2063 mL	0.4126 mL	1.0314 mL
	80 mM	0.0309 mL	0.1547 mL	0.3094 mL	0.7736 mL
	100 mM	0.0248 mL	0.1238 mL	0.2475 mL	0.6189 mL

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Perphenazine

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

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Neurotransmitter Receptor Compound Library

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Anti-Alzheimer's Disease Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

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5-HT Receptor Compound Library

FDA-Approved Anticancer Drug Library

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Mass Spectrometry Human Metabolite Library

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Publications Citing Use of MedChemExpress (MCE) Perphenazine

All Dopamine Receptor Isoforms

All Histamine Receptor Isoforms

All 5-HT Receptor Isoforms

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Perphenazine Related Classifications

HY-A0077 Related Classifications